Sulpiride

Summary

Sulpiride (CHEMBL26) is an approved small-molecule antidepressant (ATC N05AL01) targeting DRD2, DRD3, and CA1; indicated across 5 conditions including psychotic disorder and anxiety.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N05AL01
• Targets: 5 (DRD2, DRD3, CA1…)
• Indications: 5 conditions
• Clinical trials: 12
• Chemistry: 341.4 Da · C15H23N3O4S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL26
Name	Sulpiride
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	5355
ChEBI	CHEBI:32168
ATC	N05AL01
Molecular formula	C15H23N3O4S
Molecular weight	341.4
InChIKey	BGRJTUBHPOOWDU-UHFFFAOYSA-N

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

IUPAC name: N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-sulfamoylbenzamide

ChEBI definition: A member of the class of benzamides obtained from formal condensation between the carboxy group of 2-methoxy-5-sulfamoylbenzoic acid and the primary amino group of (1-ethylpyrrolidin-2-yl)methylamine.

Pharmacological roles (ChEBI): antidepressant, antiemetic, antipsychotic agent, dopaminergic antagonist.

Also known as: Abilit, Aiglonyl, Coolspan, Dobren, Dogmatil, Dogmatyl, Dolmatil, Guastil, Meresa, Mirbanil, Misulvan, N05AL01

Patent coverage: 25,200 distinct patent families (58,543 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 58,369 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
DRD2	D2 receptor	Antagonist	7.92	0%	P14416
DRD3	D3 receptor	Antagonist	7.85	0%	P35462
CA1	carbonic anhydrase 1	Inhibition	5.92	0%	P00915
CA12	carbonic anhydrase 12	Inhibition	8.41	0.2%	O43570
CA7	carbonic anhydrase 7	Inhibition	5.44	1.6%	P43166

Broader ChEMBL bioactivity targets: 28 (assay-derived). Sample: Microtubule-associated protein tau, RecQ-like DNA helicase BLM, Alpha-2A adrenergic receptor, Carbonic anhydrase 2, D(1A) dopamine receptor, Dopamine receptor, D(2) dopamine receptor, D(4) dopamine receptor, Prostaglandin G/H synthase 1, Carbonic anhydrase 7.

Bioactivity

ChEMBL activities: 123 potent at pChembl ≥ 5 of 136 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
CA6	9.1	Ki	0.8	nM	CHEMBL_ACT_1804235
CA6	9.1	Ki	0.8	nM	CHEMBL_ACT_2496769
CA6	9.1	Ki	0.8	nM	CHEMBL_ACT_5131591
P61169	8.82	Kd	1.5	nM	CHEMBL_ACT_1283227
BLM	8.8	Potency	1.6	nM	CHEMBL_ACT_4749991
BLM	8.8	Potency	1.6	nM	CHEMBL_ACT_4937874
DRD2	8.55	Kd	2.82	nM	CHEMBL_ACT_18246939
CA7	8.44	Ki	3.6	nM	CHEMBL_ACT_13859513
CA12	8.41	Ki	3.9	nM	CHEMBL_ACT_13440640
CA12	8.41	Ki	3.9	nM	CHEMBL_ACT_13910691
CA12	8.41	Ki	3.9	nM	CHEMBL_ACT_1437700
P61169	8.26	Ki	5.51	nM	CHEMBL_ACT_376124
DRD2	8.12	Ki	7.6	nM	CHEMBL_ACT_14550162
DRD3	8.1	Ki	8	nM	CHEMBL_ACT_690086
DRD2	8.01	Ki	9.8	nM	CHEMBL_ACT_24961689
DRD2	7.99	IC50	10.28	nM	CHEMBL_ACT_6200322
CA5B	7.75	Ki	18	nM	CHEMBL_ACT_1655310
CA9	7.51	Ki	31	nM	CHEMBL_ACT_1760578
P61169	7.48	IC50	33	nM	CHEMBL_ACT_143926
P61169	7.44	IC50	36	nM	CHEMBL_ACT_143927
CA2	7.4	Ki	40	nM	CHEMBL_ACT_10946403
CA2	7.4	Ki	40	nM	CHEMBL_ACT_12655977
CA2	7.4	Ki	40	nM	CHEMBL_ACT_13286813
CA2	7.4	Ki	40	nM	CHEMBL_ACT_13407616
CA2	7.4	Ki	40	nM	CHEMBL_ACT_13440703
CA2	7.4	Ki	40	nM	CHEMBL_ACT_13866456
CA2	7.4	Ki	40	nM	CHEMBL_ACT_13910733
CA2	7.4	Ki	40	nM	CHEMBL_ACT_1437699
CA2	7.4	Ki	40	nM	CHEMBL_ACT_14661463
CA2	7.4	Ki	40	nM	CHEMBL_ACT_15108416

Target pathways

Aggregated over 5 target gene(s): DRD2, DRD3, CA1, CA12, CA7.

Top Reactome pathways

14 total, by targets touching each:

Pathway	Targets	Genes
Metabolism	3	CA1, CA12, CA7
Reversible hydration of carbon dioxide	3	CA1, CA12, CA7
Dopamine receptors	2	DRD2, DRD3
Erythrocytes take up carbon dioxide and release oxygen	1	CA1
Erythrocytes take up oxygen and release carbon dioxide	1	CA1
Cytokine Signaling in Immune system	1	CA1
O2/CO2 exchange in erythrocytes	1	CA1
Immune System	1	CA1
Transport of small molecules	1	CA1
G alpha (i) signalling events	1	DRD3
Interleukin-12 family signaling	1	CA1
Signaling by Interleukins	1	CA1
Gene and protein expression by JAK-STAT signaling after Interleukin-12 stimulation	1	CA1
Interleukin-12 signaling	1	CA1

Dominant GO biological processes

GO term	Targets
G protein-coupled receptor internalization	2
intracellular calcium ion homeostasis	2
adenylate cyclase-inhibiting dopamine receptor signaling pathway	2
locomotory behavior	2
visual learning	2
response to xenobiotic stimulus	2
regulation of dopamine secretion	2
positive regulation of cytokinesis	2
circadian regulation of gene expression	2
response to histamine	2
response to cocaine	2
dopamine metabolic process	2
regulation of potassium ion transport	2
response to morphine	2
negative regulation of blood pressure	2

Indications & clinical

Indications

5 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
psychotic disorder	4	MONDO:0005485	EFO:0005407
anxiety	3	MONDO:0011918	EFO:0005230
dementia	3	MONDO:0001627	HP:0000726
depressive disorder	3	MONDO:0002050	MONDO:0002050

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 12.

Phase distribution

Phase	Trials
Not specified	6
PHASE4	3
PHASE2/PHASE3	1
PHASE3	1
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00654576	PHASE4	COMPLETED	Effectiveness of Antipsychotic Combination With Psychosocial Intervention on Outcome of Patients With Schizophrenia
NCT02307396	PHASE4	COMPLETED	Evaluation of the Necessity of Long-term Pharmacological Treatment With Antipsychotics in Schizophrenic Patients
NCT04583111	PHASE4	UNKNOWN	The Effect of Antiemetics on Bowel Preparation Before Colonoscopy
NCT00866645	PHASE2/PHASE3	COMPLETED	A Study To Evaluate The Efficacy And Safety Of Intramuscular Levosulpiride In Patients With Agitation Of Schizophrenia
NCT02374567	PHASE3	TERMINATED	Pharmacovigilance in Gerontopsychiatric Patients
NCT02481583	PHASE1	COMPLETED	Pharmacokinetic Study of Levosulpiride
NCT00280501	Not specified	COMPLETED	Dopaminergic Modulation of Choroidal Blood Flow Changes During Dark/Light Transitions
NCT01777685	Not specified	COMPLETED	Therapeutic Drug Monitoring and Pharmacokinetic Compartmental Analysis of Sulpiride After Oral Administration to Healthy Volunteers
NCT01896349	Not specified	UNKNOWN	Interpersonal Psychotherapy for Treatment Resistant Depression
NCT04697641	Not specified	COMPLETED	Helicobacter Pylori Eradication in Functional Dyspepsia
NCT05208294	Not specified	COMPLETED	The Role of Dopamine, Reward Learning and Prefrontal Activity in Expectation-induced Mood Enhancement
NCT05884671	Not specified	COMPLETED	Dopamine and Cognition

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

595 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
DOBUTAMINE	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7, DRD2, DRD3
VERALIPRIDE	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7, DRD2, DRD3
THIMEROSAL	ChEMBL	Phase 3	CA12, CA7, DRD2, DRD3
SONEPIPRAZOLE	ChEMBL	Phase 2	CA1, CA12, CA7, DRD2
ACETAMINOPHEN	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
ACETAZOLAMIDE	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
BORTEZOMIB	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
BRINZOLAMIDE	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
CELECOXIB	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
CHLORTHALIDONE	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
COUMARIN	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
DICHLORPHENAMIDE	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
DORZOLAMIDE	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
ETHOXZOLAMIDE	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
FAMOTIDINE	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
FUROSEMIDE	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
IMATINIB	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
INDAPAMIDE	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
LACOSAMIDE	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
LEVETIRACETAM	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
MAFENIDE	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
METHAZOLAMIDE	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
NILOTINIB	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
SALICYLIC ACID	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
SULFANILAMIDE	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
TOPIRAMATE	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
TRICHLORMETHIAZIDE	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
TRIENTINE	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
VALDECOXIB	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
ZONISAMIDE	ChEMBL	Phase 4 (approved)	CA1, CA12, CA7
CAFFEIC ACID	ChEMBL	Phase 3	CA1, CA12, CA7
CURCUMIN	ChEMBL	Phase 3	CA1, CA12, CA7
P-TOLUENESULFONAMIDE	ChEMBL	Phase 3	CA1, CA12, CA7
QUERCETIN	ChEMBL	Phase 3	CA1, CA12, CA7
RESVERATROL	ChEMBL	Phase 3	CA1, CA12, CA7
SACCHARIN	ChEMBL	Phase 3	CA1, CA12, CA7
SPERMIDINE	ChEMBL	Phase 3	CA1, CA12, CA7
CARZENIDE	ChEMBL	Phase 2	CA1, CA12, CA7
COUMAPHOS	ChEMBL	Phase 2	CA1, CA12, CA7
ELLAGIC ACID	ChEMBL	Phase 2	CA1, CA12, CA7
GALLIC ACID	ChEMBL	Phase 2	CA1, CA12, CA7
INDISULAM	ChEMBL	Phase 2	CA1, CA12, CA7
IROSUSTAT	ChEMBL	Phase 2	CA1, CA12, CA7
PCI-27483	ChEMBL	Phase 2	CA1, CA12, CA7
DIHYDROERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	DRD2, DRD3
GENTIAN VIOLET	ChEMBL + PubChem	Phase 4 (approved)	DRD2, DRD3
PAZOPANIB	ChEMBL + PubChem	Phase 4 (approved)	CA1, CA12
ACETOPHENAZINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
AMIODARONE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
AMISULPRIDE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
AMLODIPINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
AMOXAPINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
APOMORPHINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
ARMODAFINIL	ChEMBL	Phase 4 (approved)	DRD2, DRD3
ASENAPINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
AZELASTINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
BAZEDOXIFENE	ChEMBL	Phase 4 (approved)	DRD2, DRD3