Identification
- Summary
Amisulpride is a dopamine D2 receptor antagonist used in the treatment of acute and chronic schizophrenia, and in the prevention and treatment of postoperative nausea and vomiting in adults.
- Brand Names
- Barhemsys
- Generic Name
- Amisulpride
- DrugBank Accession Number
- DB06288
- Background
Amisulpride is a benzamide derivative and a dopamine receptor antagonist that selectively works on dopamine D2 and D3 receptors. As an antipsychotic agent, amisulpride alleviates both positive and negative symptoms of schizophrenia, and it exhibits antidepressant properties in patients with psychiatric disorders, dysthymia, and major depression.5 Amisulpride predominantly works in the limbic system, which explains its relatively lower risk of extrapyramidal adverse effects compared to other atypical antipsychotic agents.2,11 Oral tablets of amisulpride is used in European countries as a treatment for acute and chronic schizophrenic disorders, as well as secondary negative symptoms in mental health disorders such as affective disorders, depressive mood, and mental retardation.11
Amisulpride is also used as an antiemetic agent. In the US, the intravenous formulation of amisulpride is used to treat and prevent postoperative nausea and vomiting in adults, either as monotherapy or in combination with another antiemetic agent of a different drug class.10 It is marketed under the brand name Barhemsys.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Amisulpride (DB06288)
- Weight
- Average: 369.479
Monoisotopic: 369.172227057 - Chemical Formula
- C17H27N3O4S
- Synonyms
- 4-Amino-N-((1-ethyl-2-pyrrolidinyl)methyl)-5-(ethylsulfonyl)-2-methoxybenzamide
- 4-Amino-N-((1-ethyl-2-pyrrolidinyl)methyl)-5-(ethylsulfonyl)-O-anisamide
- Aminosultopride
- Amisulprida
- Amisulpride
- Amisulpridum
Pharmacology
- Indication
Intravenous amisulpride is indicated in adults for the prevention of postoperative nausea and vomiting, either alone or in combination with an antiemetic of a different class. It is also indicated for the treatment of postoperative nausea and vomiting in patients who have received anti-emetic prophylaxis with an agent of a different class or have not received prophylaxis.10
Oral amisulpride is indicated for the treatment of acute and chronic schizophrenic disorders, characterized by positive symptoms with delusions, hallucinations, thought disorders, hostility and suspicious behavior; or primarily negative symptoms (deficit syndrome) with blunted affect, emotional and social withdrawal. Amisulpride also controls secondary negative symptoms in productive conditions as well as affective disorders such as depressive mood or retardation.11
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Acute schizophrenia •••••••••••• ••••••••• •••••• Treatment of Chronic schizophrenia •••••••••••• ••••••••• •••••• Treatment of Negative symptom •••••••••••• ••••••••• •••••• Treatment of Negative symptom •••••••••••• ••••••••• •••••• Treatment of Negative symptom •••••••••••• ••••••••• •••••• - 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
Amisulpride is a selective dopamine D2 and D3 receptor antagonist with no affinity towards other dopamine receptor subtypes. Amisulpride is an atypical antipsychotic agent that works as an antagonist at dopamine receptors in the limbic system. Since it works preferentially in the limbic system, amisulpride is less likely to be associated with extrapyramidal adverse effects than other atypical antipsychotic agents. Amisulpride has no affinity for serotonin, alpha-adrenergic, H1-histamine, cholinergic, and sigma receptors. In clinical trials, amisulpride improved reduced secondary negative symptoms, affective symptoms, and psychomotor retardation in patients with acute exacerbation of schizophrenia. Notably, amisulpride has a differential target binding profile at different doses: at low doses, amisulpride selectively binds to presynaptic dopamine autoreceptors. At high doses, it preferentially binds to post-synaptic dopamine receptors.3 This explains how amisulpride reduces negative symptoms at low doses and mediates antipsychotic effects at high doses.11 One study alluded that the antinociceptive effects of amisulpride are mediated through opioid receptor acvitation and D2 receptor antagonism. 3,5 The actions of amisulpride at opioid receptors may explain its pro-convulsant properties.5
Amisulpride is also an antiemetic agent that prevents and alleviates postoperative nausea and vomiting. It primarily works by blocking dopamine signalling in the chemoreceptor trigger zone, which is a brain area that relays stimuli to the vomiting center.11
In clinical trials comprising Caucasian and Japanese subjects, amisulpride caused dose- and concentration-dependent prolongation of the QT interval; thus, intravenous infusion under a strict dosing regimen and close monitoring of patients with pre-existing cardiovascular conditions are recommended.10 Amisulpride increases plasma prolactin levels, leading to an association with benign pituitary tumours such as prolactinoma.11
- Mechanism of action
Dopamine is an essential and critical neurotransmitter produced in the substantia nigra and ventral tegmental regions of the brain. Dopaminergic projection function in the nigrostriatal, mesolimbic, and mesocortical systems. Hyperactive dopamine transmission in the mesolimbic areas, or dopamine dysregulation in various major brain regions, is understood as the key driver of positive and negative symptoms of schizophrenia.9 Many antipsychotic agents act as D2 receptor antagonists, as with amisulpride.2 Amisulpride is a selective dopamine D2 and D3 receptor antagonist.10 It has high preferential activity towards dopamine receptors in the limbic system rather than the striatum, leading to a lower risk of extrapyramidal side effects than other atypical antipsychotic agents.4,6 At low doses, amisulpride reduces negative symptoms of schizophrenia by blocking pre-synaptic dopamine D2 and D3 receptors, increasing the levels of dopamine in the synaptic cleft and facilitating dopaminergic transmission.4 At higher doses, amisulpride blocks postsynaptic receptors, inhibiting dopaminergic hyperactivity: this explains the drug improving positive symptoms.1 Amisulpride also works as an antagonist at 5-HT7A receptors 8 and 5-HT2A receptors,4 which may be related to its antidepressant effects.5
The chemoreceptor trigger zone (CTZ), also commonly known as the area postrema (AP), is an important brain region located within the dorsal surface of the medulla oblongata. CTZ is involved in emesis: it contains receptors, such as dopamine receptors, that are activated in response to emetic agents in the blood and relay information to the vomiting center, which is responsible for inducing the vomiting reflex.7 Amisulpride is an antiemetic agent that works to limit signals that promote nausea and vomiting. Amisulpride binds to D2 and D3 receptors in the CTZ, leading to reduced dopaminergic signalling into the vomiting center.10
Target Actions Organism A5-hydroxytryptamine receptor 7 antagonistHumans A5-hydroxytryptamine receptor 2A antagonistHumans ADopamine D2 receptor antagonistHumans ADopamine D3 receptor antagonistHumans NMu-type opioid receptor agonistHumans NDelta-type opioid receptor agonistHumans NKappa-type opioid receptor agonistHumans - Absorption
Following oral administration, amisulpride is rapidly absorbed with absolute bioavailability of 48%.1 Amisulpride has two absorption peaks, with one rapidly achieved within one hour post-dose and a second peak occurring between three to four hours post-dose. Following oral administration of a 50 mg dose, two peak plasma concentrations were 39 ± 3 and 54 ± 4 ng/mL.11
Following intravenous administration, the peak plasma concentration of amisulpride is achieved at the end of the infusion period and the plasma concentration decreases by 50% within approximately 15 minutes. The AUC(0-∞) increases dose-proportionally in the dose range from 5 mg to 40 mg, which is about four times the maximum recommended dose. In healthy patients receiving intravenous amisulpride, the mean (SD) Cmax was 200 (139) ng/mL at the dose of 5 mg and 451 (230) ng/mL at the dose of 10 mg. The AUC ranged from 136 to 154 ng x h/mL in the dose range of 5 mg to 10 mg. In patients undergoing surgery, the mean (SD) Cmax ranged from 127 (62) to 161 (58) ng/mL at the dose of 5 mg. At the dose of 10 mg, it was 285 (446) ng/mL. The AUC ranged from 204 to 401 ng x h/mL.10
- Volume of distribution
Following oral administration, the volume of distribution is 5.8 L/kg.11 Following intravenous infusion, the mean volume of distribution of amisulpride is estimated to be 127 to 144 L in surgical patients and 171 L in healthy subjects.10
- Protein binding
Plasma protein binding ranges from 25% to 30% in the concentration range from 37 to 1850 ng/mL. Amisulpride distributes into erythrocytes.10
- Metabolism
Amisulpride undergoes minimal metabolism 1 and its metabolites in plasma are largely undetectable. Two identified metabolites, formed by de-ethylation and oxidation, are pharmacologically inactive 6 and account for approximately 4% of the dose.11 Metabolites remain largely uncharacterized. Metabolism of amisulpride does not involve cytochrome P450 enzymes.10
- Route of elimination
Following intravenous administration, about 74% of amisulpride is excreted in urine, where 58% of the recovered dose was excreted as unchanged amisulpride. About 23% of the dose is excreted in feces, with 20% of the excreted dose as unchanged parent drug. Following intravenous administration, about four metabolites were identified in urine and feces, accounting for less than 7% of the total dose administered.10 About 22 to 25% of orally administered amisulpride is excreted in urine, mostly as the unchanged parent drug.1
- Half-life
Elimination is biphasic.6 The elimination half-life of amisulpride is approximately 12 hours after an oral dose.11 The mean elimination half-life is approximately four to five hours in both healthy subjects and patients undergoing surgery receiving intravenous amisulpride.10
- Clearance
The plasma clearance of amisulpride is 20.6 L/h in surgical patients and 24.1 L/h in healthy subjects following intravenous administration. Renal clearance was estimated to be 20.5 L/hr (342 mL/min) in healthy subjects.10
- Adverse Effects
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In mice, oral LD50 is 1024 mg/kg, intraperitoneal LD50 is 175 mg/kg, and subcutaneous LD50 is 224 mg/kg. The Lowest published toxic dose (TDLo) following subcutaneous administration is 0.24 mg/kg in rats. The oral TDLo in men is 4.3 mg/kg.12
Oral doses of amisulpride above 1200 mg/day are associated with adverse effects related to dopamine-2 (D2) antagonism. Cardiovascular adverse reactions include prolongation of the QT interval, torsades de pointes, bradycardia, and hypotension. Neuropsychiatric adverse reactions include sedation, coma, seizures, and dystonic and extrapyramidal reactions. As there is no specific antidote for amisulpride overdosage, management includes cardiac monitoring and treatment of severe extrapyramidal symptoms. Drug elimination with the use of hemodialysis is effective.10 Severe extrapyramidal effects may be managed with anticholinergic drugs.11
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- 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 Amisulpride is combined with 1,2-Benzodiazepine. Acenocoumarol The risk or severity of adverse effects can be increased when Amisulpride is combined with Acenocoumarol. Acetazolamide The risk or severity of CNS depression can be increased when Acetazolamide is combined with Amisulpride. Acetophenazine Acetophenazine may increase the antipsychotic activities of Amisulpride. Acrivastine The risk or severity of QTc prolongation can be increased when Amisulpride is combined with Acrivastine. - Food Interactions
- Avoid alcohol. Amisulpride may enhance the effects of alcohol.
- Take with or without food. A high fat meal does not significantly affect drug pharmacokinetics, although a carbohydrate rich meal decreases drug absorption and levels.
Products
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- Deniban (Sanofi-Aventis) / Solian (Sanofi-Aventis)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Barhemsys Injection, solution 2.5 mg/1mL Intravenous Acacia Pharma Ltd 2020-02-27 Not applicable US 
Categories
- ATC Codes
- N05AL05 — Amisulpride
- Drug Categories
- Acids, Carbocyclic
- Amides
- Antidepressive Agents
- Antidepressive Agents, Second-Generation
- Antiemetics
- Antipsychotic Agents
- Antipsychotic Agents (Second Generation [Atypical])
- BCRP/ABCG2 Substrates
- Benzamides and benzamide derivatives
- Benzene Derivatives
- Benzoates
- Central Nervous System Agents
- Central Nervous System Depressants
- Dopamine Agents
- Dopamine Antagonists
- Dopamine D2 Receptor Antagonists
- MATE 1 Inhibitors
- MATE 1 Substrates
- MATE 2 Inhibitors
- MATE 2 Substrates
- MATE inhibitors
- MATE substrates
- Nervous System
- Neurotoxic agents
- Neurotransmitter Agents
- OCT1 substrates
- Opioid Agonist
- P-glycoprotein substrates
- Potential QTc-Prolonging Agents
- Psycholeptics
- Psychotropic Drugs
- QTc Prolonging Agents
- Serotonin 5-HT2 Receptor Antagonists
- Serotonin 5-HT2A Receptor Antagonists
- Serotonin Agents
- Serotonin Receptor Antagonists
- Tranquilizing Agents
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as aminobenzamides. These are organic compounds containing a benzamide moiety with an amine group attached to the benzene ring.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Benzene and substituted derivatives
- Sub Class
- Benzoic acids and derivatives
- Direct Parent
- Aminobenzamides
- Alternative Parents
- Aminophenyl ethers / Methoxyanilines / Benzenesulfonyl compounds / Benzamides / Phenoxy compounds / Methoxybenzenes / Anisoles / Benzoyl derivatives / Alkyl aryl ethers / N-alkylpyrrolidines show 9 more
- Substituents
- Alkyl aryl ether / Amine / Amino acid or derivatives / Aminobenzamide / Aminophenyl ether / Aniline or substituted anilines / Anisole / Aromatic heteromonocyclic compound / Azacycle / Benzamide show 26 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- sulfone, benzamides, pyrrolidines, aromatic amine, aromatic amide (CHEBI:64045)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 8110R61I4U
- CAS number
- 71675-85-9
- InChI Key
- NTJOBXMMWNYJFB-UHFFFAOYSA-N
- InChI
- InChI=1S/C17H27N3O4S/c1-4-20-8-6-7-12(20)11-19-17(21)13-9-16(25(22,23)5-2)14(18)10-15(13)24-3/h9-10,12H,4-8,11,18H2,1-3H3,(H,19,21)
- IUPAC Name
- 4-amino-5-(ethanesulfonyl)-N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxybenzamide
- SMILES
- CCN1CCCC1CNC(=O)C1=CC(=C(N)C=C1OC)S(=O)(=O)CC
References
- Synthesis Reference
- US4401822
- General References
- Rosenzweig P, Canal M, Patat A, Bergougnan L, Zieleniuk I, Bianchetti G: A review of the pharmacokinetics, tolerability and pharmacodynamics of amisulpride in healthy volunteers. Hum Psychopharmacol. 2002 Jan;17(1):1-13. [Article]
- Moller HJ: Amisulpride: limbic specificity and the mechanism of antipsychotic atypicality. Prog Neuropsychopharmacol Biol Psychiatry. 2003 Oct;27(7):1101-11. [Article]
- Weizman T, Pick CG, Backer MM, Rigai T, Bloch M, Schreiber S: The antinociceptive effect of amisulpride in mice is mediated through opioid mechanisms. Eur J Pharmacol. 2003 Oct 8;478(2-3):155-9. [Article]
- Leucht S, Pitschel-Walz G, Engel RR, Kissling W: Amisulpride, an unusual "atypical" antipsychotic: a meta-analysis of randomized controlled trials. Am J Psychiatry. 2002 Feb;159(2):180-90. [Article]
- Rehni AK, Singh TG, Chand P: Amisulpride-induced seizurogenic effect: a potential role of opioid receptor-linked transduction systems. Basic Clin Pharmacol Toxicol. 2011 May;108(5):310-7. doi: 10.1111/j.1742-7843.2010.00655.x. Epub 2010 Dec 22. [Article]
- Curran MP, Perry CM: Amisulpride: a review of its use in the management of schizophrenia. Drugs. 2001;61(14):2123-50. doi: 10.2165/00003495-200161140-00014. [Article]
- MacDougall MR, Sharma S: Physiology, Chemoreceptor Trigger Zone . [Article]
- Abbas AI, Hedlund PB, Huang XP, Tran TB, Meltzer HY, Roth BL: Amisulpride is a potent 5-HT7 antagonist: relevance for antidepressant actions in vivo. Psychopharmacology (Berl). 2009 Jul;205(1):119-28. doi: 10.1007/s00213-009-1521-8. Epub 2009 Apr 1. [Article]
- Brisch R, Saniotis A, Wolf R, Bielau H, Bernstein HG, Steiner J, Bogerts B, Braun K, Jankowski Z, Kumaratilake J, Henneberg M, Gos T: The role of dopamine in schizophrenia from a neurobiological and evolutionary perspective: old fashioned, but still in vogue. Front Psychiatry. 2014 May 19;5:47. doi: 10.3389/fpsyt.2014.00047. eCollection 2014. [Article]
- FDA Approved Drug Products: BARHEMSYS (amisulpride) injection, for intravenous use [Link]
- Summary of Product Characteristics: Amisulpride Oral Tablets [Link]
- Cayman Chemical: Amisulpride Safety Data Sheet [Link]
- External Links
- Human Metabolome Database
- HMDB0015633
- KEGG Drug
- D07310
- PubChem Compound
- 2159
- PubChem Substance
- 99443244
- ChemSpider
- 2074
- BindingDB
- 81790
- 46303
- ChEBI
- 64045
- ChEMBL
- CHEMBL243712
- Therapeutic Targets Database
- DAP000848
- PharmGKB
- PA162565877
- Guide to Pharmacology
- GtP Drug Page
- Wikipedia
- Amisulpride
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Treatment Neurocognitive Function / Tardive Dyskinesia (TD) 1 4 Completed Treatment Psychosis / Schizophrenia 2 4 Completed Treatment Schizoaffective Disorders / Schizophrenia 1 4 Completed Treatment Schizoaffective Disorders / Schizophrenia / Schizophrenia and Disorders With Psychotic Features 1 4 Completed Treatment Schizoaffective Disorders / Schizophrenia / Schizophreniform Disorders 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral 100 MG Tablet, film coated Oral 400 MG Tablet Oral Tablet, film coated Oral Tablet, coated Oral Injection, solution Intravenous 2.5 mg/1mL Tablet Oral 400 MG Solution Oral 100 MG/ML Tablet Oral 200.000 mg Tablet, coated Oral 100 mg Solution / drops 100 mg/ml Tablet, coated Oral 400 mg Tablet Oral 50 mg Tablet, film coated Oral 100 mg Tablet Oral 200 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US9545426 No 2017-01-17 2031-03-10 US US9084765 No 2015-07-21 2031-03-10 US US9889118 No 2018-02-13 2031-03-10 US US10525033 No 2020-01-07 2031-03-10 US US11357753 No 2018-02-09 2038-02-09 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 126-127 https://www.pharmacopoeia.com/Catalogue/Preview?uri=%2Fcontent%2Ffile%2Fproducts%2Fhealthandsafety%2FCat_1143_GB.pdf water solubility Insoluble https://www.pharmacopoeia.com/Catalogue/Preview?uri=%2Fcontent%2Ffile%2Fproducts%2Fhealthandsafety%2FCat_1143_GB.pdf logP 1.06 MANNHOLD,R ET AL. (1990) pKa 9.37 Not Available - Predicted Properties
Property Value Source Water Solubility 0.293 mg/mL ALOGPS logP 1.5 ALOGPS logP 0.25 Chemaxon logS -3.1 ALOGPS pKa (Strongest Acidic) 14.03 Chemaxon pKa (Strongest Basic) 8.28 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 6 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 101.73 Å2 Chemaxon Rotatable Bond Count 7 Chemaxon Refractivity 99.84 m3·mol-1 Chemaxon Polarizability 39.82 Å3 Chemaxon Number of Rings 2 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 + 0.864 Blood Brain Barrier + 0.9441 Caco-2 permeable - 0.7127 P-glycoprotein substrate Substrate 0.7242 P-glycoprotein inhibitor I Non-inhibitor 0.8209 P-glycoprotein inhibitor II Non-inhibitor 0.8668 Renal organic cation transporter Non-inhibitor 0.7899 CYP450 2C9 substrate Non-substrate 0.794 CYP450 2D6 substrate Non-substrate 0.8272 CYP450 3A4 substrate Substrate 0.5667 CYP450 1A2 substrate Non-inhibitor 0.8888 CYP450 2C9 inhibitor Non-inhibitor 0.8348 CYP450 2D6 inhibitor Non-inhibitor 0.8572 CYP450 2C19 inhibitor Non-inhibitor 0.8578 CYP450 3A4 inhibitor Non-inhibitor 0.8942 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9081 Ames test Non AMES toxic 0.5931 Carcinogenicity Non-carcinogens 0.6637 Biodegradation Not ready biodegradable 0.8868 Rat acute toxicity 2.4706 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9398 hERG inhibition (predictor II) Inhibitor 0.7128
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 202.0668392 predictedDarkChem Lite v0.1.0 [M-H]- 181.99512 predictedDeepCCS 1.0 (2019) [M+H]+ 203.4629392 predictedDarkChem Lite v0.1.0 [M+H]+ 184.41965 predictedDeepCCS 1.0 (2019) [M+Na]+ 202.7511392 predictedDarkChem Lite v0.1.0 [M+Na]+ 191.94908 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Serotonin receptor activity
- Specific 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 ...
- Gene Name
- HTR7
- Uniprot ID
- P34969
- Uniprot Name
- 5-hydroxytryptamine receptor 7
- Molecular Weight
- 53554.43 Da
References
- Abbas AI, Hedlund PB, Huang XP, Tran TB, Meltzer HY, Roth BL: Amisulpride is a potent 5-HT7 antagonist: relevance for antidepressant actions in vivo. Psychopharmacology (Berl). 2009 Jul;205(1):119-28. doi: 10.1007/s00213-009-1521-8. Epub 2009 Apr 1. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Virus receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
- Gene Name
- HTR2A
- Uniprot ID
- P28223
- Uniprot Name
- 5-hydroxytryptamine receptor 2A
- Molecular Weight
- 52602.58 Da
References
- Tyson PJ, Roberts KH, Mortimer AM: Are the cognitive effects of atypical antipsychotics influenced by their affinity to 5HT-2A receptors? Int J Neurosci. 2004 Jun;114(6):593-611. [Article]
- Leucht S, Pitschel-Walz G, Engel RR, Kissling W: Amisulpride, an unusual "atypical" antipsychotic: a meta-analysis of randomized controlled trials. Am J Psychiatry. 2002 Feb;159(2):180-90. [Article]
- 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
- Rosenzweig P, Canal M, Patat A, Bergougnan L, Zieleniuk I, Bianchetti G: A review of the pharmacokinetics, tolerability and pharmacodynamics of amisulpride in healthy volunteers. Hum Psychopharmacol. 2002 Jan;17(1):1-13. [Article]
- Horacek J, Bubenikova-Valesova V, Kopecek M, Palenicek T, Dockery C, Mohr P, Hoschl C: Mechanism of action of atypical antipsychotic drugs and the neurobiology of schizophrenia. CNS Drugs. 2006;20(5):389-409. [Article]
- Seeman P: Atypical antipsychotics: mechanism of action. Can J Psychiatry. 2002 Feb;47(1):27-38. [Article]
- Xiberas X, Martinot JL, Mallet L, Artiges E, Canal M, Loc'h C, Maziere B, Paillere-Martinot ML: In vivo extrastriatal and striatal D2 dopamine receptor blockade by amisulpride in schizophrenia. J Clin Psychopharmacol. 2001 Apr;21(2):207-14. doi: 10.1097/00004714-200104000-00013. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- 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
- Rosenzweig P, Canal M, Patat A, Bergougnan L, Zieleniuk I, Bianchetti G: A review of the pharmacokinetics, tolerability and pharmacodynamics of amisulpride in healthy volunteers. Hum Psychopharmacol. 2002 Jan;17(1):1-13. [Article]
- Horacek J, Bubenikova-Valesova V, Kopecek M, Palenicek T, Dockery C, Mohr P, Hoschl C: Mechanism of action of atypical antipsychotic drugs and the neurobiology of schizophrenia. CNS Drugs. 2006;20(5):389-409. [Article]
- Seeman P: Atypical antipsychotics: mechanism of action. Can J Psychiatry. 2002 Feb;47(1):27-38. [Article]
- Xiberas X, Martinot JL, Mallet L, Artiges E, Canal M, Loc'h C, Maziere B, Paillere-Martinot ML: In vivo extrastriatal and striatal D2 dopamine receptor blockade by amisulpride in schizophrenia. J Clin Psychopharmacol. 2001 Apr;21(2):207-14. doi: 10.1097/00004714-200104000-00013. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Agonist
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone...
- Gene Name
- OPRM1
- Uniprot ID
- P35372
- Uniprot Name
- Mu-type opioid receptor
- Molecular Weight
- 44778.855 Da
References
- Weizman T, Pick CG, Backer MM, Rigai T, Bloch M, Schreiber S: The antinociceptive effect of amisulpride in mice is mediated through opioid mechanisms. Eur J Pharmacol. 2003 Oct 8;478(2-3):155-9. [Article]
- Rehni AK, Singh TG, Chand P: Amisulpride-induced seizurogenic effect: a potential role of opioid receptor-linked transduction systems. Basic Clin Pharmacol Toxicol. 2011 May;108(5):310-7. doi: 10.1111/j.1742-7843.2010.00655.x. Epub 2010 Dec 22. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Agonist
- General Function
- Opioid receptor activity
- Specific Function
- G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine n...
- Gene Name
- OPRD1
- Uniprot ID
- P41143
- Uniprot Name
- Delta-type opioid receptor
- Molecular Weight
- 40368.235 Da
References
- Weizman T, Pick CG, Backer MM, Rigai T, Bloch M, Schreiber S: The antinociceptive effect of amisulpride in mice is mediated through opioid mechanisms. Eur J Pharmacol. 2003 Oct 8;478(2-3):155-9. [Article]
- Rehni AK, Singh TG, Chand P: Amisulpride-induced seizurogenic effect: a potential role of opioid receptor-linked transduction systems. Basic Clin Pharmacol Toxicol. 2011 May;108(5):310-7. doi: 10.1111/j.1742-7843.2010.00655.x. Epub 2010 Dec 22. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Agonist
- General Function
- Opioid receptor activity
- Specific Function
- G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synt...
- Gene Name
- OPRK1
- Uniprot ID
- P41145
- Uniprot Name
- Kappa-type opioid receptor
- Molecular Weight
- 42644.665 Da
References
- Weizman T, Pick CG, Backer MM, Rigai T, Bloch M, Schreiber S: The antinociceptive effect of amisulpride in mice is mediated through opioid mechanisms. Eur J Pharmacol. 2003 Oct 8;478(2-3):155-9. [Article]
- Rehni AK, Singh TG, Chand P: Amisulpride-induced seizurogenic effect: a potential role of opioid receptor-linked transduction systems. Basic Clin Pharmacol Toxicol. 2011 May;108(5):310-7. doi: 10.1111/j.1742-7843.2010.00655.x. Epub 2010 Dec 22. [Article]
Carriers
References
- FDA Approved Drug Products: BARHEMSYS (amisulpride) injection, for intravenous use [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- 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
- FDA Approved Drug Products: BARHEMSYS (amisulpride) injection, for intravenous use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- 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
- FDA Approved Drug Products: BARHEMSYS (amisulpride) injection, for intravenous use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- 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
- FDA Approved Drug Products: BARHEMSYS (amisulpride) injection, for intravenous use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- 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
- FDA Approved Drug Products: BARHEMSYS (amisulpride) injection, for intravenous use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- 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
- FDA Approved Drug Products: BARHEMSYS (amisulpride) injection, for intravenous use [Link]
Drug created at March 19, 2008 16:22 / Updated at May 10, 2021 12:36