Sulpiride

Identification

Summary

Sulpiride is a selective D2 dopamine receptor antagonist indicated to treat chronic and acute schizophrenia.

Generic Name
Sulpiride
DrugBank Accession Number
DB00391
Background

Sulpiride first appeared in published literature in 1967.1 Clinical studies show a greater effect on treating the negative symptoms of schizophrenia rather than positive symptoms at low doses, though the effects are more equal at higher doses.7

Sulpiride is not approved by the FDA, Health Canada, or the EMA; though it is approved in individual European countries.11

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 341.426
Monoisotopic: 341.140926929
Chemical Formula
C15H23N3O4S
Synonyms
  • (±)-sulpiride
  • 5-(Aminosulfonyl)-N-((1-ethyl-2-pyrrolidinyl)methyl)-2-methoxybenzamide
  • N-((1-Ethyl-2-pyrrolidinyl)methyl)-2-methoxy-5-sulfamoylbenzamide
  • N-((1-Ethyl-2-pyrrolidinyl)methyl)-5-sulfamoyl-o-anisamide
  • Sulpirid
  • Sulpirida
  • Sulpiride
  • Sulpiridum
  • Sulpyrid

Pharmacology

Indication

Sulpiride is indicated for the treatment of acute and chronic schizophrenia.10

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Sulpiride is a substituted benzamide derivative and a selective dopamine D2 antagonist indicated to treat acute and chronic schizophrenia.6,7,8,10 It has a short duration of action as it is given twice daily, and a wide therapeutic window as patients have survived single doses as high as 16g.10 Patients should be counselled regarding increased motor agitation, extrapyramidal reactions, and neuroleptic malignant syndrome.10

Mechanism of action

Sulpiride is a selective dopamine D2 and D3 receptor antagonist.6,7,8 In silico studies show that sulpiride may interact with the Asp-119 and Phe-417 amino acid residues of these receptors.8 It is estimated that D2 receptors should be 65-80% occupied for optimal treatment and minimal adverse effects.9

TargetActionsOrganism
ADopamine D2 receptor
antagonist
Humans
UDopamine D3 receptor
antagonist
Humans
UCarbonic anhydrase 2
inhibitor
Humans
UCarbonic anhydrase 3
inhibitor
Humans
UDopamine D4 receptor
antagonist
Humans
Absorption

Sulpiride has an oral bioavailability of 27 ± 9%.4 A 100-108 mg dose of sulpiride reaches a Cmax of 232-403 ng/mL, with a Tmax of 8.3 h.2 In another study, the AUC of a 100mg oral dose of sulpiride is 1156 ± 522 h*ng/mL and for an intravenous dose is 3981 ± 813 h*ng/mL.4

Volume of distribution

The average volume of distribution of sulpiride is 2.72 ± 0.66 L/kg.4

Protein binding

Sulpiride is approximately 40% protein bound in plasma, particularly to albumin.3

Metabolism

95% of a dose of sulpiride is not metabolized.2

Route of elimination

An intravenous dose of sulpiride is 70 ± 9% eliminated in the urine within 36 hours, while an oral dose is 27 ± 9% eliminated in urine.4 In both cases, the dose is recovered as the unchanged parent compound.4

Half-life

Reports of the half life of sulpiride have only been performed with small numbers of subjects.2,4 Therefore, the average half life may be 7.15 hours4 to 8.3 hours.2

Clearance

The total systemic clearance of sulpiride if 415 ± 84 mL/min, while the mean renal clearance was 310 ± 91 mL/min.4

Adverse Effects
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Toxicity

Patients experiencing an overdose of sulpiride may present with hypotension, sinus tachycardia, arrhythmia, dystonia, CNS depression, hallucinations, vomiting, agitation, dysarthria, salivation, as well as increased muscle tone, hyperreflexia, and extensor plantar reflex.5 Patients should be treated with symptomatic and supportive treatment.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.
DrugInteraction
1,2-BenzodiazepineThe risk or severity of adverse effects can be increased when Sulpiride is combined with 1,2-Benzodiazepine.
AcebutololSulpiride may increase the bradycardic activities of Acebutolol.
AcenocoumarolThe risk or severity of adverse effects can be increased when Sulpiride is combined with Acenocoumarol.
AcetazolamideThe risk or severity of adverse effects can be increased when Sulpiride is combined with Acetazolamide.
AcetophenazineAcetophenazine may increase the antipsychotic activities of Sulpiride.
AcetylcholineThe risk or severity of adverse effects can be increased when Sulpiride is combined with Acetylcholine.
AcetyldigitoxinThe risk or severity of QTc prolongation can be increased when Sulpiride is combined with Acetyldigitoxin.
AclidiniumAclidinium may increase the anticholinergic activities of Sulpiride.
AcrivastineThe risk or severity of QTc prolongation can be increased when Acrivastine is combined with Sulpiride.
AdenosineThe risk or severity of QTc prolongation can be increased when Sulpiride is combined with Adenosine.
Interactions
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Food Interactions
  • Avoid alcohol. Alcohol enhances the sedative effects of sulpiride.

Products

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International/Other Brands
Bosnyl / Dogmatil / Dogmatyl / Dolmatil / Eglonyl / Espiride / Meresa / Modal

Categories

ATC Codes
N05AL01 — Sulpiride
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as benzenesulfonamides. These are organic compounds containing a sulfonamide group that is S-linked to a benzene ring.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Benzenesulfonamides
Direct Parent
Benzenesulfonamides
Alternative Parents
Benzenesulfonyl compounds / Phenoxy compounds / Methoxybenzenes / Anisoles / Alkyl aryl ethers / Organosulfonamides / N-alkylpyrrolidines / Aminosulfonyl compounds / Trialkylamines / Propargyl-type 1,3-dipolar organic compounds
show 5 more
Substituents
Alkyl aryl ether / Amine / Aminosulfonyl compound / Anisole / Aromatic heteromonocyclic compound / Azacycle / Benzenesulfonamide / Benzenesulfonyl group / Carboximidic acid / Carboximidic acid derivative
show 23 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
sulfonamide, benzamides, N-alkylpyrrolidine (CHEBI:32168)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
7MNE9M8287
CAS number
15676-16-1
InChI Key
BGRJTUBHPOOWDU-UHFFFAOYSA-N
InChI
InChI=1S/C15H23N3O4S/c1-3-18-8-4-5-11(18)10-17-15(19)13-9-12(23(16,20)21)6-7-14(13)22-2/h6-7,9,11H,3-5,8,10H2,1-2H3,(H,17,19)(H2,16,20,21)
IUPAC Name
N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-sulfamoylbenzamide
SMILES
CCN1CCCC1CNC(=O)C1=C(OC)C=CC(=C1)S(N)(=O)=O

References

General References
  1. Justin-Besancon L, Thominet M, Laville C, Margarit J: [Chemical consitution and biological properties of sulpiride]. C R Acad Hebd Seances Acad Sci D. 1967 Oct 23;265(17):1253-4. [Article]
  2. Imondi AR, Alam AS, Brennan JJ, Hagerman LM: Metabolism of sulpiride in man and rhesus monkeys. Arch Int Pharmacodyn Ther. 1978 Mar;232(1):79-91. [Article]
  3. da Silva Fragoso VM, de Morais Coura CP, Hoppe LY, Soares MA, Silva D, Cortez CM: Binding of Sulpiride to Seric Albumins. Int J Mol Sci. 2016 Jan 4;17(1). pii: ijms17010059. doi: 10.3390/ijms17010059. [Article]
  4. Wiesel FA, Alfredsson G, Ehrnebo M, Sedvall G: The pharmacokinetics of intravenous and oral sulpiride in healthy human subjects. Eur J Clin Pharmacol. 1980 May;17(5):385-91. doi: 10.1007/BF00558453. [Article]
  5. Capel MM, Colbridge MG, Henry JA: Overdose profiles of new antipsychotic agents. Int J Neuropsychopharmacol. 2000 Mar;3(1):51-54. doi: 10.1017/S1461145700001760. [Article]
  6. Jenner P, Marsden CD: The mode of action of sulpiride as an atypical antidepressant agent. Adv Biochem Psychopharmacol. 1982;32:85-103. [Article]
  7. Mauri MC, Bravin S, Bitetto A, Rudelli R, Invernizzi G: A risk-benefit assessment of sulpiride in the treatment of schizophrenia. Drug Saf. 1996 May;14(5):288-98. doi: 10.2165/00002018-199614050-00003. [Article]
  8. Kecel-Gunduz S, Budama-Kilinc Y, Cakir-Koc R, Zorlu T, Bicak B, Kokcu Y, Kaya Z, Ozel AE, Akyuz S: In silico Analysis of Sulpiride, Synthesis, Characterization and In vitro Studies of its Nanoparticle for the Treatment of Schizophrenia. Curr Comput Aided Drug Des. 2020;16(2):104-121. doi: 10.2174/1573409915666190627125643. [Article]
  9. Moriguchi S, Bies RR, Remington G, Suzuki T, Mamo DC, Watanabe K, Mimura M, Pollock BG, Uchida H: Estimated dopamine D(2) receptor occupancy and remission in schizophrenia: analysis of the CATIE data. J Clin Psychopharmacol. 2013 Oct;33(5):682-5. doi: 10.1097/JCP.0b013e3182979a0a. [Article]
  10. Electronic Medicines Compendium: Sulpiride 200 mg Tablets Summary of Product Characteristics [Link]
  11. AIFA: Levobren (sulpiride) solution for injection, tablet, oral solution [Link]
Human Metabolome Database
HMDB0014535
KEGG Drug
D01226
PubChem Compound
5355
PubChem Substance
46504855
ChemSpider
5162
BindingDB
11638
RxNav
10239
ChEBI
32168
ChEMBL
CHEMBL26
Therapeutic Targets Database
DAP000310
PharmGKB
PA164745485
Guide to Pharmacology
GtP Drug Page
Wikipedia
Sulpiride
MSDS
Download (57 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentSchizoaffective Disorders / Schizophrenia / Schizophrenia and Disorders With Psychotic Features1
4CompletedTreatmentSchizophrenia1
4RecruitingPreventionBowel preparation therapy1
3CompletedTreatmentHot Flushes / Menopausal Syndromes1
3TerminatedTreatmentAnxiety Disorders / Dementia / Depression / Psychosomatic Disorders / Schizophrenia1
3Unknown StatusTreatmentPsychosis Nos/Other1
Not AvailableCompletedNot AvailableHealthy Volunteers1
Not AvailableCompletedTreatmentPhysiology, Ocular / Regional Blood Flow1
Not AvailableUnknown StatusNot AvailableSchizophrenia1
Not AvailableUnknown StatusTreatmentMajor depressive disorder, recurrent episode1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, solutionIntramuscular
SyrupOral
CapsuleOral50 mg/1
SolutionOral25 mg/5mL
TabletOral
CapsuleOral
TabletOral200 mg/1
SolutionOral20 mg
SolutionOral0.5 g
SolutionOral
Capsule, coatedOral50 mg
Solution / dropsOral
Injection
Tablet, film coatedOral
TabletOral100 MG
CapsuleOral50 MG
TabletOral50 MG
Tablet, film coatedOral50 MG
TabletOral200 mg
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)178 dec °CPhysProp
logP0.57HOEGBERG,T ET AL. 1986
Caco2 permeability-6.16ADME Research, USCD
pKa9.12EL TAYAR,N ET AL. (1985)
Predicted Properties
PropertyValueSource
Water Solubility0.537 mg/mLALOGPS
logP1.2ALOGPS
logP0.22ChemAxon
logS-2.8ALOGPS
pKa (Strongest Acidic)10.24ChemAxon
pKa (Strongest Basic)8.39ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area101.73 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity88.63 m3·mol-1ChemAxon
Polarizability36.18 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9946
Blood Brain Barrier+0.9444
Caco-2 permeable-0.8957
P-glycoprotein substrateSubstrate0.7319
P-glycoprotein inhibitor INon-inhibitor0.857
P-glycoprotein inhibitor IINon-inhibitor0.8994
Renal organic cation transporterNon-inhibitor0.7685
CYP450 2C9 substrateNon-substrate0.7898
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.54
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.9656
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9409
Ames testNon AMES toxic0.6229
CarcinogenicityNon-carcinogens0.7139
BiodegradationNot ready biodegradable0.8542
Rat acute toxicity1.8612 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8546
hERG inhibition (predictor II)Inhibitor0.549
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0006-0109000000-838e3fc396f400ef6f4b
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0a4i-2901000000-15575a206ad43d931d6a
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0a4i-3900000000-b83b6287d83301602f00
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0a6r-8900000000-5a447dc363e7b3d43351
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-004i-9200000000-0a29790b32c5ae5e192a
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-004i-9000000000-32eb95f9c75cc8d8ee85
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0006-0009000000-b451c07c9adbe534b75c
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-01ox-0049000000-eaadc21e5bafdd34a66e
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-03di-0090000000-16b776d58e4e2dbc163e
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-03di-0090000000-9fda88d7482dee887457
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0006-0009000000-338379e29df68a5396b7
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0006-0209000000-d61c87359158078fa846
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-03di-2931000000-6a28d0dd33433a572e50
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-03di-4940000000-dcee56e4387108740566
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-03di-8960000000-9f1a7605079446735287
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-03e9-9620000000-c3bb475e828d5f8c88aa
MS/MS Spectrum - , positiveLC-MS/MSsplash10-03di-3972000000-4f53a77ce37004c9eac3

Targets

Drugtargets
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Details
1. Dopamine D2 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Potassium channel regulator activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name
DRD2
Uniprot ID
P14416
Uniprot Name
D(2) dopamine receptor
Molecular Weight
50618.91 Da
References
  1. Cavallotti C, Nuti F, Bruzzone P, Mancone M: Age-related changes in dopamine D2 receptors in rat heart and coronary vessels. Clin Exp Pharmacol Physiol. 2002 May-Jun;29(5-6):412-8. [Article]
  2. Jaber M, Tison F, Fournier MC, Bloch B: Differential influence of haloperidol and sulpiride on dopamine receptors and peptide mRNA levels in the rat striatum and pituitary. Brain Res Mol Brain Res. 1994 Apr;23(1-2):14-20. [Article]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Details
2. Dopamine D3 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name
DRD3
Uniprot ID
P35462
Uniprot Name
D(3) dopamine receptor
Molecular Weight
44224.335 Da
References
  1. Lipina TV, Vishnivetskaia GB: [Effect of sulpiride on immobility reflex and pinch-induced catalepsy in CBA/Lac male mice with various social status]. Zh Vyssh Nerv Deiat Im I P Pavlova. 2009 Jul-Aug;59(4):482-7. [Article]
  2. Collo G, Zanetti S, Missale C, Spano P: Dopamine D3 receptor-preferring agonists increase dendrite arborization of mesencephalic dopaminergic neurons via extracellular signal-regulated kinase phosphorylation. Eur J Neurosci. 2008 Oct;28(7):1231-40. doi: 10.1111/j.1460-9568.2008.06423.x. [Article]
Details
3. Carbonic anhydrase 2
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Zinc ion binding
Specific Function
Essential for bone resorption and osteoclast differentiation (By similarity). Reversible hydration of carbon dioxide. Can hydrate cyanamide to urea. Involved in the regulation of fluid secretion in...
Gene Name
CA2
Uniprot ID
P00918
Uniprot Name
Carbonic anhydrase 2
Molecular Weight
29245.895 Da
References
  1. Nishimori I, Minakuchi T, Onishi S, Vullo D, Cecchi A, Scozzafava A, Supuran CT: Carbonic anhydrase inhibitors: cloning, characterization, and inhibition studies of the cytosolic isozyme III with sulfonamides. Bioorg Med Chem. 2007 Dec 1;15(23):7229-36. Epub 2007 Aug 25. [Article]
Details
4. Carbonic anhydrase 3
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Zinc ion binding
Specific Function
Reversible hydration of carbon dioxide.
Gene Name
CA3
Uniprot ID
P07451
Uniprot Name
Carbonic anhydrase 3
Molecular Weight
29557.215 Da
References
  1. Nishimori I, Minakuchi T, Onishi S, Vullo D, Cecchi A, Scozzafava A, Supuran CT: Carbonic anhydrase inhibitors: cloning, characterization, and inhibition studies of the cytosolic isozyme III with sulfonamides. Bioorg Med Chem. 2007 Dec 1;15(23):7229-36. Epub 2007 Aug 25. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Sh3 domain binding
Specific 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. Its activity is mediated by G proteins ...
Gene Name
DRD4
Uniprot ID
P21917
Uniprot Name
D(4) dopamine receptor
Molecular Weight
48359.86 Da
References
  1. Ciszowski K, Szpak D, Wilimowska J: [Toxicity of sulpiride]. Przegl Lek. 2010;67(8):606-9. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Identical protein binding
Specific Function
Esterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters.
Gene Name
BCHE
Uniprot ID
P06276
Uniprot Name
Cholinesterase
Molecular Weight
68417.575 Da
References
  1. Vacca C, Maione S, Tozzi A, Marmo E: Benzamides and cholinesterases. Res Commun Chem Pathol Pharmacol. 1987 Feb;55(2):193-201. [Article]
  2. Dross K: [The relevance of anticholinesterase properties to toxicity and neuromuscular effects of sulpiride (author's transl)]. Arzneimittelforschung. 1977 Feb;27(2):404-6. [Article]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. da Silva Fragoso VM, de Morais Coura CP, Hoppe LY, Soares MA, Silva D, Cortez CM: Binding of Sulpiride to Seric Albumins. Int J Mol Sci. 2016 Jan 4;17(1). pii: ijms17010059. doi: 10.3390/ijms17010059. [Article]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Secondary active organic cation transmembrane transporter activity
Specific Function
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
Gene Name
SLC22A1
Uniprot ID
O15245
Uniprot Name
Solute carrier family 22 member 1
Molecular Weight
61153.345 Da
References
  1. Li L, Weng Y, Wang W, Bai M, Lei H, Zhou H, Jiang H: Multiple organic cation transporters contribute to the renal transport of sulpiride. Biopharm Drug Dispos. 2017 Dec;38(9):526-534. doi: 10.1002/bdd.2104. Epub 2017 Nov 20. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Quaternary ammonium group transmembrane transporter activity
Specific Function
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
Gene Name
SLC22A2
Uniprot ID
O15244
Uniprot Name
Solute carrier family 22 member 2
Molecular Weight
62579.99 Da
References
  1. Li L, Weng Y, Wang W, Bai M, Lei H, Zhou H, Jiang H: Multiple organic cation transporters contribute to the renal transport of sulpiride. Biopharm Drug Dispos. 2017 Dec;38(9):526-534. doi: 10.1002/bdd.2104. Epub 2017 Nov 20. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Monovalent cation:proton antiporter activity
Specific Function
Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide (NMN), metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfat...
Gene Name
SLC47A1
Uniprot ID
Q96FL8
Uniprot Name
Multidrug and toxin extrusion protein 1
Molecular Weight
61921.585 Da
References
  1. Takano H, Ito S, Zhang X, Ito H, Zhang MR, Suzuki H, Maeda K, Kusuhara H, Suhara T, Sugiyama Y: Possible Role of Organic Cation Transporters in the Distribution of [(11)C]Sulpiride, a Dopamine D2 Receptor Antagonist. J Pharm Sci. 2017 Sep;106(9):2558-2565. doi: 10.1016/j.xphs.2017.05.006. Epub 2017 May 10. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Drug transmembrane transporter activity
Specific Function
Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide, metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfate, acy...
Gene Name
SLC47A2
Uniprot ID
Q86VL8
Uniprot Name
Multidrug and toxin extrusion protein 2
Molecular Weight
65083.915 Da
References
  1. Takano H, Ito S, Zhang X, Ito H, Zhang MR, Suzuki H, Maeda K, Kusuhara H, Suhara T, Sugiyama Y: Possible Role of Organic Cation Transporters in the Distribution of [(11)C]Sulpiride, a Dopamine D2 Receptor Antagonist. J Pharm Sci. 2017 Sep;106(9):2558-2565. doi: 10.1016/j.xphs.2017.05.006. Epub 2017 May 10. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Toxin transporter activity
Specific Function
Mediates potential-dependent transport of a variety of organic cations. May play a significant role in the disposition of cationic neurotoxins and neurotransmitters in the brain.
Gene Name
SLC22A3
Uniprot ID
O75751
Uniprot Name
Solute carrier family 22 member 3
Molecular Weight
61279.485 Da
References
  1. Bai M, Ma Z, Sun D, Zheng C, Weng Y, Yang X, Jiang T, Jiang H: Multiple drug transporters mediate the placental transport of sulpiride. Arch Toxicol. 2017 Dec;91(12):3873-3884. doi: 10.1007/s00204-017-2008-8. Epub 2017 Jun 9. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Bai M, Ma Z, Sun D, Zheng C, Weng Y, Yang X, Jiang T, Jiang H: Multiple drug transporters mediate the placental transport of sulpiride. Arch Toxicol. 2017 Dec;91(12):3873-3884. doi: 10.1007/s00204-017-2008-8. Epub 2017 Jun 9. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. Bai M, Ma Z, Sun D, Zheng C, Weng Y, Yang X, Jiang T, Jiang H: Multiple drug transporters mediate the placental transport of sulpiride. Arch Toxicol. 2017 Dec;91(12):3873-3884. doi: 10.1007/s00204-017-2008-8. Epub 2017 Jun 9. [Article]

Drug created on June 13, 2005 13:24 / Updated on May 05, 2021 23:19