AMISULPRIDE

Details

Stereochemistry	RACEMIC
Molecular Formula	C17H27N3O4S
Molecular Weight	369.4807
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCN1CCCC1CN=C(c2cc(c(cc2OC)N)S(=O)(=O)CC)O

InChI

InChIKey=NTJOBXMMWNYJFB-UHFFFAOYSA-N

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)

HIDE SMILES / InChI

Molecular Formula	C17H27N3O4S
Molecular Weight	369.4807
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description
Sources: http://www.sanofi.com.au/products/aus_pi_solian.pdf
Curator's Comment:: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/8996185 | https://www.ncbi.nlm.nih.gov/pubmed/19337725 | https://www.ncbi.nlm.nih.gov/pubmed/11735643

Amisulpride, a benzamide derivative, shows a unique therapeutic profile being atypical antipsychotic. At low doses, it enhances dopaminergic neurotransmission by preferentially blocking presynaptic dopamine D2/D3 autoreceptors. At higher doses, amisupride antagonises postsynaptic dopamine D2 and D3 receptors, preferentially in the limbic system rather than the striatum, thereby reducing dopaminergic transmission. In addition its antagonism at serotonin 5-HT7 receptors likely underlies the antidepressant actions. Amisulpride is approved for clinical use in treating schizophrenia in a number of European countries and also for treating dysthymia, a mild form of depression, in Italy.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Dopamine D2 receptor 283 Target ID: CHEMBL217 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8996185 \| https://www.ncbi.nlm.nih.gov/pubmed/19337725	Antagonist 2575	2.8 nM [Ki]
Dopamine D3 receptor 85 Target ID: CHEMBL234 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8996185 \| https://www.ncbi.nlm.nih.gov/pubmed/19337725	Antagonist 2575	3.2 nM [Ki]
Serotonin 7 (5-HT7) receptor 22 Target ID: CHEMBL3155 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19337725	Antagonist 2575	11.5 nM [Ki]
Serotonin 2b (5-HT2b) receptor 54 Target ID: CHEMBL1833 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19337725	Antagonist 2575	13.0 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Schizophrenia 276 Sources: http://www.sanofi.com.au/products/aus_pi_solian.pdf	Primary		Approved 8043	SOLIAN Approved Use Amisulpride is indicated for the treatment of acute and chronic schizophrenic disorders, in which positive symptoms (such as delusions, hallucinations, thought disorders) and/or negative symptoms (such as blunted affect, emotional and social withdrawal) are prominent, including patients characterised by predominant negative symptoms.

C_max

Value	Dose	Co-administered	Analyte	Population
586.3 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/28793958	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:		AMISULPRIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Co-administered	Analyte	Population
5043.2 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/28793958	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:		AMISULPRIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Co-administered	Analyte	Population
11.7 h REVIEW https://www.ncbi.nlm.nih.gov/pubmed/12404702	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:		AMISULPRIDE unknown	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
6 g single, oral Overdose Dose: 6 g Route: oral Route: single Dose: 6 g Sources: https://pubmed.ncbi.nlm.nih.gov/20531221	unhealthy, 29 years (range: 23-40 years) n = 23 Health Status: unhealthy Age Group: 29 years (range: 23-40 years) Sex: M+F Population Size: 23 Sources: https://pubmed.ncbi.nlm.nih.gov/20531221	Other AEs: Bradycardia, Dystonic reaction... Other AEs: Bradycardia (24%) Dystonic reaction (2 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/20531221
6 g single, oral Overdose Dose: 6 g Route: oral Route: single Dose: 6 g Sources: https://pubmed.ncbi.nlm.nih.gov/20531221	unhealthy, 29 years (range: 23-40 years) n = 49 Health Status: unhealthy Age Group: 29 years (range: 23-40 years) Sex: M+F Population Size: 49 Sources: https://pubmed.ncbi.nlm.nih.gov/20531221	Other AEs: QT interval prolonged, Tachycardia... Other AEs: QT interval prolonged (64%) Tachycardia (23%) Sources: https://pubmed.ncbi.nlm.nih.gov/20531221
80 g single, oral Overdose Dose: 80 g Route: oral Route: single Dose: 80 g Sources: https://pubmed.ncbi.nlm.nih.gov/20531221	unhealthy, 29 years (range: 23-40 years) n = 49 Health Status: unhealthy Age Group: 29 years (range: 23-40 years) Sex: M+F Population Size: 49 Sources: https://pubmed.ncbi.nlm.nih.gov/20531221	Other AEs: Torsades de pointes... Other AEs: Torsades de pointes (7%) Sources: https://pubmed.ncbi.nlm.nih.gov/20531221
20 mg single, intravenous Highest studied dose Dose: 20 mg Route: intravenous Route: single Dose: 20 mg Sources: https://pubmed.ncbi.nlm.nih.gov/28801850	unhealthy n = 18 Health Status: unhealthy Population Size: 18 Sources: https://pubmed.ncbi.nlm.nih.gov/28801850	Sources: https://pubmed.ncbi.nlm.nih.gov/28801850
200 mg single, oral Highest studied dose Dose: 200 mg Route: oral Route: single Dose: 200 mg Sources: https://pubmed.ncbi.nlm.nih.gov/28793958	healthy n = 20 Health Status: healthy Sex: M+F Population Size: 20 Sources: https://pubmed.ncbi.nlm.nih.gov/28793958	Sources: https://pubmed.ncbi.nlm.nih.gov/28793958
1200 mg single, oral Overdose Dose: 1200 mg Route: oral Route: single Dose: 1200 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209510s000lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209510s000lbl.pdf	Other AEs: Extrapyramidal disorder... Other AEs: Extrapyramidal disorder Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209510s000lbl.pdf
3000 mg single, oral Overdose Dose: 3000 mg Route: oral Route: single Dose: 3000 mg Sources: https://pubmed.ncbi.nlm.nih.gov/7779461	unhealthy n = 1 Health Status: unhealthy Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/7779461	Other AEs: Hyperthermia, Mydriasis... Other AEs: Hyperthermia (1 patient) Mydriasis (1 patient) Coma (1 patient) Seizures (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/7779461

AEs

AE	Significance	Dose	Population
Dystonic reaction	2 patients	6 g single, oral Overdose Dose: 6 g Route: oral Route: single Dose: 6 g Sources: https://pubmed.ncbi.nlm.nih.gov/20531221	unhealthy, 29 years (range: 23-40 years) n = 23 Health Status: unhealthy Age Group: 29 years (range: 23-40 years) Sex: M+F Population Size: 23 Sources: https://pubmed.ncbi.nlm.nih.gov/20531221
Bradycardia	24%	6 g single, oral Overdose Dose: 6 g Route: oral Route: single Dose: 6 g Sources: https://pubmed.ncbi.nlm.nih.gov/20531221	unhealthy, 29 years (range: 23-40 years) n = 23 Health Status: unhealthy Age Group: 29 years (range: 23-40 years) Sex: M+F Population Size: 23 Sources: https://pubmed.ncbi.nlm.nih.gov/20531221
Tachycardia	23%	6 g single, oral Overdose Dose: 6 g Route: oral Route: single Dose: 6 g Sources: https://pubmed.ncbi.nlm.nih.gov/20531221	unhealthy, 29 years (range: 23-40 years) n = 49 Health Status: unhealthy Age Group: 29 years (range: 23-40 years) Sex: M+F Population Size: 49 Sources: https://pubmed.ncbi.nlm.nih.gov/20531221
QT interval prolonged	64%	6 g single, oral Overdose Dose: 6 g Route: oral Route: single Dose: 6 g Sources: https://pubmed.ncbi.nlm.nih.gov/20531221	unhealthy, 29 years (range: 23-40 years) n = 49 Health Status: unhealthy Age Group: 29 years (range: 23-40 years) Sex: M+F Population Size: 49 Sources: https://pubmed.ncbi.nlm.nih.gov/20531221
Torsades de pointes	7%	80 g single, oral Overdose Dose: 80 g Route: oral Route: single Dose: 80 g Sources: https://pubmed.ncbi.nlm.nih.gov/20531221	unhealthy, 29 years (range: 23-40 years) n = 49 Health Status: unhealthy Age Group: 29 years (range: 23-40 years) Sex: M+F Population Size: 49 Sources: https://pubmed.ncbi.nlm.nih.gov/20531221
Extrapyramidal disorder		1200 mg single, oral Overdose Dose: 1200 mg Route: oral Route: single Dose: 1200 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209510s000lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/209510s000lbl.pdf
Coma	1 patient	3000 mg single, oral Overdose Dose: 3000 mg Route: oral Route: single Dose: 3000 mg Sources: https://pubmed.ncbi.nlm.nih.gov/7779461	unhealthy n = 1 Health Status: unhealthy Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/7779461
Hyperthermia	1 patient	3000 mg single, oral Overdose Dose: 3000 mg Route: oral Route: single Dose: 3000 mg Sources: https://pubmed.ncbi.nlm.nih.gov/7779461	unhealthy n = 1 Health Status: unhealthy Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/7779461
Mydriasis	1 patient	3000 mg single, oral Overdose Dose: 3000 mg Route: oral Route: single Dose: 3000 mg Sources: https://pubmed.ncbi.nlm.nih.gov/7779461	unhealthy n = 1 Health Status: unhealthy Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/7779461
Seizures	1 patient	3000 mg single, oral Overdose Dose: 3000 mg Route: oral Route: single Dose: 3000 mg Sources: https://pubmed.ncbi.nlm.nih.gov/7779461	unhealthy n = 1 Health Status: unhealthy Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/7779461

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1601 inhibitor 1467 inducer 707	substrate 936 inhibitor 1604	substrate 1118 inhibitor 1702	inhibitor 1475

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2B6 717 CYP2C8 818 CYP2C19 1325 OCT1 480 MATE2 251 OCT2 594 OAT3 588 P-gp 1330 BCRP 643 OATP1B3 657 OAT1 554 OATP1B1 733 MATE1 290 CYP1A2 1383	CYP1A2 972 CYP2A6 485 CYP2B6 616 CYP2C8 634 CYP2C19 910 CYP2E1 606 P-gp 1400 BCRP 515 MATE2 91 OCT1 302 OATP1B1 370 OATP1B3 319 OAT1 294 OAT3 305 OCT2 316	CYP1A2 637 CYP2B6 501

Drug as perpetrator

Target	Modality	Activity
CYP2D6 1738	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no [IC50 46.1 uM]
BCRP 713	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	no [IC50 >100 uM]
P-gp 1514	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	no [IC50 >100 uM]
CYP1A2 1532	inducer 1440 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=179 Page: 179.0	no
CYP1A2 1532	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP2B6 884	inducer 1440 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=179 Page: 179.0	no
CYP2B6 884	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP2C19 1392	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP2C8 865	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP2C9 1648	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP3A4 1772	inducer 1440 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=179 Page: 179.0	no
CYP3A4 1772	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
OAT1 558	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	no
OATP1B1 748	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	no
OATP1B3 666	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	no
OAT3 590	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	weak [Inhibition 100 uM]
OCT2 595	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	weak [Inhibition 100 uM]
MATE2 251	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	yes [IC50 10.1 uM]
OCT1 495	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	yes [IC50 16.1 uM]
MATE1 292	inhibitor 3045 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=87 Page: 87.0	yes

Drug as victim

Target	Modality	Activity
CYP1A2 972	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP2A6 485	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP2B6 616	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP2C19 910	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP2C8 634	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP2C9 936	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP2D6 1118	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP2E1 606	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP3A4 1601	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
OAT1 294	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	no
OAT3 305	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	no
OATP1B1 370	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	no
OATP1B3 319	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	no
OCT2 316	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	no
OCT1 302	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=179 Page: 179.0	weak
BCRP 515	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=179 Page: 179.0	yes
MATE2 91	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=179 Page: 179.0	yes
P-gp 1400	substrate 3113 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=179 Page: 179.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1507	inhibitor 1489 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=59 Page: 59.0

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:64045	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:64045
ChemicalBook	CB7312326	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB7312326
MolPort	MolPort-003-983-463	https://www.molport.com/shop/molecule-link/MolPort-003-983-463
Selleck Chemicals	Amisulpride	http://www.selleckchem.com/products/Amisulpride.html
eMolecules	1985473	https://www.emolecules.com/cgi-bin/more?vid=1985473

PubMed

Title	Date	PubMed
Amisulpride: is there a treatment for negative symptoms in schizophrenia patients?	2002	12693427
Amisulpride: progress and outcomes.	2002	12418608
Clinical implications of dopamine research in schizophrenia.	2002	12418605
Long-term effects of the substituted benzamide derivative amisulpride on baseline and stimulated prolactin levels.	2002	12207145
Switching antipsychotic medications: general recommendations and switching to amisulpride.	2002	12201620
Focus on amisulpride.	2002	12094819
Sub-chronic treatment with classical but not atypical antipsychotics produces morphological changes in rat nigro-striatal dopaminergic neurons directly related to "early onset" vacuous chewing.	2002 Apr	11982629
Review: amisulpride is effective and safe for schizophrenia.	2002 Aug	12180452
A comparison of paroxetine and amisulpride in the treatment of dysthymic disorder.	2002 Aug	12128243
Amisulpride improves depressive symptoms in acute exacerbations of schizophrenia: comparison with haloperidol and risperidone.	2002 Aug	12126869
SPECT imaging, clinical features, and cognition before and after low doses of amisulpride in schizophrenic patients with the deficit syndrome.	2002 Aug 20	12165366
Dopaminergic deficit and the role of amisulpride in the treatment of schizophrenia.	2002 Dec	12685918
Dopaminergic deficit and the role of amisulpride in the treatment of mood disorders.	2002 Dec	12685917
Liver function tests during treatment with antipsychotic drugs: a case series of 23 patients.	2002 Dec	12502031
Effects of amisulpride on consummatory negative contrast.	2002 Dec	12478217
Amisulpride vs. risperidone in chronic schizophrenia: results of a 6-month double-blind study.	2002 Dec	12464464
Dose-related effects of amisulpride on five dimensions of psychopathology in patients with acute exacerbation of schizophrenia.	2002 Dec	12454554
Atypical antipsychotics: mechanism of action.	2002 Feb	11873706
A review of the pharmacokinetics, tolerability and pharmacodynamics of amisulpride in healthy volunteers.	2002 Jan	12404702
Efficacy and safety of amisulpride 50 mg versus paroxetine 20 mg in major depression: a randomized, double-blind, parallel group study.	2002 Jan	11800503
Effect of the amisulpride isomers on rat prolactinemia.	2002 Jul 19	12144950
Striatal dopamine-2 receptor occupancy as measured with [123I]iodobenzamide and SPECT predicted the occurrence of EPS in patients treated with atypical antipsychotics and haloperidol.	2002 Jun	12107616
Carmoxirole is able to reduce amisulpride-induced hyperprolactinemia without affecting its central effect.	2002 Jun 28	12106810
Neuroleptic malignant syndrome due to atypical neuroleptics: three episodes in one patient.	2002 May	12107858
Switching to amisulpride due to hepatic complications.	2002 May	12052579
Effect of the amisulpride isomers on rat catalepsy.	2002 May 24	12191584
Age-related changes in dopamine D2 receptors in rat heart and coronary vessels.	2002 May-Jun	12010185
Amisulpride does not prevent relapse in primary alcohol dependence: results of a pilot randomized, placebo-controlled trial.	2002 Oct	12394288
A comparison of paroxetine versus paroxetine plus amisulpride in the treatment of dysthymic disorder: efficacy and psychosocial outcomes.	2002 Oct 10	12429360
Differential effects of high-dose amisulpride versus flupentixol on latent dimensions of depressive and negative symptomatology in acute schizophrenia: an evaluation using confirmatory factor analysis.	2002 Sep	12177587
New generation antipsychotics for first episode schizophrenia.	2003	14584012
Is regionally selective D2/D3 dopamine occupancy sufficient for atypical antipsychotic effect? an in vivo quantitative [123I]epidepride SPET study of amisulpride-treated patients.	2003 Aug	12900302
Which neuroleptic would psychiatrists take for themselves or their relatives?	2003 Feb	12648897
Respective roles of dopamine D2 and D3 receptors in food-seeking behaviour in rats.	2003 Feb	12525958
Automated determination of amisulpride by liquid chromatography with column switching and spectrophotometric detection.	2003 Feb 5	12505788
Amisulpride versus risperidone in the treatment of schizophrenic patients: a double-blind pilot study in Taiwan.	2003 Jan	12684609
[Frontal dysfunctions in Huntington's disease -- neuropsychology and therapy].	2003 Jan	12524580
Quantification of D2-like dopamine receptors in the human brain with 18F-desmethoxyfallypride.	2003 Jan	12515884
The new and evolving pharmacotherapy of schizophrenia.	2003 Mar	12683264
How does the benzamide antipsychotic amisulpride get into the brain?--An in vitro approach comparing amisulpride with clozapine.	2003 Nov	12865899
Amisulpride: limbic specificity and the mechanism of antipsychotic atypicality.	2003 Oct	14642970
Response of catatonic schizophrenia to amisulpride: a case report.	2003 Sep	14574833
Adverse metabolic effects associated with atypical antipsychotics: literature review and clinical implications.	2004	15025545
Amisulpride is an "atypical" antipsychotic associated with low weight gain.	2004 Apr	14647963
Combination of clozapine and amisulpride in treatment-resistant schizophrenia--case reports and review of the literature.	2004 Jan	14750045
Dopaminergic receptors in rat dura mater: pharmacological characteristics.	2004 Mar	15008964
Lower risk for tardive dyskinesia associated with second-generation antipsychotics: a systematic review of 1-year studies.	2004 Mar	14992963
How do we choose between atypical antipsychotics? The advantages of amisulpride.	2004 Mar	14972081
Successful treatment of Tourette's disorder with amisulpride.	2004 May	15010520
Prolactinemia is uncoupled from central D2/D3 dopamine receptor occupancy in amisulpride treated patients.	2004 Sep	14997280

Patents

Sample Use Guides

In Vivo Use Guide

For acute psychotic episodes, oral doses between 400 mg/d and 800 mg/d are recommended. In individual cases, the daily dose may be increased up to 1200 mg/d. Doses above 1200 mg/d have not been extensively evaluated for safety and therefore should not be used. Doses above 800 mg/d have not been shown to be superior to lower doses and may increase the incidence of adverse events. No specific titration is required when initiating the treatment with amisulpride. Doses should be adjusted according to individual response.

Route of Administration: Oral

In Vitro Use Guide

In NG108-15 cells stably transfected with the human D3 dopamine receptor amisulpride inhibited quinpirole-elicited mitogenesis with an IC50 value of 22 nM

Substance Class	Chemical Created by `admin` on `Fri Jun 25 21:12:55 UTC 2021` Edited by `admin` on `Fri Jun 25 21:12:55 UTC 2021`
Record UNII	8110R61I4U
Record Status	`Validated (UNII)`
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Language

AMISULPRIDE

Official Name

English

APD421

Code

English

BARHEMSYS

Brand Name

English

BENZAMIDE, 4-AMINO-N-((1-ETHYL-2-PYRROLIDINYL)METHYL)-5-(ETHYLSULFONYL)-2-METHOXY-

Systematic Name

English

SULAMID

Brand Name

English

AMISULPRIDE [WHO-DD]

Common Name

English

DAN-2163

Code

English

AMISULPRIDE [MI]

Common Name

English

APD-421

Code

English

SOLIAN

Brand Name

English

NSC-760085

Code

English

DENIBAN

Brand Name

English

(+/-)-AMISULPRIDE

Common Name

English

AMISULPRIDE [EP MONOGRAPH]

Common Name

English

SOCIAN

Brand Name

English

AMISULPRIDE [MART.]

Common Name

English

4-AMINO-N-((1-ETHYL-2-PYRROLIDINYL)METHYL)-5-(ETHYLSULFONYL)-O-ANISAMIDE

Common Name

English

AMISULPRIDE [INN]

Common Name

English

AMINOSULTOPRIDE

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C66883