mozavaptan 🐶 Veterinary Use | 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:

PropertyValueReference
BA (Bioavailability) 0.01 % Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Approvals:

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

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
MeSH PA D065092 Antidiuretic Hormone Receptor Antagonists
MeSH PA D045283 Natriuretic Agents
CHEBI has role CHEBI:194423 aquaretic agent

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Paraneoplastic hyponatremia indication 405566004




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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
Vasopressin V1b receptor GPCR ANTAGONIST Ki 4.80 IUPHAR
Oxytocin receptor GPCR Ki 6.18 CHEMBL
Vasopressin V1a receptor GPCR Ki 6.71 CHEMBL
Vasopressin V1a receptor GPCR IC50 5.85 CHEMBL
Vasopressin V1 receptor GPCR IC50 5.30 CHEMBL
Vasopressin V2 receptor GPCR IC50 7.92 CHEMBL

External reference:

IDSource
D01855 KEGG_DRUG
C2975283 UMLSCUI
CHEBI:135694 CHEBI
CHEMBL420762 ChEMBL_ID
C076251 MESH_SUPPLEMENTAL_RECORD_UI
119369 PUBCHEM_CID
2197 IUPHAR_LIGAND_ID
8248 INN_ID
138470-70-9 SECONDARY_CAS_RN
17OJ42922Y UNII
CHEMBL106229 ChEMBL_ID

Pharmaceutical products:

None