mosapride indications/contra

Stem definitionDrug idCAS RN
sulpiride derivatives 1848 112885-41-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • gasmotin
  • AS 4370
  • mosapride citrate hydrate
  • mosapride
  • mosapride citrate
  • mosapride citrate dihydrate
  • AS-4370
Mosapride is a 5-HT4 receptor agonist which increases the release of acetylcholine and stimulates GI motility.
  • Molecular weight: 421.90
  • Formula: C21H25ClFN3O3
  • CLOGP: 3.44
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 2
  • TPSA: 76.82
  • ALOGS: -4.29
  • ROTB: 7

Drug dosage:

None

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1998 YEAR INTRODUCED

FDA Adverse Event Reporting System

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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
Hepatic function abnormal 100.43 46.60 21 121 11206 3374511

Pharmacologic Action:

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SourceCodeDescription
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018490 Serotonin Agents
MeSH PA D017366 Serotonin Receptor Agonists

Drug Use (View source of the data)

None

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 5.95 Basic
pKa2 1.11 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
5-hydroxytryptamine receptor 4 GPCR AGONIST Ki 6.90 IUPHAR SCIENTIFIC LITERATURE
Alpha-2A adrenergic receptor GPCR Ki 5.86 DRUG MATRIX
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 6.89 DRUG MATRIX
Cytochrome P450 3A4 Enzyme IC50 6.15 DRUG MATRIX
Sodium-dependent serotonin transporter Transporter Ki 5.69 DRUG MATRIX
5-hydroxytryptamine receptor 2B GPCR Ki 6.73 DRUG MATRIX
5-hydroxytryptamine receptor 2C GPCR Ki 6.68 DRUG MATRIX
Alpha-2B adrenergic receptor GPCR Ki 6.06 DRUG MATRIX
Cytochrome P450 2C9 Enzyme IC50 6 DRUG MATRIX
Cytochrome P450 1A2 Enzyme IC50 6.40 DRUG MATRIX
Cytochrome P450 2C19 Enzyme IC50 6 DRUG MATRIX
5-hydroxytryptamine receptor 3A Ion channel Ki 5.70 WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.32 CHEMBL
5-hydroxytryptamine receptor 4 GPCR Ki 7.16 CHEMBL
Serotonin 3 (5-HT3) receptor Ion channel Ki 5.92 CHEMBL

External reference:

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IDSource
242 IUPHAR_LIGAND_ID
C0526501 UMLSCUI
D01994 KEGG_DRUG
73033I28Y6 UNII
636582-62-2 SECONDARY_CAS_RN
CHEMBL60889 ChEMBL_ID
008862 NDDF
135091 RXNORM
119584 PUBCHEM_CID
C062720 MESH_SUPPLEMENTAL_RECORD_UI
6855 INN_ID
DB11675 DRUGBANK_ID
CHEBI:31867 CHEBI

Pharmaceutical products:

None