AMISULPRIDE

Details

Stereochemistry	RACEMIC
Molecular Formula	C17H27N3O4S
Molecular Weight	369.479
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCN1CCCC1CNC(=O)C2=C(OC)C=C(N)C(=C2)S(=O)(=O)CC

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	369.479
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 297 Target ID: CHEMBL217 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8996185 \| https://www.ncbi.nlm.nih.gov/pubmed/19337725	Antagonist 2778	2.8 nM [Ki]
Dopamine D3 receptor 91 Target ID: CHEMBL234 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8996185 \| https://www.ncbi.nlm.nih.gov/pubmed/19337725	Antagonist 2778	3.2 nM [Ki]
Serotonin 7 (5-HT7) receptor 31 Target ID: CHEMBL3155 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19337725	Antagonist 2778	11.5 nM [Ki]
Serotonin 2b (5-HT2b) receptor 60 Target ID: CHEMBL1833 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19337725	Antagonist 2778	13.0 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Schizophrenia 298 Sources: http://www.sanofi.com.au/products/aus_pi_solian.pdf	Primary		Approved 8429	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 1737 inhibitor 1587 inducer 781	substrate 1037 inhibitor 1767	substrate 1217 inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2B6 810 CYP2C8 911 CYP2C19 1478 OCT1 512 MATE2 263 OCT2 647 OAT3 642 P-gp 1461 BCRP 699 OATP1B3 706 OAT1 599 OATP1B1 788 MATE1 306 CYP1A2 1524	CYP1A2 1054 CYP2A6 543 CYP2B6 664 CYP2C8 693 CYP2C19 991 CYP2E1 667 P-gp 1537 BCRP 561 MATE2 96 OCT1 327 OATP1B1 406 OATP1B3 350 OAT1 326 OAT3 339 OCT2 355	CYP1A2 701 CYP2B6 547

Drug as perpetrator

Target	Modality	Activity
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no [IC50 46.1 uM]
BCRP 773	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	no [IC50 >100 uM]
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	no [IC50 >100 uM]
CYP1A2 1692	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=179 Page: 179.0	no
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP2B6 1001	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=179 Page: 179.0	no
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP3A4 1925	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=179 Page: 179.0	no
CYP3A4 1925	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
OAT1 603	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	no
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	no
OATP1B3 715	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	no
OAT3 644	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	weak [Inhibition 100 uM]
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	weak [Inhibition 100 uM]
MATE2 263	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	yes [IC50 10.1 uM]
OCT1 543	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	yes [IC50 16.1 uM]
MATE1 308	inhibitor 3277 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 1054	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP2A6 543	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP2B6 664	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP2C19 991	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP2C8 693	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP2C9 1037	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP2D6 1217	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP2E1 667	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
CYP3A4 1737	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=99 Page: 99.0	no
OAT1 326	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	no
OAT3 339	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	no
OATP1B1 406	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	no
OATP1B3 350	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	no
OCT2 355	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=180 Page: 180.0	no
OCT1 327	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=179 Page: 179.0	weak
BCRP 561	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=179 Page: 179.0	yes
MATE2 96	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/209510Orig1s000MultidisciplineR.pdf#page=179 Page: 179.0	yes
P-gp 1537	substrate 3367 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 1647	inhibitor 1626 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
Pharmacology of human dopamine D3 receptor expressed in a mammalian cell line: comparison with D2 receptor.	1992 Apr 10	1354163
Amisulpride: efficacy in the management of chronic patients with predominant negative symptoms of schizophrenia.	2001 Oct	11829208
Amisulpride: is there a treatment for negative symptoms in schizophrenia patients?	2002	12693427
Switching to amisulpride.	2002	12418609
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
Amisulpride for schizophrenia.	2002	12076408
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
Amisulpride, an unusual "atypical" antipsychotic: a meta-analysis of randomized controlled trials.	2002 Feb	11823257
A review of the pharmacokinetics, tolerability and pharmacodynamics of amisulpride in healthy volunteers.	2002 Jan	12404702
New antipsychotic agents for schizophrenia: pharmacokinetics and metabolism update.	2002 Jul	12186270
Effect of the amisulpride isomers on rat prolactinemia.	2002 Jul 19	12144950
The glial growth factors deficiency and synaptic destabilization hypothesis of schizophrenia.	2002 Jul 3	12095426
[Use of atypical antipsychotics in Charles Perrens psychiatric hospital (Bordeaux) analysis of prescribing practices for Amisulpride, Clozapine, Olanzapine and Risperidone].	2002 Jul-Aug	12232542
Variations in prescribing atypical antipsychotic drugs in primary care: cross-sectional study.	2002 Jun	12138596
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
Gateways to clinical trials.	2002 May	12092009
Switching to amisulpride due to hepatic complications.	2002 May	12052579
Amisulpride does not prevent relapse in primary alcohol dependence: results of a pilot randomized, placebo-controlled trial.	2002 Oct	12394288
The differential effects of atypical antipsychotics on prolactin elevation are explained by their differential blood-brain disposition: a pharmacological analysis in rats.	2002 Sep	12183672
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
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
Analysis of eighteen antidepressants, four atypical antipsychotics and active metabolites in serum by liquid chromatography: a simple tool for therapeutic drug monitoring.	2003 Aug 25	12888196
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
Quantification of D2-like dopamine receptors in the human brain with 18F-desmethoxyfallypride.	2003 Jan	12515884
Lack of effect of amisulpride on the pharmacokinetics and safety of lithium.	2003 Jun	12890302
A meta-analysis of the efficacy of second-generation antipsychotics.	2003 Jun	12796218
Rapid high-performance liquid chromatographic measurement of amisulpride in human plasma: application to manage acute intoxication.	2003 Jun 5	12726848
The new and evolving pharmacotherapy of schizophrenia.	2003 Mar	12683264
[Plasma prolactin level and incidence of adverse endocrinologic effects during therapy with atypical neuroleptics].	2003 May	14509051
New generation antipsychotics versus low-potency conventional antipsychotics: a systematic review and meta-analysis.	2003 May 10	12747876
How does the benzamide antipsychotic amisulpride get into the brain?--An in vitro approach comparing amisulpride with clozapine.	2003 Nov	12865899
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
Quetiapine. A review of its use in the management of schizophrenia.	2004	14871161
Combination of amisulpride and olanzapine in treatment-resistant schizophrenic psychoses.	2004 Feb	14969782
Evidence-based pharmacotherapy of schizophrenia.	2004 Jun	15043765
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 `Sat Dec 16 17:29:20 GMT 2023` Edited by `admin` on `Sat Dec 16 17:29:20 GMT 2023`
Record UNII	8110R61I4U
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

AMISULPRIDE

Official Name

English

Amisulpride [WHO-DD]

Common 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

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 [ORANGE BOOK]

Common Name

English

amisulpride [INN]

Common Name

English

AMINOSULTOPRIDE

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C66883