mozavaptan Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
vasopressin receptor antagonists 4004 137975-06-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • mozavaptan
  • mozavaptan hydrochloride
  • physulime
  • OPC-31260
  • mozavaptan HCl
Mozavaptan is a benzazepine derivative that antagonizes the binding of arginine vasopressin (AVP) to vasopressin receptors. Mozavaptan can inhibit the antidiuretic action of AVP promoting aquaresis.
  • Molecular weight: 427.55
  • Formula: C27H29N3O2
  • CLOGP: 3.97
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 52.65
  • ALOGS: -5.25
  • ROTB: 4

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
July 26, 2006 PMDA Otsuka Pharmaceutical Co., Ltd.

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
MeSH PA D065092 Antidiuretic Hormone Receptor Antagonists
MeSH PA D045283 Natriuretic Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Paraneoplastic hyponatremia indication 405566004

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.2 acidic
pKa2 7.61 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
Vasopressin V2 receptor GPCR ANTAGONIST Ki 8.03 CHEMBL SCIENTIFIC LITERATURE
Oxytocin receptor GPCR Ki 6.18 CHEMBL
Vasopressin V1b receptor GPCR ANTAGONIST Ki 4.80 IUPHAR
Vasopressin V1a receptor GPCR Ki 6.71 CHEMBL
Vasopressin V2 receptor GPCR IC50 7.92 CHEMBL
Vasopressin V1a receptor GPCR IC50 5.85 CHEMBL
Vasopressin V1 receptor GPCR IC50 5.30 CHEMBL

External reference:

IDSource
D01855 KEGG_DRUG
17OJ42922Y UNII
8248 INN_ID
CHEMBL420762 ChEMBL_ID
CHEMBL106229 ChEMBL_ID
138470-70-9 SECONDARY_CAS_RN
CHEBI:135694 CHEBI
119369 PUBCHEM_CID
2197 IUPHAR_LIGAND_ID
C076251 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

None