MOZAVAPTAN

Details

Stereochemistry	RACEMIC
Molecular Formula	C27H29N3O2
Molecular Weight	427.5381
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CN(C)C1CCCN(C(=O)C2=CC=C(NC(=O)C3=CC=CC=C3C)C=C2)C4=C1C=CC=C4

InChI

InChIKey=WRNXUQJJCIZICJ-UHFFFAOYSA-N

InChI=1S/C27H29N3O2/c1-19-9-4-5-10-22(19)26(31)28-21-16-14-20(15-17-21)27(32)30-18-8-13-24(29(2)3)23-11-6-7-12-25(23)30/h4-7,9-12,14-17,24H,8,13,18H2,1-3H3,(H,28,31)

HIDE SMILES / InChI

Description
Sources: http://www.pharmacodia.com/yaodu/html/v1/chemicals/818f4654ed39a1c147d1e51a00ffb4cb.html
Curator's Comment: Description was created based on several sources, including http://adisinsight.springer.com/drugs/800001739 http://www.rad-ar.or.jp/siori/english/kekka.cgi?n=33180

Mozavaptan hydrochloride was approved by Pharmaceuticals and Medical Devices Agency of Japan (PMDA) on July 26, 2006. It was developed and marketed as Physuline® by Otsuka in Japan. Mozavaptan hydrochloride is a vasopressin receptor antagonist. It is indicated for the treatment of hyponatremia due to excessive fluid retention when restriction of fluid intake is ineffective. Physuline® is available as film-coated tablet for oral use, containing 30 mg of Mozavaptan hydrochloride. The recommended dose is one tablet (30 mg) once daily after a meal.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Vasopressin V1 receptor 2 Target ID: CHEMBL2111456 Sources: http://www.selleckchem.com/products/mozavaptan.html	Antagonist 2778		1.2 µM [IC50]
Vasopressin V2 receptor 15 Target ID: CHEMBL1790 Sources: http://adisinsight.springer.com/drugs/800001739	Antagonist 2778		14.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hyponatremia 4 Sources: http://adisinsight.springer.com/drugs/800001739	Primary		Approved 8429	PHYSULINE Approved Use PHYSULINE is used for the treatment of hyponatremia due to excessive fluid retention when restriction of fluid intake is ineffective. Launch Date 2006

PubMed

Title	Date	PubMed
Gateways to clinical trials.	2003 Jun	12851663
Prevention of hypoxic brain oedema by the administration of vasopressin receptor antagonist OPC-31260.	2008	18655905
[Vasopressin receptor antagonists: the vaptans].	2010 May	21130961

Patents

Sample Use Guides

In Vivo Use Guide

The recommended dose is one tablet (30 mg) once daily after a meal.

Route of Administration: Oral

In Vitro Use Guide

Mozavaptan caused a concentration-dependent displacement of the selective AVP V2 receptor antagonist radioligand, [3H]desGly-NH2(9)[d(CH2)5, D-Ile2,Ile4]AVP from V2 receptors in rat kidney medulla membranes. The concentration of Mozavaptan that displaced 50% of specific AVP binding (IC50) was 20 +/- 2 nmol/l for renal V2 receptors.

Name

Type

Language

MOZAVAPTAN

Official Name

English

mozavaptan [INN]

Common Name

English

N-(4-(((5RS)-5-(DIMETHYLAMINO)-2,3,4,5-TETRAHYDRO-1H-1-BENZAZEPIN-1-YL)CARBONYL)PHENYL)-2-METHYLBENZAMIDE

Systematic Name

English

Mozavaptan [WHO-DD]

Common Name

English

MOZAVAPTAN [MI]

Common Name

English

MOZAVAPTAN [MART.]

Common Name

English

MOZAVAPTANE

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C2180