mozavaptan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| vasopressin receptor antagonists | 4004 | 137975-06-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
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Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 0.01 % | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| 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:
| Source | Code | Description |
|---|---|---|
| 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|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Paraneoplastic hyponatremia | indication | 405566004 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| 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