sulpiride Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
sulpiride derivatives 2537 15676-16-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • sulpiride
  • sulpirid
  • sulpitil
  • sulpyrid
  • sursumid
A dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid. (From Merck Index, 11th ed)
  • Molecular weight: 341.43
  • Formula: C15H23N3O4S
  • CLOGP: 1.11
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 2
  • TPSA: 101.73
  • ALOGS: -2.80
  • ROTB: 6

Drug dosage:

DoseUnitRoute
0.80 g O
0.80 g P

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1972 YEAR INTRODUCED

FDA Adverse Event Reporting System

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Torsade de pointes 180.52 56.86 31 238 2998 3382592
Electrocardiogram QT prolonged 158.21 56.86 34 235 10761 3374829
Ventricular fibrillation 143.63 56.86 27 242 4306 3381284
Hypomagnesaemia 115.78 56.86 22 247 3680 3381910
Neuroleptic malignant syndrome 111.78 56.86 22 247 4419 3381171
Parkinsonism 92.43 56.86 17 252 2361 3383229
Overdose 71.45 56.86 23 246 33955 3351635
Hypokalaemia 67.40 56.86 18 251 13787 3371803

Pharmacologic Action:

SourceCodeDescription
ATC N05AL01 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Benzamides
CHEBI has role CHEBI:35469 antidepressant
CHEBI has role CHEBI:50919 antiemetic
CHEBI has role CHEBI:35476 antipsychotic agent
CHEBI has role CHEBI:48561 dopaminergic antagonist
MeSH PA D000928 Antidepressive Agents
MeSH PA D018687 Antidepressive Agents, Second-Generation
MeSH PA D014150 Antipsychotic Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D015259 Dopamine Agents
MeSH PA D018492 Dopamine Antagonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014149 Tranquilizing Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Schizophrenia indication 58214004

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.47 acidic
pKa2 12.66 acidic
pKa3 8.85 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
D(2) dopamine receptor GPCR ANTAGONIST Ki 8.12 CHEMBL IUPHAR
Carbonic anhydrase 2 Enzyme IC50 7.40 WOMBAT-PK
Carbonic anhydrase 5A, mitochondrial Enzyme Ki 6.76 CHEMBL
Carbonic anhydrase 12 Enzyme Ki 8.41 CHEMBL
D(4) dopamine receptor GPCR Ki 5.68 CHEMBL
D(3) dopamine receptor GPCR Ki 8.10 CHEMBL
Carbonic anhydrase 3 Enzyme Ki 4.97 CHEMBL
Carbonic anhydrase 7 Enzyme Ki 8.44 CHEMBL
Carbonic anhydrase 9 Enzyme Ki 7.51 CHEMBL
Carbonic anhydrase 1 Enzyme Ki 5.92 CHEMBL
Carbonic anhydrase 5B, mitochondrial Enzyme Ki 7.74 CHEMBL
Carbonic anhydrase 6 Enzyme Ki 9.10 CHEMBL
Alpha-2A adrenergic receptor GPCR Ki 6.12 DRUG MATRIX
Dopamine receptor GPCR Ki 5.80 CHEMBL
Alpha carbonic anhydrase Unclassified Ki 6.37 CHEMBL
Astrosclerin-3 Unclassified Ki 6.42 CHEMBL
Beta-carbonic anhydrase 1 Enzyme Ki 5.64 CHEMBL
Carbonic anhydrase Unclassified Ki 6.38 CHEMBL
Delta carbonic anhydrase Unclassified Ki 6.59 CHEMBL
Carbonic anhydrase Enzyme Ki 6.91 CHEMBL
D(2) dopamine receptor GPCR IC50 6.70 CHEMBL
D(2) dopamine receptor GPCR Kd 8.82 CHEMBL
Carbonic anhydrase Enzyme Ki 6.75 CHEMBL
Carbonic anhydrase 15 Enzyme Ki 7.14 CHEMBL
Carbonic anhydrase Enzyme Ki 7.40 CHEMBL
Carbonic anhydrase 2 Enzyme Ki 6.58 CHEMBL
Carbonic anhydrase Unclassified Ki 7.53 CHEMBL
Carbonic anhydrase Enzyme Ki 6.95 CHEMBL

External reference:

IDSource
DB00391 DRUGBANK_ID
N0000166882 NUI
C0038803 UMLSCUI
5501 IUPHAR_LIGAND_ID
D01226 KEGG_DRUG
CHEMBL26 ChEMBL_ID
7MNE9M8287 UNII
2359 INN_ID
N0000166882 NDFRT
10239 RXNORM
321506004 SNOMEDCT_US
395891007 SNOMEDCT_US
003764 NDDF
5355 PUBCHEM_CID
D013469 MESH_DESCRIPTOR_UI
CHEBI:32168 CHEBI

Pharmaceutical products:

None