Quetiapine
Explore a selection of our essential drug information below, or:
Identification
- Summary
Quetiapine is an atypical antipsychotic agent used for the management of bipolar disorder, schizophrenia, and major depressive disorder.
- Brand Names
- Seroquel
- Generic Name
- Quetiapine
- DrugBank Accession Number
- DB01224
- Background
Initially approved by the FDA in 1997, quetiapine is a second-generation atypical antipsychotic used in schizophrenia, major depression, and bipolar disorder.19 Quetiapine demonstrates a high level of therapeutic efficacy and low risk of adverse effects during long-term treatment. It is well-tolerated and a suitable option for some patients with high sensitivity to other drugs, such as clozapine and olanzapine.1
- Type
- Small Molecule
- Groups
- Approved
- Structure
- Weight
- Average: 383.507
Monoisotopic: 383.166747749 - Chemical Formula
- C21H25N3O2S
- Synonyms
- 2-[2-(4-Dibenzo[b,f][1,4]thiazepin-11-yl-1-piperazinyl)ethoxy]ethanol
- Quetiapina
- Quétiapine
- Quetiapine
- Quetiapinum
Pharmacology
- Indication
Quetiapine is used in the symptomatic treatment of schizophrenia. In addition, it may be used for the management of acute manic or mixed episodes in patients with bipolar I disorder, as a monotherapy or combined with other drugs. It may be used to manage depressive episodes in bipolar disorder. In addition to the above indications, quetiapine is used in combination with antidepressant drugs for the treatment of major depression.19
Some off-label uses for this drug include the management of post-traumatic stress disorder (PTSD), generalized anxiety disorder, and psychosis associated with Parkinson's disease.7,10,18
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Adjunct therapy in management of Bipolar 1 disorder •••••••••••• ••••••• ••••••• •••••••• •••••••• ••••••• •••• ••••••• ••••••• •••• ••••••• •••••••• •••••••• ••••••• ••••••••••• •••••••• ••••••• Adjunct therapy in management of Bipolar 1 disorder •••••••••••• ••••••• •••••••• •••••••• ••••••• •••• ••••••• •••••••• •••••••• ••••••• ••••••••••• •••••••• •••••••• ••••••• ••••••• •••• •••••• Management of Generalized anxiety disorder ••• ••••• Adjunct therapy in treatment of Major depressive disorders •••••••••••• ••••••• •••••••• •••••••• ••••••• •••• ••••••• •••••••• •••••••• ••••••• ••••••••••• •••••••• ••••••• Treatment of Manic episode •••••••••••• ••••••• ••••••• •••••••• •••••••• ••••••• •••• ••••••• ••••••• •••• ••••••• •••••••• •••••••• ••••••• ••••••••••• •••••••• ••••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
Quetiapine improves the positive and negative symptoms of schizophrenia and major depression by acting on various neurotransmitter receptors, such as the serotonin and dopamine receptors. In bipolar disorder, it improves both depressive and manic symptoms.1,8,9
A note on suicidality in young patients and administration in the elderly
Quetiapine can cause suicidal thinking or behavior in children and adolescents and should not be given to children under 10 years of age. It is important to monitor for suicidality if this drug is given to younger patients. In addition, this drug is not indicated for the treatment of psychosis related to dementia due to an increased death rate in elderly patients taking this drug.19
- Mechanism of action
Although the mechanism of action of quetiapine is not fully understood, several proposed mechanisms exist. In schizophrenia, its actions could occur from the antagonism of dopamine type 2 (D2) and serotonin 2A (5HT2A) receptors. In bipolar depression and major depression, quetiapine's actions may be attributed to the binding of this drug or its metabolite to the norepinephrine transporter. Additional effects of quetiapine, including somnolence, orthostatic hypotension, and anticholinergic effects, may result from the antagonism of H1 receptors, adrenergic α1 receptors, and muscarinic M1 receptors, respectively.1,7,19
- Absorption
Quetiapine is rapidly and well absorbed after administration of an oral dose.21 Steady-state is achieved within 48 hours 15 and peak plasma concentrations are achieved within 1.5 hours.21 The steady-state Cmax of quetiapine in Han Chinese patients with schizophrenia after a 300 mg oral dose of the extended released formulation was approximately 467 ng/mL and the AUC at steady-state was 5094 ng·h/mL.17 While the absolute bioavailability has not been fully elucidated and is reported to be low,5 the tablet formulation is 100% bioavailable relative to solution.21 Absorption of quetiapine is affected by food, with Cmax increased by 25% and AUC increased by 15%.21
- Volume of distribution
Quetiapine distributes throughout body tissues. The apparent volume of distribution of this drug is about 10±4 L/kg.19
- Protein binding
- Metabolism
The metabolism of quetiapine occurs mainly in the liver. Sulfoxidation and oxidation are the main metabolic pathways of this drug. According to in vitro studies, cytochrome P450 3A4 metabolizes quetiapine to an inactive sulfoxide metabolite and also participates in the metabolism of its active metabolite, N-desalkyl quetiapine. CYP2D6 also regulates the metabolism of quetiapine. In one study, three metabolites of N-desalkylquetiapine were identified. Two of the metabolites were identified as N-desalkylquetiapine sulfoxide and 7-hydroxy-N-desalkylquetiapine. CYP2D6 has been found to be responsible for metabolism of quetiapine to 7-hydroxy-N-desalkylquetiapine, a pharmacologically active metabolite. Individual differences in CYP2D6 metabolism may be present, which may affect the concentrations of the active metabolite.4,11,19
Hover over products below to view reaction partners
- Route of elimination
After an oral dose of radiolabeled quetiapine, less than 1% of unchanged drug was detected in the urine8, suggesting that quetiapine is heavily metabolized. About 73% of a dose was detected in the urine, and about 20% in the feces.5,19
- Half-life
The average terminal half-life of quetiapine is about 6-7 hours.8,19
- Clearance
The clearance of quetiapine healthy volunteers in the fasted state during a clinical study was 101.04±39.11 L/h.16 Elderly patients may require lower doses of quetiapine, as clearance in these patients may be reduced by up to 50%.19 Those with liver dysfunction may also require lower doses.14
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
The oral LD50 if quetiapine in rats is 2000 mg/kg.20
Overdose information
Some signs and symptoms of a quetiapine overdose include sedation, drowsiness, tachycardia, and hypotension. Clinical trials demonstrate that overdoses of up to 30 grams of quetiapine did not result in death. A lethal outcome was reported in a clinical trial after an overdose of 13.6 grams of quetiapine. In the case of an acute overdose, ensure to maintain an airway and provide adequate ventilation and oxygenation. Gastric lavage following intubation (if necessary) along with activated charcoal and a laxative may be considered. The possibility of obtundation, seizure or dystonic reaction of the head and neck following overdose may create a risk of aspiration with induced emesis. Cardiac monitoring should also take place.19
A note on QT-interval prolongation in an overdose
Postmarketing reports reveal increases in the cardiac QT interval in cases of quetiapine overdose, concomitant illness, and in those taking drugs that increase QT interval or affect electrolyte levels.19 Note that disopyramide, procainamide, and quinidine may exert additive QT-prolonging effects when administered in patients who have overdosed with quetiapine, and should be avoided.12,13,19
- Pathways
Pathway Category Quetiapine H1-Antihistamine Action Drug action - Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Quetiapine is combined with 1,2-Benzodiazepine. Abacavir Abacavir may decrease the excretion rate of Quetiapine which could result in a higher serum level. Abaloparatide The risk or severity of adverse effects can be increased when Quetiapine is combined with Abaloparatide. Abametapir The serum concentration of Quetiapine can be increased when it is combined with Abametapir. Abatacept The metabolism of Quetiapine can be increased when combined with Abatacept. - Food Interactions
- Avoid alcohol.
- Take with or without food. If taken with food, take with a light meal.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key Quetiapine fumarate 2S3PL1B6UJ 111974-72-2 ZTHJULTYCAQOIJ-WXXKFALUSA-N - Product Images
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Act Quetiapine Tablet 150 mg Oral TEVA Canada Limited Not applicable Not applicable Canada Act Quetiapine Tablet 100 mg Oral TEVA Canada Limited 2008-09-04 Not applicable Canada Act Quetiapine Tablet 300 mg Oral TEVA Canada Limited 2008-09-04 Not applicable Canada Act Quetiapine Tablet 25 mg Oral TEVA Canada Limited 2008-09-04 Not applicable Canada Act Quetiapine Tablet 200 mg Oral TEVA Canada Limited 2008-09-04 Not applicable Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Abbott-quetiapine Tablet, multilayer, extended release 25 mg Oral Bgp Pharma Ulc 2014-06-09 2015-12-31 Canada Abbott-quetiapine Tablet, multilayer, extended release 100 mg Oral Bgp Pharma Ulc 2014-06-09 2015-12-31 Canada Abbott-quetiapine Tablet, multilayer, extended release 200 mg Oral Bgp Pharma Ulc 2014-06-13 2015-12-31 Canada Abbott-quetiapine Tablet, multilayer, extended release 300 mg Oral Bgp Pharma Ulc 2014-06-09 2015-12-31 Canada Accel-quetiapine Tablet 25 mg Oral Accel Pharma Inc 2015-03-26 2017-01-27 Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image QUETAMED Quetiapine (25 MG) + Quetiapine (100 MG) + Quetiapine (200 MG) Tablet, coated Oral Fairmed Healthcare Gmbh 2014-07-08 Not applicable Italy QUETAMED Quetiapine (25 MG) + Quetiapine (100 MG) + Quetiapine (200 MG) Tablet, coated Oral Fairmed Healthcare Gmbh 2014-07-08 Not applicable Italy QUETAMED Quetiapine (25 MG) + Quetiapine (100 MG) + Quetiapine (200 MG) Tablet, coated Oral Fairmed Healthcare Gmbh 2014-07-08 Not applicable Italy Quetialan 4 Tage Startpackung - Filmtabletten Quetiapine fumarate (25 mg) + Quetiapine fumarate (100 mg) Kit; Tablet, film coated Oral G.L. Pharma Gmb H 2007-08-28 Not applicable Austria Quetialan 4 Tage Startpackung - Filmtabletten Quetiapine fumarate (25 mg) + Quetiapine fumarate (100 mg) Kit; Tablet, film coated Oral G.L. Pharma Gmb H 2007-08-28 Not applicable Austria
Categories
- ATC Codes
- N05AH04 — Quetiapine
- Drug Categories
- Adrenergic alpha-1 Receptor Antagonists
- Adrenergic alpha-Antagonists
- Adrenergic Antagonists
- Agents producing tachycardia
- Agents that produce hypertension
- Anticholinergic Agents
- Antidepressive Agents
- Antidepressive Agents Indicated for Depression
- Antipsychotic Agents
- Antipsychotic Agents (Second Generation [Atypical])
- Azepines
- Central Nervous System Agents
- Central Nervous System Depressants
- Cytochrome P-450 CYP2C19 Substrates
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 CYP3A7 Substrates
- Cytochrome P-450 Substrates
- Diazepines, Oxazepines, Thiazepines and Oxepines
- Dibenzothiazepines
- Dopamine Antagonists
- Dopamine D2 Receptor Antagonists
- Drugs that are Mainly Renally Excreted
- Heterocyclic Compounds, Fused-Ring
- Histamine Antagonists
- Histamine H1 Antagonists
- Hyperglycemia-Associated Agents
- Hypotensive Agents
- Moderate Risk QTc-Prolonging Agents
- Muscarinic Antagonists
- Nervous System
- P-glycoprotein substrates
- Psycholeptics
- Psychotropic Drugs
- QTc Prolonging Agents
- Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
- Serotonin 5-HT1 Receptor Antagonists
- Serotonin 5-HT1A Receptor Antagonists
- Serotonin 5-HT2 Receptor Antagonists
- Serotonin 5-HT2A Receptor Antagonists
- Serotonin Agents
- Serotonin Receptor Antagonists
- Thiazepines
- Thiepins
- Tranquilizing Agents
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as dibenzothiazepines. These are compounds containing a dibenzothiazepine moiety, which consists of two benzene connected by a thiazepine ring.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Benzothiazepines
- Sub Class
- Dibenzothiazepines
- Direct Parent
- Dibenzothiazepines
- Alternative Parents
- Diarylthioethers / N-alkylpiperazines / Imidolactams / Benzenoids / Trialkylamines / Propargyl-type 1,3-dipolar organic compounds / Dialkyl ethers / Carboxamidines / Azacyclic compounds / Primary alcohols show 2 more
- Substituents
- 1,4-diazinane / Alcohol / Amidine / Amine / Aromatic heteropolycyclic compound / Aryl thioether / Azacycle / Benzenoid / Carboxylic acid amidine / Dialkyl ether show 18 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- N-arylpiperazine, N-alkylpiperazine, dibenzothiazepine (CHEBI:8707)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- BGL0JSY5SI
- CAS number
- 111974-69-7
- InChI Key
- URKOMYMAXPYINW-UHFFFAOYSA-N
- InChI
- InChI=1S/C21H25N3O2S/c25-14-16-26-15-13-23-9-11-24(12-10-23)21-17-5-1-3-7-19(17)27-20-8-4-2-6-18(20)22-21/h1-8,25H,9-16H2
- IUPAC Name
- 2-[2-(4-{2-thia-9-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(15),3,5,7,9,11,13-heptaen-10-yl}piperazin-1-yl)ethoxy]ethan-1-ol
- SMILES
- OCCOCCN1CCN(CC1)C1=NC2=CC=CC=C2SC2=CC=CC=C12
References
- Synthesis Reference
Kansal VK., Lal K.Suhail, Leonov AD.,(2006).US7687622B2.Retrieved from https://patents.google.com/patent/US7687622B2/en
US4879288- General References
- Dev V, Raniwalla J: Quetiapine: a review of its safety in the management of schizophrenia. Drug Saf. 2000 Oct;23(4):295-307. [Article]
- Mukaddes NM, Abali O: Quetiapine treatment of children and adolescents with Tourette's disorder. J Child Adolesc Psychopharmacol. 2003 Fall;13(3):295-9. [Article]
- Tallerico T, Novak G, Liu IS, Ulpian C, Seeman P: Schizophrenia: elevated mRNA for dopamine D2(Longer) receptors in frontal cortex. Brain Res Mol Brain Res. 2001 Mar 5;87(2):160-5. [Article]
- Urichuk L, Prior TI, Dursun S, Baker G: Metabolism of atypical antipsychotics: involvement of cytochrome p450 enzymes and relevance for drug-drug interactions. Curr Drug Metab. 2008 Jun;9(5):410-8. [Article]
- DeVane CL, Nemeroff CB: Clinical pharmacokinetics of quetiapine: an atypical antipsychotic. Clin Pharmacokinet. 2001;40(7):509-22. doi: 10.2165/00003088-200140070-00003. [Article]
- McConville BJ, Arvanitis LA, Thyrum PT, Yeh C, Wilkinson LA, Chaney RO, Foster KD, Sorter MT, Friedman LM, Brown KL, Heubi JE: Pharmacokinetics, tolerability, and clinical effectiveness of quetiapine fumarate: an open-label trial in adolescents with psychotic disorders. J Clin Psychiatry. 2000 Apr;61(4):252-60. doi: 10.4088/jcp.v61n0403. [Article]
- Maneeton N, Maneeton B, Woottiluk P, Likhitsathian S, Suttajit S, Boonyanaruthee V, Srisurapanont M: Quetiapine monotherapy in acute treatment of generalized anxiety disorder: a systematic review and meta-analysis of randomized controlled trials. Drug Des Devel Ther. 2016 Jan 12;10:259-76. doi: 10.2147/DDDT.S89485. eCollection 2016. [Article]
- Muneer A: Pharmacotherapy of bipolar disorder with quetiapine: a recent literature review and an update. Clin Psychopharmacol Neurosci. 2015 Apr 30;13(1):25-35. doi: 10.9758/cpn.2015.13.1.25. [Article]
- Suttajit S, Srisurapanont M, Maneeton N, Maneeton B: Quetiapine for acute bipolar depression: a systematic review and meta-analysis. Drug Des Devel Ther. 2014 Jun 25;8:827-38. doi: 10.2147/DDDT.S63779. eCollection 2014. [Article]
- Shotbolt P, Samuel M, David A: Quetiapine in the treatment of psychosis in Parkinson's disease. Ther Adv Neurol Disord. 2010 Nov;3(6):339-50. doi: 10.1177/1756285610389656. [Article]
- Bakken GV, Molden E, Knutsen K, Lunder N, Hermann M: Metabolism of the active metabolite of quetiapine, N-desalkylquetiapine in vitro. Drug Metab Dispos. 2012 Sep;40(9):1778-84. doi: 10.1124/dmd.112.045237. Epub 2012 Jun 11. [Article]
- Beelen AP, Yeo KT, Lewis LD: Asymptomatic QTc prolongation associated with quetiapine fumarate overdose in a patient being treated with risperidone. Hum Exp Toxicol. 2001 Apr;20(4):215-9. doi: 10.1191/096032701678766778. [Article]
- Gajwani P, Pozuelo L, Tesar GE: QT interval prolongation associated with quetiapine (Seroquel) overdose. Psychosomatics. 2000 Jan-Feb;41(1):63-5. doi: 10.1016/S0033-3182(00)71175-3. [Article]
- Riedel M, Muller N, Strassnig M, Spellmann I, Severus E, Moller HJ: Quetiapine in the treatment of schizophrenia and related disorders. Neuropsychiatr Dis Treat. 2007 Apr;3(2):219-35. doi: 10.2147/nedt.2007.3.2.219. [Article]
- Li KY, Li X, Cheng ZN, Peng WX, Zhang BK, Li HD: Multiple dose pharmacokinetics of quetiapine and some of its metabolites in Chinese suffering from schizophrenia. Acta Pharmacol Sin. 2004 Mar;25(3):390-4. [Article]
- Huang X, Zhang S, Ma Y, Yang H, He C, Tian R, Mei H, Liu L, Zhang B: Bioequivalence of two quetiapine extended release tablets in Chinese healthy volunteers under fasting and fed conditions and effects of food on pharmacokinetic profiles. Drug Des Devel Ther. 2018 Dec 31;13:255-264. doi: 10.2147/DDDT.S182965. eCollection 2019. [Article]
- Li Q, Su YA, Liu Y, Chen JX, Tan YL, Yang FD, Si TM: Pharmacokinetics and tolerability of extended-release quetiapine fumarate in Han Chinese patients with schizophrenia. Clin Pharmacokinet. 2014 May;53(5):455-65. doi: 10.1007/s40262-013-0127-9. [Article]
- Jasdave S. Maan; Abdolreza Saadabadi (2019). Quetiapine. Stat Pearls Publishing.
- Quetiapine fumarate fda label [Link]
- AstraZeneca SDS: Quetiapine [Link]
- FDA Approved Drug Products: SEROQUEL (quetiapine) tablets, for oral use (January 2022) [Link]
- External Links
- Human Metabolome Database
- HMDB0005021
- KEGG Drug
- D08456
- KEGG Compound
- C07397
- PubChem Compound
- 5002
- PubChem Substance
- 46504800
- ChemSpider
- 4827
- BindingDB
- 50095890
- 51272
- ChEBI
- 8707
- ChEMBL
- CHEMBL716
- ZINC
- ZINC000019632628
- Therapeutic Targets Database
- DAP000001
- PharmGKB
- PA451201
- Guide to Pharmacology
- GtP Drug Page
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Quetiapine
- FDA label
- Download (273 KB)
- MSDS
- Download (57.1 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Completed Not Available Bipolar Disorder (BD) 4 somestatus stop reason just information to hide Not Available Completed Not Available Bipolar Disorder (BD) / Depression 1 somestatus stop reason just information to hide Not Available Completed Not Available Bipolar Disorder (BD) / Psychosis / Schizoaffective Disorders / Schizophrenia / Type 2 Diabetes Mellitus 1 somestatus stop reason just information to hide Not Available Completed Not Available Bipolar Disorder (BD) / Psychosis / Syndrome, Metabolic 1 somestatus stop reason just information to hide Not Available Completed Not Available Schizophrenia 4 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Advanced Pharmaceutical Services Inc.
- AQ Pharmaceuticals Inc.
- A-S Medication Solutions LLC
- AstraZeneca Inc.
- Atlantic Biologicals Corporation
- Bryant Ranch Prepack
- Cardinal Health
- Comprehensive Consultant Services Inc.
- Coupler Enterprises Inc.
- Direct Dispensing Inc.
- Heartland Repack Services LLC
- Innoviant Pharmacy Inc.
- Lake Erie Medical and Surgical Supply
- Murfreesboro Pharmaceutical Nursing Supply
- Neuman Distributors Inc.
- Norwich Pharmaceuticals Inc.
- Nucare Pharmaceuticals Inc.
- PD-Rx Pharmaceuticals Inc.
- Physicians Total Care Inc.
- Prepackage Specialists
- Prepak Systems Inc.
- Rebel Distributors Corp.
- Remedy Repack
- Resource Optimization and Innovation LLC
- Southwood Pharmaceuticals
- Tya Pharmaceuticals
- Vangard Labs Inc.
- Wyeth Pharmaceuticals
- Dosage Forms
Form Route Strength Tablet, multilayer, extended release Oral 150 mg Tablet Oral 115.120 mg Tablet Oral 28.780 mg Tablet Oral 57.566 mg Tablet, coated Oral Tablet, coated Oral 345.4 mg Capsule, liquid filled Oral 25 mg Capsule, liquid filled Oral 300 mg Tablet, film coated Oral 25 mg Tablet Oral 28.750 mg Tablet Oral 28.783 mg Tablet Oral 100.000 mg Tablet Oral 50 mg Tablet Oral 300.000 mg Tablet Oral 50.000 mg Tablet, coated Oral 2500000 mg Tablet, coated Oral 20000000 mg Tablet, coated Oral Tablet, extended release Oral Kit; tablet, film coated Oral Tablet, film coated Oral 150 MG Tablet, film coated Oral Tablet, film coated Oral 400 MG Tablet, film coated Oral 50 MG Tablet, extended release Oral 600 MG Tablet, film coated Oral 10000000 mg Tablet, coated Oral 28.78 mg Tablet, coated Oral 230.265 mg Tablet Oral 100 mg/1 Tablet Oral 150 mg/1 Tablet Oral 200 mg/1 Tablet Oral 25 mg/1 Tablet Oral 300 mg/1 Tablet Oral 400 mg/1 Tablet Oral 50 mg/1 Tablet, extended release Oral 230270 Mg Tablet, film coated Oral 115120 MG Tablet, film coated Oral 150 mg/1 Tablet, film coated Oral 230240 MG Tablet, film coated Oral 28780 MG Tablet, film coated Oral 345360 Mg Tablet, film coated, extended release Oral 150 mg/1 Tablet, film coated, extended release Oral 200 mg/1 Tablet, film coated, extended release Oral 300 mg/1 Tablet, film coated, extended release Oral 400 mg/1 Tablet, film coated, extended release Oral 50 mg/1 Tablet Oral 20000000 mg Tablet, coated Oral 10000000 mg Tablet Oral 25.000 mg Tablet Oral 100.00 mg Tablet, film coated Oral 100 mg/1 Tablet, film coated Oral 115.13 mg Tablet, film coated Oral 200 mg/1 Tablet, film coated Oral 230.26 mg Tablet, film coated Oral 25 mg/1 Tablet, film coated Oral 28.72 mg Tablet, film coated Oral 300 mg/1 Tablet, film coated Oral 345.39 mg Tablet, film coated Oral 400 mg/1 Tablet, film coated Oral 50 mg/1 Tablet, multilayer, extended release Oral 100 mg Tablet, multilayer, extended release Oral 150 mg / tab Tablet, multilayer, extended release Oral 200 mg Tablet, multilayer, extended release Oral 25 mg Tablet, multilayer, extended release Oral 300 mg Tablet, film coated Oral Tablet, film coated Oral 100 mg Tablet, film coated Oral 300 mg Tablet Oral Tablet Oral 150.000 mg Tablet, extended release Oral 150 mg/1 Tablet, extended release Oral 200 mg/1 Tablet, extended release Oral 300 mg/1 Tablet, extended release Oral 400 mg/1 Tablet, extended release Oral 50 mg/1 Tablet Oral 400 mg Tablet, film coated, extended release Oral 400 mg Tablet, extended release Oral 230 MG Tablet, extended release Oral 345 MG Tablet, extended release Oral 460 MG Tablet, extended release Oral 200 mg Tablet, film coated, extended release Oral 200 mg Tablet, film coated, extended release Oral 300 mg Tablet, film coated, extended release Oral 50 mg Tablet Oral 100 mg Tablet Oral 150 mg Tablet Oral 200 mg Tablet Oral 25 mg Tablet Oral 300 mg Tablet, film coated Oral 200 mg Tablet Oral 50.0000 mg Tablet, coated Oral 300 mg Tablet, coated Oral 100 mg Tablet, coated Oral 200 mg Tablet, coated Oral 25 mg Tablet, extended release Oral 150 mg Tablet, extended release Oral 300 mg Tablet, extended release Oral 400 mg Tablet, extended release Oral 50 mg - Prices
Unit description Cost Unit Seroquel 400 mg tablet 16.71USD tablet Seroquel xr 400 mg tablet 14.82USD tablet Seroquel 300 mg tablet 14.21USD tablet Seroquel xr 300 mg tablet 12.61USD tablet Seroquel 200 mg tablet 10.84USD tablet SEROquel XR 200 mg 24 Hour tablet 10.0USD tablet Seroquel xr 200 mg tablet 9.62USD tablet SEROquel XR 150 mg 24 Hour tablet 9.09USD tablet Seroquel xr 150 mg tablet 8.74USD tablet Seroquel 100 mg tablet 5.75USD tablet Seroquel 50 mg tablet 5.5USD tablet SEROquel XR 50 mg 24 Hour tablet 5.06USD tablet Seroquel xr 50 mg tablet 4.87USD tablet Seroquel 300 mg Tablet 4.35USD tablet Seroquel 25 mg tablet 3.35USD tablet Seroquel 200 mg Tablet 2.98USD tablet Apo-Quetiapine 300 mg Tablet 2.44USD tablet Co Quetiapine 300 mg Tablet 2.44USD tablet Jamp-Quetiapine 300 mg Tablet 2.44USD tablet Mylan-Quetiapine 300 mg Tablet 2.44USD tablet Novo-Quetiapine 300 mg Tablet 2.44USD tablet Pms-Quetiapine 300 mg Tablet 2.44USD tablet Ratio-Quetiapine 300 mg Tablet 2.44USD tablet Sandoz Quetiapine 300 mg Tablet 2.44USD tablet Apo-Quetiapine 200 mg Tablet 1.67USD tablet Co Quetiapine 200 mg Tablet 1.67USD tablet Jamp-Quetiapine 200 mg Tablet 1.67USD tablet Mylan-Quetiapine 200 mg Tablet 1.67USD tablet Novo-Quetiapine 200 mg Tablet 1.67USD tablet Pms-Quetiapine 200 mg Tablet 1.67USD tablet Ratio-Quetiapine 200 mg Tablet 1.67USD tablet Sandoz Quetiapine 200 mg Tablet 1.67USD tablet Seroquel 100 mg Tablet 1.48USD tablet Novo-Quetiapine 150 mg Tablet 1.42USD tablet Apo-Quetiapine 100 mg Tablet 0.83USD tablet Co Quetiapine 100 mg Tablet 0.83USD tablet Jamp-Quetiapine 100 mg Tablet 0.83USD tablet Mylan-Quetiapine 100 mg Tablet 0.83USD tablet Novo-Quetiapine 100 mg Tablet 0.83USD tablet Pms-Quetiapine 100 mg Tablet 0.83USD tablet Ratio-Quetiapine 100 mg Tablet 0.83USD tablet Sandoz Quetiapine 100 mg Tablet 0.83USD tablet Seroquel 25 mg Tablet 0.56USD tablet Apo-Quetiapine 25 mg Tablet 0.31USD tablet Co Quetiapine 25 mg Tablet 0.31USD tablet Jamp-Quetiapine 25 mg Tablet 0.31USD tablet Mylan-Quetiapine 25 mg Tablet 0.31USD tablet Novo-Quetiapine 25 mg Tablet 0.31USD tablet Pms-Quetiapine 25 mg Tablet 0.31USD tablet Ratio-Quetiapine 25 mg Tablet 0.31USD tablet Sandoz Quetiapine 25 mg Tablet 0.31USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US4879288 No 1989-11-07 2011-09-26 US CA2251944 No 2007-04-10 2017-05-27 Canada US5948437 Yes 1999-09-07 2017-11-28 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 174-176 https://www.chemicalbook.com/ChemicalProductProperty_US_CB9270451.aspx boiling point (°C) 556.5±60.0 http://www.chemspider.com/Chemical-Structure.4827.html logP 2.81 http://www.t3db.ca/toxins/T3D2555 logS -4 http://www.t3db.ca/toxins/T3D2555 pKa 7.06 http://www.t3db.ca/toxins/T3D2555 - Predicted Properties
Property Value Source Water Solubility 0.0403 mg/mL ALOGPS logP 2.93 ALOGPS logP 2.81 Chemaxon logS -4 ALOGPS pKa (Strongest Acidic) 15.12 Chemaxon pKa (Strongest Basic) 7.06 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 48.3 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 114.09 m3·mol-1 Chemaxon Polarizability 42.78 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9155 Blood Brain Barrier + 0.9906 Caco-2 permeable - 0.6037 P-glycoprotein substrate Substrate 0.8424 P-glycoprotein inhibitor I Inhibitor 0.9117 P-glycoprotein inhibitor II Inhibitor 0.9325 Renal organic cation transporter Inhibitor 0.5554 CYP450 2C9 substrate Non-substrate 0.6438 CYP450 2D6 substrate Substrate 0.8919 CYP450 3A4 substrate Non-substrate 0.6049 CYP450 1A2 substrate Inhibitor 0.5744 CYP450 2C9 inhibitor Non-inhibitor 0.6305 CYP450 2D6 inhibitor Inhibitor 0.588 CYP450 2C19 inhibitor Non-inhibitor 0.7033 CYP450 3A4 inhibitor Inhibitor 0.7961 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.5375 Ames test Non AMES toxic 0.7479 Carcinogenicity Non-carcinogens 0.869 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.6537 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9483 hERG inhibition (predictor II) Inhibitor 0.8684
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 202.7059893 predictedDarkChem Lite v0.1.0 [M-H]- 182.08702 predictedDeepCCS 1.0 (2019) [M+H]+ 202.2814893 predictedDarkChem Lite v0.1.0 [M+H]+ 184.44502 predictedDeepCCS 1.0 (2019) [M+Na]+ 202.9761893 predictedDarkChem Lite v0.1.0 [M+Na]+ 190.53816 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin) (PubMed:1330647, PubMed:18703043, PubMed:19057895). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD) (PubMed:28129538). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors (PubMed:28129538). Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways (PubMed:28129538). Signaling activates phospholipase C and a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and promotes the release of Ca(2+) ions from intracellular stores (PubMed:18703043, PubMed:28129538). Affects neural activity, perception, cognition and mood (PubMed:18297054). Plays a role in the regulation of behavior, including responses to anxiogenic situations and psychoactive substances. Plays a role in intestinal smooth muscle contraction, and may play a role in arterial vasoconstriction
- Specific Function
- 1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding
- Gene Name
- HTR2A
- Uniprot ID
- P28223
- Uniprot Name
- 5-hydroxytryptamine receptor 2A
- Molecular Weight
- 52602.58 Da
References
- Goldstein JM: Quetiapine fumarate (Seroquel): a new atypical antipsychotic. Drugs Today (Barc). 1999 Mar;35(3):193-210. [Article]
- McIntyre RS, Soczynska JK, Woldeyohannes HO, Alsuwaidan M, Konarski JZ: A preclinical and clinical rationale for quetiapine in mood syndromes. Expert Opin Pharmacother. 2007 Jun;8(9):1211-9. [Article]
- Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
- Yatham LN, Goldstein JM, Vieta E, Bowden CL, Grunze H, Post RM, Suppes T, Calabrese JR: Atypical antipsychotics in bipolar depression: potential mechanisms of action. J Clin Psychiatry. 2005;66 Suppl 5:40-8. [Article]
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Quetiapine FDA label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase (PubMed:21645528). Positively regulates postnatal regression of retinal hyaloid vessels via suppression of VEGFR2/KDR activity, downstream of OPN5 (By similarity)
- Specific Function
- dopamine binding
- Gene Name
- DRD2
- Uniprot ID
- P14416
- Uniprot Name
- D(2) dopamine receptor
- Molecular Weight
- 50618.91 Da
References
- Kapur S, Zipursky R, Jones C, Shammi CS, Remington G, Seeman P: A positron emission tomography study of quetiapine in schizophrenia: a preliminary finding of an antipsychotic effect with only transiently high dopamine D2 receptor occupancy. Arch Gen Psychiatry. 2000 Jun;57(6):553-9. [Article]
- Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
- Seeman P: Atypical antipsychotics: mechanism of action. Can J Psychiatry. 2002 Feb;47(1):27-38. [Article]
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Quetiapine FDA label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- AntagonistPartial agonist
- General Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling inhibits adenylate cyclase activity and activates a phosphatidylinositol-calcium second messenger system that regulates the release of Ca(2+) ions from intracellular stores. Plays a role in the regulation of 5-hydroxytryptamine release and in the regulation of dopamine and 5-hydroxytryptamine metabolism. Plays a role in the regulation of dopamine and 5-hydroxytryptamine levels in the brain, and thereby affects neural activity, mood and behavior. Plays a role in the response to anxiogenic stimuli
- Specific Function
- G protein-coupled serotonin receptor activity
- Gene Name
- HTR1A
- Uniprot ID
- P08908
- Uniprot Name
- 5-hydroxytryptamine receptor 1A
- Molecular Weight
- 46106.335 Da
References
- Ichikawa J, Li Z, Dai J, Meltzer HY: Atypical antipsychotic drugs, quetiapine, iloperidone, and melperone, preferentially increase dopamine and acetylcholine release in rat medial prefrontal cortex: role of 5-HT1A receptor agonism. Brain Res. 2002 Nov 29;956(2):349-57. [Article]
- McIntyre RS, Soczynska JK, Woldeyohannes HO, Alsuwaidan M, Konarski JZ: A preclinical and clinical rationale for quetiapine in mood syndromes. Expert Opin Pharmacother. 2007 Jun;8(9):1211-9. [Article]
- Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
- Wood MD, Scott C, Clarke K, Cato KJ, Patel N, Heath J, Worby A, Gordon L, Campbell L, Riley G, Davies CH, Gribble A, Jones DN: Pharmacological profile of antipsychotics at monoamine receptors: atypicality beyond 5-HT2A receptor blockade. CNS Neurol Disord Drug Targets. 2006 Aug;5(4):445-52. [Article]
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances, such as lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. Arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Regulates the release of 5-hydroxytryptamine, dopamine and acetylcholine in the brain, and thereby affects neural activity, nociceptive processing, pain perception, mood and behavior. Besides, plays a role in vasoconstriction of cerebral arteries
- Specific Function
- G protein-coupled serotonin receptor activity
- Gene Name
- HTR1B
- Uniprot ID
- P28222
- Uniprot Name
- 5-hydroxytryptamine receptor 1B
- Molecular Weight
- 43567.535 Da
References
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. Regulates the release of 5-hydroxytryptamine in the brain, and thereby affects neural activity. May also play a role in regulating the release of other neurotransmitters. May play a role in vasoconstriction
- Specific Function
- G protein-coupled serotonin receptor activity
- Gene Name
- HTR1D
- Uniprot ID
- P28221
- Uniprot Name
- 5-hydroxytryptamine receptor 1D
- Molecular Weight
- 41906.38 Da
References
- Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various alkaloids and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity
- Specific Function
- G protein-coupled receptor activity
- Gene Name
- HTR1E
- Uniprot ID
- P28566
- Uniprot Name
- 5-hydroxytryptamine receptor 1E
- Molecular Weight
- 41681.57 Da
References
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-iodophenyl-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling activates a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and down-stream signaling cascades and promotes the release of Ca(2+) ions from intracellular stores. Regulates neuronal activity via the activation of short transient receptor potential calcium channels in the brain, and thereby modulates the activation of pro-opiomelacortin neurons and the release of CRH that then regulates the release of corticosterone. Plays a role in the regulation of appetite and eating behavior, responses to anxiogenic stimuli and stress. Plays a role in insulin sensitivity and glucose homeostasis
- Specific Function
- 1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding
- Gene Name
- HTR2C
- Uniprot ID
- P28335
- Uniprot Name
- 5-hydroxytryptamine receptor 2C
- Molecular Weight
- 51804.645 Da
References
- Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- Forms serotonin (5-hydroxytryptamine/5-HT3)-activated cation-selective channel complexes, which when activated cause fast, depolarizing responses in neurons
- Specific Function
- excitatory extracellular ligand-gated monoatomic ion channel activity
- Gene Name
- HTR3A
- Uniprot ID
- P46098
- Uniprot Name
- 5-hydroxytryptamine receptor 3A
- Molecular Weight
- 55279.835 Da
References
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase. It has a high affinity for tricyclic psychotropic drugs (By similarity). Controls pyramidal neurons migration during corticogenesis, through the regulation of CDK5 activity (By similarity). Is an activator of TOR signaling (PubMed:23027611)
- Specific Function
- G protein-coupled serotonin receptor activity
- Gene Name
- HTR6
- Uniprot ID
- P50406
- Uniprot Name
- 5-hydroxytryptamine receptor 6
- Molecular Weight
- 46953.625 Da
References
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Bymaster FP, Falcone JF, Bauzon D, Kennedy JS, Schenck K, DeLapp NW, Cohen ML: Potent antagonism of 5-HT(3) and 5-HT(6) receptors by olanzapine. Eur J Pharmacol. 2001 Nov 2;430(2-3):341-9. doi: 10.1016/s0014-2999(01)01399-1. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase
- Specific Function
- G protein-coupled serotonin receptor activity
- Gene Name
- HTR7
- Uniprot ID
- P34969
- Uniprot Name
- 5-hydroxytryptamine receptor 7
- Molecular Weight
- 53554.43 Da
References
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase
- Specific Function
- arrestin family protein binding
- Gene Name
- DRD1
- Uniprot ID
- P21728
- Uniprot Name
- D(1A) dopamine receptor
- Molecular Weight
- 49292.765 Da
References
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Tauscher J, Hussain T, Agid O, Verhoeff NP, Wilson AA, Houle S, Remington G, Zipursky RB, Kapur S: Equivalent occupancy of dopamine D1 and D2 receptors with clozapine: differentiation from other atypical antipsychotics. Am J Psychiatry. 2004 Sep;161(9):1620-5. doi: 10.1176/appi.ajp.161.9.1620. [Article]
- Moallem N, Ray LA: Quetiapine improves response inhibition in alcohol dependent patients: a placebo-controlled pilot study. Pharmacol Biochem Behav. 2012 Jan;100(3):490-3. doi: 10.1016/j.pbb.2011.10.012. Epub 2011 Oct 20. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase
- Specific Function
- dopamine binding
- Gene Name
- DRD5
- Uniprot ID
- P21918
- Uniprot Name
- D(1B) dopamine receptor
- Molecular Weight
- 52950.5 Da
References
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Jain M: Quetiapine associated Central Serous Chorioretinopathy: Implicit role of serotonin and dopamine pathways. Indian J Ophthalmol. 2019 Feb;67(2):292-294. doi: 10.4103/ijo.IJO_929_18. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation
- Specific Function
- dopamine neurotransmitter receptor activity, coupled via Gi/Go
- Gene Name
- DRD3
- Uniprot ID
- P35462
- Uniprot Name
- D(3) dopamine receptor
- Molecular Weight
- 44194.315 Da
References
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Vernaleken I, Janouschek H, Raptis M, Hellmann S, Veselinovic T, Brocheler A, Boy C, Cumming P, Hiemke C, Rosch F, Schafer WM, Grunder G: Dopamine D2/3 receptor occupancy by quetiapine in striatal and extrastriatal areas. Int J Neuropsychopharmacol. 2010 Aug;13(7):951-60. doi: 10.1017/S1461145710000374. Epub 2010 Apr 15. [Article]
- Bressan RA, Erlandsson K, Jones HM, Mulligan RS, Ell PJ, Pilowsky LS: Optimizing limbic selective D2/D3 receptor occupancy by risperidone: a [123I]-epidepride SPET study. J Clin Psychopharmacol. 2003 Feb;23(1):5-14. doi: 10.1097/00004714-200302000-00002. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Activated by dopamine, but also by epinephrine and norepinephrine, and by numerous synthetic agonists and drugs (PubMed:16423344, PubMed:27659709, PubMed:29051383, PubMed:9003072). Agonist binding triggers signaling via G proteins that inhibit adenylyl cyclase (PubMed:16423344, PubMed:27659709, PubMed:29051383, PubMed:7512953, PubMed:7643093). Modulates the circadian rhythm of contrast sensitivity by regulating the rhythmic expression of NPAS2 in the retinal ganglion cells (By similarity)
- Specific Function
- dopamine binding
- Gene Name
- DRD4
- Uniprot ID
- P21917
- Uniprot Name
- D(4) dopamine receptor
- Molecular Weight
- 43900.84 Da
References
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Li P, Snyder GL, Vanover KE: Dopamine Targeting Drugs for the Treatment of Schizophrenia: Past, Present and Future. Curr Top Med Chem. 2016;16(29):3385-3403. doi: 10.2174/1568026616666160608084834. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system
- Specific Function
- G protein-coupled serotonin receptor activity
- Gene Name
- HRH1
- Uniprot ID
- P35367
- Uniprot Name
- Histamine H1 receptor
- Molecular Weight
- 55783.61 Da
References
- Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Quetiapine FDA label [Link]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes
- Specific Function
- alpha1-adrenergic receptor activity
Components:
Name | UniProt ID |
---|---|
Alpha-1A adrenergic receptor | P35348 |
Alpha-1B adrenergic receptor | P35368 |
Alpha-1D adrenergic receptor | P25100 |
References
- Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Shayegan DK, Stahl SM: Atypical antipsychotics: matching receptor profile to individual patient's clinical profile. CNS Spectr. 2004 Oct;9(10 Suppl 11):6-14. [Article]
- Quetiapine FDA label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianserine > chlorpromazine = spiperone = prazosin > propanolol > alprenolol = pindolol
- Specific Function
- alpha-1B adrenergic receptor binding
- Gene Name
- ADRA2A
- Uniprot ID
- P08913
- Uniprot Name
- Alpha-2A adrenergic receptor
- Molecular Weight
- 50646.17 Da
References
- Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Jensen NH, Rodriguiz RM, Caron MG, Wetsel WC, Rothman RB, Roth BL: N-desalkylquetiapine, a potent norepinephrine reuptake inhibitor and partial 5-HT1A agonist, as a putative mediator of quetiapine's antidepressant activity. Neuropsychopharmacology. 2008 Sep;33(10):2303-12. doi: 10.1038/sj.npp.1301646. Epub 2007 Dec 5. [Article]
- Riedel M, Muller N, Strassnig M, Spellmann I, Severus E, Moller HJ: Quetiapine in the treatment of schizophrenia and related disorders. Neuropsychiatr Dis Treat. 2007 Apr;3(2):219-35. doi: 10.2147/nedt.2007.3.2.219. [Article]
- Jasdave S. Maan; Abdolreza Saadabadi (2019). Quetiapine. Stat Pearls Publishing.
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phentolamine > mianserine > spiperone > prazosin > alprenolol > propanolol > pindolol
- Specific Function
- alpha2-adrenergic receptor activity
- Gene Name
- ADRA2B
- Uniprot ID
- P18089
- Uniprot Name
- Alpha-2B adrenergic receptor
- Molecular Weight
- 49953.145 Da
References
- Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Suttajit S, Srisurapanont M, Maneeton N, Maneeton B: Quetiapine for acute bipolar depression: a systematic review and meta-analysis. Drug Des Devel Ther. 2014 Jun 25;8:827-38. doi: 10.2147/DDDT.S63779. eCollection 2014. [Article]
- Jensen NH, Rodriguiz RM, Caron MG, Wetsel WC, Rothman RB, Roth BL: N-desalkylquetiapine, a potent norepinephrine reuptake inhibitor and partial 5-HT1A agonist, as a putative mediator of quetiapine's antidepressant activity. Neuropsychopharmacology. 2008 Sep;33(10):2303-12. doi: 10.1038/sj.npp.1301646. Epub 2007 Dec 5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins
- Specific Function
- alpha-2A adrenergic receptor binding
- Gene Name
- ADRA2C
- Uniprot ID
- P18825
- Uniprot Name
- Alpha-2C adrenergic receptor
- Molecular Weight
- 49521.585 Da
References
- Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Uys MM, Shahid M, Harvey BH: Therapeutic Potential of Selectively Targeting the alpha2C-Adrenoceptor in Cognition, Depression, and Schizophrenia-New Developments and Future Perspective. Front Psychiatry. 2017 Aug 14;8:144. doi: 10.3389/fpsyt.2017.00144. eCollection 2017. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover
- Specific Function
- G protein-coupled acetylcholine receptor activity
- Gene Name
- CHRM1
- Uniprot ID
- P11229
- Uniprot Name
- Muscarinic acetylcholine receptor M1
- Molecular Weight
- 51420.375 Da
References
- Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Quetiapine FDA label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is adenylate cyclase inhibition. Signaling promotes phospholipase C activity, leading to the release of inositol trisphosphate (IP3); this then triggers calcium ion release into the cytosol
- Specific Function
- arrestin family protein binding
- Gene Name
- CHRM2
- Uniprot ID
- P08172
- Uniprot Name
- Muscarinic acetylcholine receptor M2
- Molecular Weight
- 51714.605 Da
References
- Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover
- Specific Function
- acetylcholine binding
- Gene Name
- CHRM3
- Uniprot ID
- P20309
- Uniprot Name
- Muscarinic acetylcholine receptor M3
- Molecular Weight
- 66127.445 Da
References
- Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Vehof J, Risselada AJ, Al Hadithy AF, Burger H, Snieder H, Wilffert B, Arends J, Wunderink L, Knegtering H, Wiersma D, Cohen D, Mulder H, Bruggeman R: Association of genetic variants of the histamine H1 and muscarinic M3 receptors with BMI and HbA1c values in patients on antipsychotic medication. Psychopharmacology (Berl). 2011 Jul;216(2):257-65. doi: 10.1007/s00213-011-2211-x. Epub 2011 Feb 19. [Article]
- Muller C, Reuter H, Dohmen C: Intoxication after extreme oral overdose of quetiapine to attempt suicide: pharmacological concerns of side effects. Case Rep Med. 2009;2009:371698. doi: 10.1155/2009/371698. Epub 2010 Jan 3. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is inhibition of adenylate cyclase
- Specific Function
- G protein-coupled acetylcholine receptor activity
- Gene Name
- CHRM4
- Uniprot ID
- P08173
- Uniprot Name
- Muscarinic acetylcholine receptor M4
- Molecular Weight
- 53048.65 Da
References
- Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover
- Specific Function
- G protein-coupled acetylcholine receptor activity
- Gene Name
- CHRM5
- Uniprot ID
- P08912
- Uniprot Name
- Muscarinic acetylcholine receptor M5
- Molecular Weight
- 60073.205 Da
References
- Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Article]
- Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of polyunsaturated fatty acids (PUFA) (PubMed:18577768, PubMed:19965576, PubMed:20972997). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:18577768, PubMed:19965576, PubMed:20972997). Catalyzes the hydroxylation of carbon-hydrogen bonds. Hydroxylates PUFA specifically at the omega-1 position (PubMed:18577768). Catalyzes the epoxidation of double bonds of PUFA (PubMed:19965576, PubMed:20972997). Also metabolizes plant monoterpenes such as limonene. Oxygenates (R)- and (S)-limonene to produce carveol and perillyl alcohol (PubMed:11950794). Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine. Hydroxylates fenbendazole at the 4' position (PubMed:23959307)
- Specific Function
- (R)-limonene 6-monooxygenase activity
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55944.565 Da
References
- Lin SN, Chang Y, Moody DE, Foltz RL: A liquid chromatographic-electrospray-tandem mass spectrometric method for quantitation of quetiapine in human plasma and liver microsomes: application to study in vitro metabolism. J Anal Toxicol. 2004 Sep;28(6):443-8. doi: 10.1093/jat/28.6.443. [Article]
- Bavle AD, Vishwaraj S: Warfarin-quetiapine interaction causing hemorrhage. Indian J Psychiatry. 2016 Jan-Mar;58(1):102-3. doi: 10.4103/0019-5545.174401. [Article]
- Cabaleiro T, Lopez-Rodriguez R, Roman M, Ochoa D, Novalbos J, Borobia A, Carcas A, Abad-Santos F: Pharmacogenetics of quetiapine in healthy volunteers: association with pharmacokinetics, pharmacodynamics, and adverse effects. Int Clin Psychopharmacol. 2015 Mar;30(2):82-8. doi: 10.1097/YIC.0000000000000047. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of fatty acids, steroids and retinoids (PubMed:18698000, PubMed:19965576, PubMed:20972997, PubMed:21289075, PubMed:21576599). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:18698000, PubMed:19965576, PubMed:20972997, PubMed:21289075, PubMed:21576599). Catalyzes the epoxidation of double bonds of polyunsaturated fatty acids (PUFA) (PubMed:19965576, PubMed:20972997). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 20-hydroxyeicosatetraenoic acid ethanolamide (20-HETE-EA) and 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:18698000, PubMed:21289075). Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes cholesterol toward 25-hydroxycholesterol, a physiological regulator of cellular cholesterol homeostasis (PubMed:21576599). Catalyzes the oxidative transformations of all-trans retinol to all-trans retinal, a precursor for the active form all-trans-retinoic acid (PubMed:10681376). Also involved in the oxidative metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants
- Specific Function
- anandamide 11,12 epoxidase activity
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- Lin SN, Chang Y, Moody DE, Foltz RL: A liquid chromatographic-electrospray-tandem mass spectrometric method for quantitation of quetiapine in human plasma and liver microsomes: application to study in vitro metabolism. J Anal Toxicol. 2004 Sep;28(6):443-8. doi: 10.1093/jat/28.6.443. [Article]
- Hasselstrom J, Linnet K: In vitro studies on quetiapine metabolism using the substrate depletion approach with focus on drug-drug interactions. Drug Metabol Drug Interact. 2006;21(3-4):187-211. [Article]
- Bakken GV, Molden E, Knutsen K, Lunder N, Hermann M: Metabolism of the active metabolite of quetiapine, N-desalkylquetiapine in vitro. Drug Metab Dispos. 2012 Sep;40(9):1778-84. doi: 10.1124/dmd.112.045237. Epub 2012 Jun 11. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of steroid hormones and vitamins during embryogenesis (PubMed:11093772, PubMed:12865317, PubMed:14559847, PubMed:17178770, PubMed:9555064). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:11093772, PubMed:12865317, PubMed:14559847, PubMed:17178770, PubMed:9555064). Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes 3beta-hydroxyandrost-5-en-17-one (dehydroepiandrosterone, DHEA), a precursor in the biosynthesis of androgen and estrogen steroid hormones (PubMed:17178770, PubMed:9555064). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1), particularly D-ring hydroxylated estrone at the C16-alpha position (PubMed:12865317, PubMed:14559847). Mainly hydroxylates all trans-retinoic acid (atRA) to 4-hydroxyretinoate and may play a role in atRA clearance during fetal development (PubMed:11093772). Also involved in the oxidative metabolism of xenobiotics including anticonvulsants (PubMed:9555064)
- Specific Function
- all-trans retinoic acid 18-hydroxylase activity
- Gene Name
- CYP3A7
- Uniprot ID
- P24462
- Uniprot Name
- Cytochrome P450 3A7
- Molecular Weight
- 57469.95 Da
References
- Lin SN, Chang Y, Moody DE, Foltz RL: A liquid chromatographic-electrospray-tandem mass spectrometric method for quantitation of quetiapine in human plasma and liver microsomes: application to study in vitro metabolism. J Anal Toxicol. 2004 Sep;28(6):443-8. doi: 10.1093/jat/28.6.443. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of sterols, steroid hormones, retinoids and fatty acids (PubMed:10681376, PubMed:11093772, PubMed:11555828, PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:19965576, PubMed:20702771, PubMed:21490593, PubMed:21576599). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:21490593, PubMed:21576599, PubMed:2732228). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2, as well as D-ring hydroxylated E1 and E2 at the C-16 position (PubMed:11555828, PubMed:12865317, PubMed:14559847). Plays a role in the metabolism of androgens, particularly in oxidative deactivation of testosterone (PubMed:15373842, PubMed:15764715, PubMed:22773874, PubMed:2732228). Metabolizes testosterone to less biologically active 2beta- and 6beta-hydroxytestosterones (PubMed:15373842, PubMed:15764715, PubMed:2732228). Contributes to the formation of hydroxycholesterols (oxysterols), particularly A-ring hydroxylated cholesterol at the C-4beta position, and side chain hydroxylated cholesterol at the C-25 position, likely contributing to cholesterol degradation and bile acid biosynthesis (PubMed:21576599). Catalyzes bisallylic hydroxylation of polyunsaturated fatty acids (PUFA) (PubMed:9435160). Catalyzes the epoxidation of double bonds of PUFA with a preference for the last double bond (PubMed:19965576). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:20702771). Plays a role in the metabolism of retinoids. Displays high catalytic activity for oxidation of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes atRA toward 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Responsible for oxidative metabolism of xenobiotics. Acts as a 2-exo-monooxygenase for plant lipid 1,8-cineole (eucalyptol) (PubMed:11159812). Metabolizes the majority of the administered drugs. Catalyzes sulfoxidation of the anthelmintics albendazole and fenbendazole (PubMed:10759686). Hydroxylates antimalarial drug quinine (PubMed:8968357). Acts as a 1,4-cineole 2-exo-monooxygenase (PubMed:11695850). Also involved in vitamin D catabolism and calcium homeostasis. Catalyzes the inactivation of the active hormone calcitriol (1-alpha,25-dihydroxyvitamin D(3)) (PubMed:29461981)
- Specific Function
- 1,8-cineole 2-exo-monooxygenase activity
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Urichuk L, Prior TI, Dursun S, Baker G: Metabolism of atypical antipsychotics: involvement of cytochrome p450 enzymes and relevance for drug-drug interactions. Curr Drug Metab. 2008 Jun;9(5):410-8. [Article]
- DeVane CL, Nemeroff CB: Clinical pharmacokinetics of quetiapine: an atypical antipsychotic. Clin Pharmacokinet. 2001;40(7):509-22. doi: 10.2165/00003088-200140070-00003. [Article]
- Bakken GV, Rudberg I, Christensen H, Molden E, Refsum H, Hermann M: Metabolism of quetiapine by CYP3A4 and CYP3A5 in presence or absence of cytochrome B5. Drug Metab Dispos. 2009 Feb;37(2):254-8. doi: 10.1124/dmd.108.023291. Epub 2008 Nov 20. [Article]
- Bakken GV, Molden E, Knutsen K, Lunder N, Hermann M: Metabolism of the active metabolite of quetiapine, N-desalkylquetiapine in vitro. Drug Metab Dispos. 2012 Sep;40(9):1778-84. doi: 10.1124/dmd.112.045237. Epub 2012 Jun 11. [Article]
- Dev V, Raniwalla J: Quetiapine: a review of its safety in the management of schizophrenia. Drug Saf. 2000 Oct;23(4):295-307. [Article]
- Flockhart Table of Drug Interactions [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of steroid hormones and vitamins (PubMed:10681376, PubMed:11093772, PubMed:12865317, PubMed:2732228). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:10681376, PubMed:11093772, PubMed:12865317, PubMed:2732228). Exhibits high catalytic activity for the formation of catechol estrogens from 17beta-estradiol (E2) and estrone (E1), namely 2-hydroxy E1 and E2 (PubMed:12865317). Catalyzes 6beta-hydroxylation of the steroid hormones testosterone, progesterone, and androstenedione (PubMed:2732228). Catalyzes the oxidative conversion of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes all trans-retinoic acid (atRA) to 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Also involved in the oxidative metabolism of xenobiotics, including calcium channel blocking drug nifedipine and immunosuppressive drug cyclosporine (PubMed:2732228)
- Specific Function
- aromatase activity
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- Kim KA, Joo HJ, Lee HM, Park JY: Influence of ABCB1 and CYP3A5 genetic polymorphisms on the pharmacokinetics of quetiapine in healthy volunteers. Pharmacogenet Genomics. 2014 Jan;24(1):35-42. doi: 10.1097/FPC.0000000000000020. [Article]
- Bakken GV, Rudberg I, Christensen H, Molden E, Refsum H, Hermann M: Metabolism of quetiapine by CYP3A4 and CYP3A5 in presence or absence of cytochrome B5. Drug Metab Dispos. 2009 Feb;37(2):254-8. doi: 10.1124/dmd.108.023291. Epub 2008 Nov 20. [Article]
- Flockhart Table of Drug Interactions [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Translocates drugs and phospholipids across the membrane (PubMed:2897240, PubMed:35970996, PubMed:8898203, PubMed:9038218). Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins (PubMed:8898203). Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells (PubMed:2897240, PubMed:35970996, PubMed:9038218)
- Specific Function
- ABC-type xenobiotic transporter activity
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- ATP-dependent translocase ABCB1
- Molecular Weight
- 141477.255 Da
References
- Boulton DW, DeVane CL, Liston HL, Markowitz JS: In vitro P-glycoprotein affinity for atypical and conventional antipsychotics. Life Sci. 2002 May 31;71(2):163-9. [Article]
- Kim KA, Joo HJ, Lee HM, Park JY: Influence of ABCB1 and CYP3A5 genetic polymorphisms on the pharmacokinetics of quetiapine in healthy volunteers. Pharmacogenet Genomics. 2014 Jan;24(1):35-42. doi: 10.1097/FPC.0000000000000020. [Article]
Drug created at June 13, 2005 13:24 / Updated at October 06, 2024 08:03