SULPIRIDE HYDROCHLORIDE

Possibly Marketed Outside US

Details

Stereochemistry	RACEMIC
Molecular Formula	C15H23N3O4S.ClH
Molecular Weight	377.887
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

Cl.CCN1CCCC1CNC(=O)C2=CC(=CC=C2OC)S(N)(=O)=O

InChI

InChIKey=PFHZICSPLHQCDZ-UHFFFAOYSA-N

InChI=1S/C15H23N3O4S.ClH/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);1H

HIDE SMILES / InChI

Molecular Formula	C15H23N3O4S
Molecular Weight	341.426
Charge	0
Count

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

Molecular Formula	ClH
Molecular Weight	36.461
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.drugbank.ca/drugs/DB00391
Curator's Comment: description was created based on several sources, including: https://www.ncbi.nlm.nih.gov/pubmed/6628519

Sulpiride is an atypical antipsychotic drug (although some texts have referred to it as a typical antipsychotic) of the benzamide class used mainly in the treatment of psychosis associated with schizophrenia and major depressive disorder, and sometimes used in low dosage to treat anxiety and mild depression. Sulpiride is commonly used in Europe, Russia and Japan. Sulpiride is a selective antagonist at dopamine D2 and D3 receptors. This action dominates in doses exceeding 600 mg daily. In doses of 600 to 1,600 mg sulpiride shows mild sedating and antipsychotic activity. Its antipsychotic potency compared to chlorpromazine is only 0.2 (1/5). In low doses (in particular 50 to 200 mg daily) its prominent feature is antagonism of presynaptic inhibitory dopamine receptors accounting for some antidepressant activity and a stimulating effect. Therefore, it is in these doses used as a second line antidepressant. Racemic and L-sulpiride significantly decreased stimulated serum gastrin concentration, but they did not affect fasting serum gastrin or basal and stimulated gastric acidity. D-sulpiride significantly decreased gastric acid secretion, without affecting serum gastrin levels.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Dopamine D2 receptor 311 Target ID: CHEMBL217 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21495689	Antagonist 2849		10.28 nM [IC50]
Dopamine D3 receptor 97 Target ID: CHEMBL234 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21495689	Antagonist 2849		66.22 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Schizophrenia 305 Sources: https://clinicaltrials.gov/ct2/show/NCT01615185	Primary		Approved 8583	Eglonyl Approved Use Indications. Acute and chronic psychosis (confusion, delirium, confusion, agrammatism, abulia), schizophrenia; neurotic state, accompanied by lethargy; psychosomatic symptoms (especially for stomach ulcers and duodenal ulcers and hemorrhagic rektokolite).
Major depressive disorder 179 Sources: https://pharmacybook.net/sulpiride/	Primary		Approved 8583	Eglonyl Approved Use Indications. Acute and chronic psychosis (confusion, delirium, confusion, agrammatism, abulia), schizophrenia; neurotic state, accompanied by lethargy; psychosomatic symptoms (especially for stomach ulcers and duodenal ulcers and hemorrhagic rektokolite).

C_max

Value	Dose	Co-administered	Analyte	Population
89.8 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23585286/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:		SULPIRIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
9.03 mg × h/L/(mg dose/kg) EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1815069/	100 mg single, intravenous dose: 100 mg route of administration: Intravenous experiment type: SINGLE co-administered:	SULPIRIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
7.81 mg × h/L/(mg dose/kg) EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1815069/	100 mg single, intramuscular dose: 100 mg route of administration: Intramuscular experiment type: SINGLE co-administered:	SULPIRIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1402.5 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23585286/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	SULPIRIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
6.47 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1815069/	100 mg single, intravenous dose: 100 mg route of administration: Intravenous experiment type: SINGLE co-administered:	SULPIRIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
7.17 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1815069/	100 mg single, intramuscular dose: 100 mg route of administration: Intramuscular experiment type: SINGLE co-administered:	SULPIRIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23585286/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	SULPIRIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

Doses

Dose	Population	Adverse events
3200 mg 2 times / day multiple, oral Highest studied dose Dose: 3200 mg, 2 times / day Route: oral Route: multiple Dose: 3200 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/	Other AEs: Dry mouth, Constipation... Other AEs: Dry mouth (25%) Constipation (19%) Palpitation (6%) Dizziness (12.5%) Fainting (6%) Increased sweating (6%) Parkinsonism (12.5%) Akathisia (44%) Hyperkinesia (19%) Tardive dyskinesia (6%) Drowsiness (12.5%) Itching (19%) Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/

AEs

AE	Significance	Dose	Population
Dizziness	12.5%	3200 mg 2 times / day multiple, oral Highest studied dose Dose: 3200 mg, 2 times / day Route: oral Route: multiple Dose: 3200 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/
Drowsiness	12.5%	3200 mg 2 times / day multiple, oral Highest studied dose Dose: 3200 mg, 2 times / day Route: oral Route: multiple Dose: 3200 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/
Parkinsonism	12.5%	3200 mg 2 times / day multiple, oral Highest studied dose Dose: 3200 mg, 2 times / day Route: oral Route: multiple Dose: 3200 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/
Constipation	19%	3200 mg 2 times / day multiple, oral Highest studied dose Dose: 3200 mg, 2 times / day Route: oral Route: multiple Dose: 3200 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/
Hyperkinesia	19%	3200 mg 2 times / day multiple, oral Highest studied dose Dose: 3200 mg, 2 times / day Route: oral Route: multiple Dose: 3200 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/
Itching	19%	3200 mg 2 times / day multiple, oral Highest studied dose Dose: 3200 mg, 2 times / day Route: oral Route: multiple Dose: 3200 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/
Dry mouth	25%	3200 mg 2 times / day multiple, oral Highest studied dose Dose: 3200 mg, 2 times / day Route: oral Route: multiple Dose: 3200 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/
Akathisia	44%	3200 mg 2 times / day multiple, oral Highest studied dose Dose: 3200 mg, 2 times / day Route: oral Route: multiple Dose: 3200 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/
Fainting	6%	3200 mg 2 times / day multiple, oral Highest studied dose Dose: 3200 mg, 2 times / day Route: oral Route: multiple Dose: 3200 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/
Increased sweating	6%	3200 mg 2 times / day multiple, oral Highest studied dose Dose: 3200 mg, 2 times / day Route: oral Route: multiple Dose: 3200 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/
Palpitation	6%	3200 mg 2 times / day multiple, oral Highest studied dose Dose: 3200 mg, 2 times / day Route: oral Route: multiple Dose: 3200 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/
Tardive dyskinesia	6%	3200 mg 2 times / day multiple, oral Highest studied dose Dose: 3200 mg, 2 times / day Route: oral Route: multiple Dose: 3200 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/6367362/

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 2252	inhibitor 2438	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 2153 CYP2E1 1060 CYP2A6 879 CYP2C19 2057 OATP1B3 961 OATP1B1 1079 CYP19A1 429 BSEP 550	OCT3 92 P-gp 2052 BCRP 697 OCT1 393 OCTN2 59 OCTN1 55 MRP2 252 OCT2 434 OAT4 93

Drug as perpetrator

Target	Modality	Activity
CYP1A2 2333	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzMzU2IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDI2In19	no [IC50 >10 uM]
CYP2A6 911	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw1MjgyIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDI2In19	no [IC50 >10 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNjIyIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDI2In19	no [IC50 >10 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzMzk3IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDI2In19	no [IC50 >10 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwyODkiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMMjYifX0=	no [IC50 >10 uM]
CYP2E1 1146	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw1MjgxIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDI2In19	no [IC50 >10 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNDAiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMMjYifX0=	no [IC50 >10 uM]
BSEP 554	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw2MDIwIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDI2In19	no [IC50 >1000 uM]
CYP19A1 430	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/5355#section=BioAssay-Results Page: 687.0	no
OATP1B1 1095	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwxNjk3NjY4IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDI2In19	yes [Inhibition 10 uM]
OATP1B3 970	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwxNzQzMTIxIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDI2In19	yes [Inhibition 10 uM]

Drug as victim

Target	Modality	Activity
MRP2 252	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/28597291/	no
OAT4 93	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/28597291/	no
OCT3 92	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/28597291/	yes [Km 166 uM]
OCT2 434	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/25155823/	yes [Km 187.2 uM]
OCT1 393	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/25155823/	yes [Km 259.7 uM]
BCRP 697	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/28597291/	yes
OCTN1 55	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/28597291/	yes
OCTN2 59	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/28597291/	yes
P-gp 2052	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/28597291/	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwyNDAiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMMjYifX0=

PubMed

Title	Date	PubMed
Hypothalamic dopaminergic receptor expressions in anorexia of tumor-bearing rats.	2001-12	11705777
Dopaminergic and cholinergic antagonism in a novel-object detection task with rats.	2001-11-29	11704266
Postnatal decrease of sodium current density in rat pituitary melanotropes following the onset of dopaminergic innervation.	2001-11-27	11716982
Development of a high-performance liquid chromatographic method for bioanalytical applications with sulpiride.	2001-11-05	11710574
Involvement of serotonergic and dopaminergic mechanisms in hyperthermia induced by a serotonin-releasing drug, p-chloroamphetamine in mice.	2001-11-02	11711040
Faster response on amisulpride 50 mg versus sertraline 50-100 mg in patients with dysthymia or double depression: a randomized, double-blind, parallel group study.	2001-11	11712619
Dopaminergic modulation of grooming behavior in virgin and pregnant rats.	2001-11	11668358
Prevalence of obesity in adolescent and young adult patients with and without schizophrenia and in relationship to antipsychotic medication.	2001-10-31	11684141
Sulpiride in the treatment of somatoform disorders: results of a European observational study to characterize the responder profile.	2001-10-26	11675904
Modulation of dopamine uptake in rat nucleus accumbens: effect of specific dopamine receptor antagonists and sigma ligands.	2001-10-26	11602337
Hypothalamic CRH mRNA levels are differentially modulated by repeated 'binge' cocaine with or without D(1) dopamine receptor blockade.	2001-10-19	11597771
Detection of pharmacologically mediated changes in cerebral activity by functional magnetic resonance imaging: the effects of sulpiride in the brain of the anaesthetised rat.	2001-10-19	11597597
Novel Ca2+ dependence and time course of somatodendritic dopamine release: substantia nigra versus striatum.	2001-10-01	11567075
Potentiation of opioid analgesia in dopamine2 receptor knock-out mice: evidence for a tonically active anti-opioid system.	2001-10-01	11567069
Catalepsy induced by a blockade of dopamine D1 or D2 receptors was reversed by a concomitant blockade of adenosine A(2A) receptors in the caudate-putamen of rats.	2001-10	11703457
Dopamine mediates striatal malonate toxicity via dopamine transporter-dependent generation of reactive oxygen species and D2 but not D1 receptor activation.	2001-10	11595758
The effects of dopamine and its antagonists on directional delay-period activity of prefrontal neurons in monkeys during an oculomotor delayed-response task.	2001-10	11591439
Characterization of the role of medial prefrontal cortex dopamine receptors in cocaine-induced locomotor activity.	2001-10	11584922
Inverse agonist actions of typical and atypical antipsychotic drugs at the human 5-hydroxytryptamine(2C) receptor.	2001-10	11561066
Changes in muscle tone are regulated by D1 and D2 dopamine receptors in the ventral striatum and D1 receptors in the substantia nigra.	2001-10	11557165
Differential time-course profiles of dopamine release and uptake changes induced by three dopamine uptake inhibitors.	2001-09-15	11494401
Repeated treatment with imipramine, fluvoxamine and tranylcypromine decreases the number of escape failures by activating dopaminergic systems in a rat learned helplessness test.	2001-09-07	11693272
[Incompatibility of olanzapine and amisulpride in multisystemic myotonic myopathy].	2001-09	11572107
Physostigmine as treatment for severe CNS anticholinergic toxicity.	2001-09	11559630
Dopamine D4 receptor activation inhibits presynaptically glutamatergic neurotransmission in the rat supraoptic nucleus.	2001-09	11535665
[Anti-stress effect of nitric oxide].	2001-08-30	11525127
Effects of kappa-opioid receptor agonists on long-term cocaine use and dopamine neurotransmission.	2001-08-24	11525767
A method to evaluate the diffusion rate of drugs from a microdialysis probe through brain tissue.	2001-08-15	11489300
Dopamine D1 and NMDA receptors mediate potentiation of basolateral amygdala-evoked firing of nucleus accumbens neurons.	2001-08-15	11487660
Amphetamine distorts stimulation-dependent dopamine overflow: effects on D2 autoreceptors, transporters, and synaptic vesicle stores.	2001-08-15	11487614
Intra-supraoptic nucleus sulpiride improves anorexia in tumor-bearing rats.	2001-08-08	11496123
A dopaminergic mechanism is involved in the 'anxiogenic-like' response induced by chronic amphetamine treatment: a behavioral and neurochemical study.	2001-08-03	11478934
[Initial experiences with amisulpride, an in Germany novel, atypical neuroleptic drug in treatment of adolescents with psychiatric disorders].	2001-08	11524899
Atypical neuroleptic drugs downregulate dopamine sensitivity in rat cortical and striatal astrocytes.	2001-08	11520180
[Pseudoneurotic schizophrenia: a case report].	2001-07-27	11470063
Adenosine A2A agonist CGS 21680 decreases the affinity of dopamine D2 receptors for dopamine in human striatum.	2001-07-03	11435907
[Participation of the dopaminergic brain system in effects of glucocorticoid hormones].	2001-07	11575124
D2-like dopamine receptor activation excites rat dorsal raphe 5-HT neurons in vitro.	2001-07	11488956
Dopamine D2 receptor mediated presynaptic inhibition of striatopallidal GABA(A) IPSCs in vitro.	2001-07	11445186
A single blind comparison of amisulpride, fluoxetine and clomipramine in the treatment of restricting anorectics.	2001-07	11444677
Accumbens dopamine mechanisms in sucrose intake.	2001-06-15	11516413
Pharmacological characterization of the D1- and D2-like dopamine receptors from the brain of the leopard frog, Rana pipiens.	2001-06	11713387
Neuroendocrine responsivities of the pituitary dopamine system in male schizophrenic patients during treatment with clozapine, olanzapine, risperidone, sulpiride, or haloperidol.	2001-06	11697576
The role of medial prefrontal cortical dopamine in spontaneous flexibility in the rat.	2001-06	11485053
The prolactin response to sulpiride in major depression: the role of the D2 receptor in depression.	2001-06	11418281
Attenuation of morphine dependence and withdrawal in rats by venlafaxine, a serotonin and noradrenaline reuptake inhibitor.	2001-05-25	11411809
Dopamine D2-like receptors and amino acid-induced glomerular hyperfiltration in humans.	2001-05	11421998
The role of the globus pallidus D2 subfamily of dopamine receptors in pallidal immediate early gene expression.	2001	11672604
Short-term modulation of prolactin secretion by melatonin in anestrous ewes following dopamine- and opiate receptor blockade.	2001	11409301
Consensus on the Practical Use of Amisulpride, an Atypical Antipsychotic, in the Treatment of Schizophrenia.	2001	11408792

Patents

Sample Use Guides

In Vivo Use Guide

400mg twice daily the doctor may reduce the dose to 200mg twice daily or increase it to a maximum of 1200mg twice daily

Route of Administration: Oral

In Vitro Use Guide

CHO-K1 D3R cells (DiscoveRx) were seeded at a density of 5000 cells/well in 384-well black, clear-bottom plates. Following 24 h of incubation, the cells were treated with multiple concentrations of the Sulpiride (0-10 μM) in Hanks’ balanced buffer solution containing 2% DMSO. Following a 10 min preincubation, the cells were next treated with an EC95 dose of dopamine (100 nM) and then incubated at 37 C for 90 min. DiscoveRx reagent (2.5) was then added to cells followed by a 60 min incubation at room temperature. Luminescence was measured on a Hamamatsu FDSS μ-cell reader.

Substance Class	Chemical Created by `admin` on `Tue Apr 01 16:31:39 GMT 2025` Edited by `admin` on `Tue Apr 01 16:31:39 GMT 2025`
Record UNII	03U3QUS07J
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

SULPIRIDE HYDROCHLORIDE

Common Name

English

BENZAMIDE, 5-(AMINOSULFONYL)-N-((1-ETHYL-2-PYRROLIDINYL)METHYL)-2-METHOXY-, MONOHYDROCHLORIDE

Preferred Name

English

SULPIRIDE MONOHYDROCHLORIDE

Common Name

English

N-((1-ETHYL-2-PYRROLIDINYL)METHYL)-2-METHOXY-5-SULFAMOYLBENZAMIDE HYDROCHLORIDE

Systematic Name

English

BENZAMIDE, 5-(AMINOSULFONYL)-N-((1-ETHYL-2-PYRROLIDINYL)METHYL)-2-METHOXY-, HYDROCHLORIDE (1:1)

Systematic Name

English

O-ANISAMIDE, N-((1-ETHYL-2-PYRROLIDINYL)METHYL)-5-SULFAMOYL-, MONOHYDROCHLORIDE

Common Name

English

Code System Code Type Description

CAS

23694-14-6