MOZAVAPTAN HYDROCHLORIDE

Details

Stereochemistry	RACEMIC
Molecular Formula	C27H29N3O2.ClH
Molecular Weight	463.999
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

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

InChI

InChIKey=MOROBKPIULFQDC-UHFFFAOYSA-N

InChI=1S/C27H29N3O2.ClH/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);1H

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
The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.	1997 Oct	9322919
Binding properties of a selective tritiated vasopressin V2 receptor antagonist, [H]-SR 121463.	2000 Oct	11012895
Ameliorative effect of NC-1900, a new AVP4-9 analog, through vasopressin V1A receptor on scopolamine-induced impairments of spatial memory in the eight-arm radial maze.	2003 Mar	12646291
[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 HYDROCHLORIDE

Common Name

English

Mozavaptan hydrochloride [WHO-DD]

Common Name

English

MOZAVAPTANE HYDROCHLORIDE

Common Name

English

MOZAVAPTANE HYDROCHLORIDE [JAN]

Common Name

English

BENZAMIDE, N-(4-((5-(DIMETHYLAMINO)-2,3,4,5-TETRAHYDRO-1H-1-BENZAZEPIN-1-YL)CARBONYL)PHENYL)-2-METHYL-, HYDROCHLORIDE (1:1)

Systematic Name

English

BENZAMIDE, N-(4-((5-(DIMETHYLAMINO)-2,3,4,5-TETRAHYDRO-1H-1-BENZAZEPIN-1-YL)CARBONYL)PHENYL)-2-METHYL-, MONOHYDROCHLORIDE, (±)-

Common Name

English

MOZAVAPTAN HYDROCHLORIDE [MI]

Common Name

English

N-(4-(((5RS)-5-(DIMETHYLAMINO)-2,3,4,5-TETRAHYDRO-1H-BENZO(B)AZEPIN-1-YL)CARBONYL(PHENYL)-2-METHYLBENZAMIDE MONOHYDROCHLORIDE

Common Name

English

PHYSULINE

Brand Name

English

Classification Tree Code System Code

NCI_THESAURUS

C2180