Cisatracurium
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Identification
- Summary
Cisatracurium is a skeletal muscle relaxant used to facilitate tracheal intubation, muscle relaxation in surgery, or mechanical ventilation.
- Brand Names
- Nimbex
- Generic Name
- Cisatracurium
- DrugBank Accession Number
- DB00565
- Background
Cisatracurium is a non-depolarising neuromuscular blocking agent of the benzylisoquinolinium class, available in its salt form, cisatracurium besylate.1,2 Cisatracurium has an intermediate duration of action and is one of the most commonly used neuromuscular blocking agents in intensive care.2,3. Cisatracurium acts on cholinergic receptors, blocking neuromuscular transmission. This action is antagonized by acetylcholinesterase inhibitors such as neostigmine.1,2 Cisatracurium is an R-cis-R-cis isomer of atracurium and has approximately 3 times its neuromuscular blocking potency.1 Compared to atracurium, cisatracurium produces a lower degree of histamine release.3
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
- Weight
- Average: 929.16
Monoisotopic: 928.507428607 - Chemical Formula
- C53H72N2O12
- Synonyms
- (1r,2r,1'r,2'r)-2,2'-{pentane-1,5-diylbis[oxy(3-oxopropane-3,1-diyl)]}bis[1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydroisoquinolinium]
- Cisatracurium cation
- Cisatracurium ion
Pharmacology
- Indication
Cisatracurium is indicated as an adjunct to general anesthesia to facilitate tracheal intubation in adults and pediatric patients 1 month to 12 years of age. Cisatracurium is also indicated to provide skeletal muscle relaxation during surgery in adults and pediatric patients 2 to 12 years of age as a bolus or infusion maintenance and for mechanical ventilation in the ICU in adults.5
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- Contraindications & Blackbox Warnings
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- Pharmacodynamics
The dose required to produce 95% suppression of twitch response to nerve stimulation (ED95) of cisatracurium is 0.05 mg/kg in adults receiving opioid/nitrous oxide/oxygen anesthesia.3,5 The degree and duration of the neuromuscular block produced by cisatracurium increases in a dose-dependent manner, while the time to maximum neuromuscular block decreases.3 Compared to other neuromuscular blocking agents, it is intermediate in its onset and duration of action.2 Cisatracurium acts on cholinergic receptors, blocking neuromuscular transmission. This action is antagonized by acetylcholinesterase inhibitors such as neostigmine.1
The use of cisatracurium may lead to residual paralysis, as well as a higher risk of seizure. Medication errors increase the risk of death, and the use of certain drugs may potentiate the neuromuscular blocking action of cisatracurium.5
- Mechanism of action
Like other non-depolarising neuromuscular blocking agents, cisatracurium binds competitively to cholinergic receptors in motor end-plate neurons, blocking acetylcholine from accessing the receptors.5 Therefore, in the presence of cisatracurium, an end-plate potential cannot be developed. Ion channels remain closed, the cell does not depolarize, and an action potential is not transmitted.1
Target Actions Organism ANeuronal acetylcholine receptor subunit alpha-2 antagonistHumans ANeuronal Acetylcholine (nACh) Receptor Subunits antagonistHumans UAcetylcholine receptor subunit alpha antagonistHumans UMuscarinic acetylcholine receptor M2 antagonistHumans - Absorption
The pharmacokinetics of cisatracurium follow a two-compartment open model.4,5 Cisatracurium is metabolized into laudanosine and monoquaternary alcohol metabolite (MQA). Following the IV infusion of cisatracurium, the Cmax of laudanosine and MQA were 6% and 11% of the parent compound, respectively.5
Compared to young patients, the volume of distribution of cisatracurium is slightly larger in elderly patients, which also leads to longer half-life values. The plasma clearance of cisatracurium was not affected by age. Patients with hepatic impairment have a slightly higher volume of distribution and plasma clearance values; however, these minor pharmacokinetic differences are not considered clinically significant. Additionally, the pharmacokinetic parameters of cisatracurium in patients with end-stage renal disease were similar to those detected in healthy adult patients.5
- Volume of distribution
Cisatracurium has a volume of distribution at steady state of 145 mL/kg.5 The volume of distribution of cisatracurium besylate is small due to its relatively large molecular weight and high polarity.4
- Protein binding
The binding of cisatracurium to plasma proteins has not been successfully studied due to its rapid degradation at physiologic pH.5
- Metabolism
The degradation of cisatracurium is largely independent of liver metabolism. Cisatracurium undergoes Hofmann elimination (a pH and temperature-dependent chemical process) to form laudanosine and the monoquaternary acrylate metabolite. Non-specific plasma esterases hydrolyze the monoquaternary acrylate metabolite to form the monoquaternary alcohol metabolite (MQA). The MQA can also undergo Hofmann elimination, but the rate of this process is slower than the one detected for cisatracurium. Laudanosine is further metabolized to desmethyl metabolites that are conjugated with glucuronic acid and excreted in the urine. Laudanosine may cause transient hypotension and, in higher doses, cerebral excitatory effects when administered to several animal species; however, the effects of laudanosine in humans have not been established.5
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- Route of elimination
The predominant elimination mechanism of cisatracurium is Hofmann elimination, a chemical process dependent on pH and temperature (approximately 80% in healthy surgical patients). The liver and kidney play a minor role in the elimination of cisatracurium (about 20%); however, they have a significant role in the metabolism of cisatracurium metabolites.5
In healthy male patients (n=6) given 14C-cisatracurium, 4% of the recovered dose was found in feces, and 95% was found in urine, mostly as conjugated metabolites. Less than 10% of the cisatracurium dose was excreted as the unchanged patent drug. In another group of patients with Foley catheters for surgical management given non-radiolabeled cisatracurium (n=12), 15% of the cisatracurium dose was excreted unchanged in urine.5
- Half-life
Cisatracurium has an elimination half-life of 22 minutes.5
- Clearance
Cisatracurium has a plasma clearance of 4.57 mL/min/kg.5
- 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
Overdosage with neuromuscular blocking agents such as cisatracurium may result in neuromuscular block beyond the time needed for surgery and anesthesia. Maintenance of a patent airway and controlled ventilation until recovery of normal neuromuscular function is the primary treatment for overdose cases. To facilitate further recovery, a cholinesterase inhibitor in conjunction with an appropriate cholinergic inhibitor may be administered once recovery from the neuromuscular block begins. If complete neuromuscular blockade is evident or suspected, cholinesterase inhibitors should not be administered. The reversal of paralysis may not be sufficient to maintain a patent airway and an appropriate level of spontaneous ventilation.5
The long-term carcinogenicity of cisatracurium has not been evaluated. In an in vitro mouse lymphoma forward gene mutation assay, cisatracurium besylate led to mutations in the presence and absence of exogenous metabolic activation. Other assays did not show evidence of mutagenicity or clastogenicity.5
- Pathways
- Not Available
- 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 Cisatracurium is combined with 1,2-Benzodiazepine. Acetazolamide The risk or severity of CNS depression can be increased when Cisatracurium is combined with Acetazolamide. Acetic acid Acetic acid may increase the neuromuscular blocking activities of Cisatracurium. Acetophenazine The risk or severity of CNS depression can be increased when Cisatracurium is combined with Acetophenazine. Acetyl sulfisoxazole Acetyl sulfisoxazole may increase the neuromuscular blocking activities of Cisatracurium. - Food Interactions
- No interactions found.
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 Cisatracurium besylate 80YS8O1MBS 96946-42-8 XXZSQOVSEBAPGS-DONVQRBFSA-L - International/Other Brands
- Nimbex (AbbVie) / Nimbex Preservative Free (AbbVie) / Nimbium (GlaxoSmithKline)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Cisatracurium Besylate Injection Solution 2 mg / mL Intravenous Mylan Pharmaceuticals Not applicable Not applicable Canada Cisatracurium Besylate Injection Solution 2 mg / mL Intravenous Accord Healthcare Inc Not applicable Not applicable Canada Cisatracurium Besylate Injection Solution 2 mg / mL Intravenous Pfizer Canada Ulc 2015-06-01 2019-03-28 Canada Cisatracurium Besylate Injection (preservative-free) Solution 2 mg / mL Intravenous Mylan Pharmaceuticals Not applicable Not applicable Canada Cisatracurium Besylate Injection Multi-dose Solution 2 mg / mL Intravenous Fresenius Kabi Not applicable Not applicable Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Aj-cisatracurium Solution 2 mg / mL Intravenous Agila Jamp Canada Inc Not applicable Not applicable Canada Aj-cisatracurium Solution 2 mg / mL Intravenous Agila Jamp Canada Inc Not applicable Not applicable Canada Cisatracurium Injection, solution 2 mg/1mL Intravenous Fresenius Kabi USA, LLC 2015-02-26 Not applicable US Cisatracurium Injection, solution 2 mg/1mL Intravenous Fresenius Kabi USA, LLC 2015-02-26 Not applicable US Cisatracurium Injection, solution 10 mg/1mL Intravenous Fresenius Kabi USA, LLC 2015-02-26 Not applicable US
Categories
- ATC Codes
- M03AC11 — Cisatracurium
- Drug Categories
- Anticholinergic Agents
- Benzylisoquinolines
- Central Nervous System Depressants
- Heterocyclic Compounds, Fused-Ring
- Isoquinolines
- Muscle Relaxants
- Muscle Relaxants, Peripherally Acting Agents
- Musculo-Skeletal System
- Neuromuscular Agents
- Neuromuscular Blocking Agents
- Neuromuscular Nondepolarizing Blockade
- Neuromuscular-Blocking Agents (Nondepolarizing)
- Nicotinic Antagonists
- Peripheral Nervous System Agents
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as benzylisoquinolines. These are organic compounds containing an isoquinoline to which a benzyl group is attached.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Isoquinolines and derivatives
- Sub Class
- Benzylisoquinolines
- Direct Parent
- Benzylisoquinolines
- Alternative Parents
- Tetrahydroisoquinolines / Dimethoxybenzenes / Phenoxy compounds / Anisoles / Alkyl aryl ethers / Aralkylamines / Dicarboxylic acids and derivatives / Tetraalkylammonium salts / Carboxylic acid esters / Azacyclic compounds show 6 more
- Substituents
- Alkyl aryl ether / Amine / Anisole / Aralkylamine / Aromatic heteropolycyclic compound / Azacycle / Benzenoid / Benzylisoquinoline / Carbonyl group / Carboxylic acid derivative show 21 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- QX62KLI41N
- CAS number
- 96946-41-7
- InChI Key
- YXSLJKQTIDHPOT-LJCJQEJUSA-N
- InChI
- InChI=1S/C53H72N2O12/c1-54(22-18-38-32-48(62-7)50(64-9)34-40(38)42(54)28-36-14-16-44(58-3)46(30-36)60-5)24-20-52(56)66-26-12-11-13-27-67-53(57)21-25-55(2)23-19-39-33-49(63-8)51(65-10)35-41(39)43(55)29-37-15-17-45(59-4)47(31-37)61-6/h14-17,30-35,42-43H,11-13,18-29H2,1-10H3/q+2/t42-,43-,54-,55-/m1/s1
- IUPAC Name
- (1R,2R)-1-[(3,4-dimethoxyphenyl)methyl]-2-(3-{[5-({3-[(1R,2R)-1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydroisoquinolin-2-ium-2-yl]propanoyl}oxy)pentyl]oxy}-3-oxopropyl)-6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydroisoquinolin-2-ium
- SMILES
- COC1=CC2=C(C=C1OC)[C@@H](CC1=CC(OC)=C(OC)C=C1)[N@@+](C)(CCC(=O)OCCCCCOC(=O)CC[N@@+]1(C)CCC3=C(C=C(OC)C(OC)=C3)[C@H]1CC1=CC(OC)=C(OC)C=C1)CC2
References
- Synthesis Reference
Arad O., et al. (2013). Process for producing cisatracurium and associated intermediates (U.S. Patent No. 2013/0041154 A1). U.S. Patent and Trademark Office. https://patentimages.storage.googleapis.com/c3/a4/c7/67ee80a0faa6dc/US20130041154A1.pdf
- General References
- Strawbridge AD, Khanna NR, Hauser JM: Cisatracurium . [Article]
- Szakmany T, Woodhouse T: Use of cisatracurium in critical care: a review of the literature. Minerva Anestesiol. 2015 Apr;81(4):450-60. Epub 2014 Apr 10. [Article]
- Bryson HM, Faulds D: Cisatracurium besilate. A review of its pharmacology and clinical potential in anaesthetic practice. Drugs. 1997 May;53(5):848-66. doi: 10.2165/00003495-199753050-00012. [Article]
- Kisor DF, Schmith VD: Clinical pharmacokinetics of cisatracurium besilate. Clin Pharmacokinet. 1999 Jan;36(1):27-40. doi: 10.2165/00003088-199936010-00003. [Article]
- FDA Approved Drug Products: Nimbex (cisatracurium besylate) injection for intravenous use [Link]
- External Links
- Human Metabolome Database
- HMDB0240286
- PubChem Compound
- 62886
- PubChem Substance
- 46506666
- ChemSpider
- 56615
- 319864
- ChEBI
- 140621
- ChEMBL
- CHEMBL1201248
- ZINC
- ZINC000238809664
- Therapeutic Targets Database
- DAP000196
- PharmGKB
- PA164744925
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Cisatracurium_besilate
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 Recruiting Treatment Acute Respiratory Distress Syndrome (ARDS) / Lung Protective Ventilation 1 somestatus stop reason just information to hide 4 Completed Not Available Neuromuscular Blockade 1 somestatus stop reason just information to hide 4 Completed Basic Science Acute Respiratory Distress Syndrome (ARDS) / ARDS, Human / Critically Ill Patients / Neuromuscular Blockade / Paralysis / Respiratory Failure 1 somestatus stop reason just information to hide 4 Completed Prevention C.Delivery; Surgery (Previous), Gynecological 1 somestatus stop reason just information to hide 4 Completed Prevention Curarization, Postoperative Residual / Residual Neuromuscular Block 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Baxter healthcare corp anesthesia and critical care
- Baxter healthcare corp anesthesia critical care
- Bedford laboratories div ben venue laboratories inc
- Hospira inc
- Marsam pharmaceuticals llc
- Teva parenteral medicines inc
- Abbott laboratories
- Packagers
- Abbott Laboratories Ltd.
- Baxter International Inc.
- Bedford Labs
- Ben Venue Laboratories Inc.
- GlaxoSmithKline Inc.
- Hospira Inc.
- Patheon Inc.
- Teva Pharmaceutical Industries Ltd.
- Dosage Forms
Form Route Strength Solution Parenteral 2.00 mg Solution Intravenous 10 mg Injection, solution 2 mg/1ml Injection, solution Intravenous bolus 5 MG/ML Injection, solution 2 MG/ML Injection, solution 5 MG/ML Injection, solution Intravenous bolus 2 MG/ML Injection, solution Injection, solution Intravenous 10 mg/1mL Injection, solution Intravenous 2 mg/1mL Injection, solution Parenteral 2 mg/ml Injection, solution Parenteral Injection, solution Parenteral 5 mg/ml Injection Intravenous 10 mg/5mL Injection Intravenous 10 mg/1mL Injection Intravenous 2 mg/1mL Injection Intravenous 20 mg/10mL Injection Intravenous 200 mg/20mL Injection, solution Intravenous 10 mg/5mL Injection, solution Intravenous 20 mg/10mL Injection, solution Intravenous 200 mg/20mL Solution Parenteral 2 mg/ml Solution 2 mg/1ml Solution 2 mg/ml Solution Intravenous 2 mg / mL Solution Parenteral 13.38 mg Injection Intravenous 10 mg Solution Intravenous 6.690 mg Injection, solution Intravenous 10 mg Injection, solution Intravenous 150 mg Injection, solution Intravenous 20 mg Injection, solution Intravenous 5 mg Injection, solution Intravenous 50 mg Liquid Intravenous 2 mg / mL Liquid Intravenous 10 mg / mL Injection, solution Intravenous 5 mg/2.5ml Injection Intravenous 50 mg/25ml Injection, solution Intravenous 150 mg/30ml Injection, solution Intravenous 2 mg/ml Injection Parenteral 2 MG/ML Solution Intravenous 5 mg Injection, solution 5 mg/1ml - Prices
Unit description Cost Unit Nimbex 10 mg/ml vial 13.8USD ml Nimbex 2 mg/ml vial 2.91USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5453510 No 1995-09-26 2012-09-26 US CA2087104 No 1998-08-18 2011-07-12 Canada
Properties
- State
- Solid
- Experimental Properties
Property Value Source logP -2.12 Nimbex (cisatracurium besylate) FDA label - Predicted Properties
Property Value Source Water Solubility 2.32e-05 mg/mL ALOGPS logP 3.41 ALOGPS logP -0.96 Chemaxon logS -7.6 ALOGPS pKa (Strongest Acidic) 19.02 Chemaxon pKa (Strongest Basic) -4.1 Chemaxon Physiological Charge 2 Chemaxon Hydrogen Acceptor Count 10 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 126.44 Å2 Chemaxon Rotatable Bond Count 26 Chemaxon Refractivity 280.68 m3·mol-1 Chemaxon Polarizability 104.19 Å3 Chemaxon Number of Rings 6 Chemaxon Bioavailability 0 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption - 0.9847 Blood Brain Barrier + 0.9291 Caco-2 permeable - 0.5966 P-glycoprotein substrate Substrate 0.6828 P-glycoprotein inhibitor I Inhibitor 0.7177 P-glycoprotein inhibitor II Inhibitor 0.5808 Renal organic cation transporter Non-inhibitor 0.5871 CYP450 2C9 substrate Non-substrate 0.7994 CYP450 2D6 substrate Non-substrate 0.7779 CYP450 3A4 substrate Substrate 0.6527 CYP450 1A2 substrate Non-inhibitor 0.8244 CYP450 2C9 inhibitor Non-inhibitor 0.7179 CYP450 2D6 inhibitor Non-inhibitor 0.791 CYP450 2C19 inhibitor Non-inhibitor 0.7048 CYP450 3A4 inhibitor Non-inhibitor 0.7338 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8547 Ames test Non AMES toxic 0.544 Carcinogenicity Non-carcinogens 0.5302 Biodegradation Ready biodegradable 0.8169 Rat acute toxicity 2.6124 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.6043 hERG inhibition (predictor II) Inhibitor 0.6507
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 340.5874517 predictedDarkChem Lite v0.1.0 [M-H]- 332.8833517 predictedDarkChem Lite v0.1.0 [M-H]- 293.16223 predictedDeepCCS 1.0 (2019) [M+H]+ 342.1155517 predictedDarkChem Lite v0.1.0 [M+H]+ 333.8848517 predictedDarkChem Lite v0.1.0 [M+H]+ 295.05765 predictedDeepCCS 1.0 (2019) [M+Na]+ 339.9729517 predictedDarkChem Lite v0.1.0 [M+Na]+ 332.8057517 predictedDarkChem Lite v0.1.0 [M+Na]+ 301.13345 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane
- Specific Function
- Acetylcholine receptor activity
- Gene Name
- CHRNA2
- Uniprot ID
- Q15822
- Uniprot Name
- Neuronal acetylcholine receptor subunit alpha-2
- Molecular Weight
- 59764.82 Da
References
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Ionotropic receptor with a probable role in the modulation of auditory stimuli. Agonist binding may induce an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane. The channel is permeable to a range of divalent cations including calcium, the influx of which may activate a potassium current which hyperpolarizes the cell membrane. In the ear, this may lead to a reduction in basilar membrane motion, altering the activity of auditory nerve fibers and reducing the range of dynamic hearing. This may protect against acoustic trauma
- Specific Function
- Acetylcholine-gated monoatomic cation-selective channel activity
Components:
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Upon acetylcholine binding, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane
- Specific Function
- Acetylcholine binding
- Gene Name
- CHRNA1
- Uniprot ID
- P02708
- Uniprot Name
- Acetylcholine receptor subunit alpha
- Molecular Weight
- 51838.14 Da
References
- Fanelli V, Morita Y, Cappello P, Ghazarian M, Sugumar B, Delsedime L, Batt J, Ranieri VM, Zhang H, Slutsky AS: Neuromuscular Blocking Agent Cisatracurium Attenuates Lung Injury by Inhibition of Nicotinic Acetylcholine Receptor-alpha1. Anesthesiology. 2016 Jan;124(1):132-40. doi: 10.1097/ALN.0000000000000907. [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 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
- Patterson E, Scherlag BJ, Zhou J, Jackman WM, Lazzara R, Coscia D, Po S: Antifibrillatory actions of cisatracurium: an atrial specific M2 receptor antagonist. J Cardiovasc Electrophysiol. 2008 Aug;19(8):861-8. doi: 10.1111/j.1540-8167.2008.01123.x. Epub 2008 Mar 21. [Article]
Drug created at June 13, 2005 13:24 / Updated at September 08, 2024 21:55