ACITAZANOLAST MONOHYDRATE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C9H7N5O3.H2O
Molecular Weight	251.1989
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O.OC(=O)C(=O)NC1=CC=CC(=C1)C2=NN=NN2

InChI

InChIKey=LEZMUVNSMYOTNL-UHFFFAOYSA-N

InChI=1S/C9H7N5O3.H2O/c15-8(9(16)17)10-6-3-1-2-5(4-6)7-11-13-14-12-7;/h1-4H,(H,10,15)(H,16,17)(H,11,12,13,14);1H2

HIDE SMILES / InChI

Description
Sources: http://www.dcchemicals.com/products_Show.asp?id=4171http://meds.qlifepro.com/detail/620006023/tazanolast
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/9150859

Tazanolast, an anti-allergic and anti-asthmatic agent with selective mast-cell stabilising effects, was developed jointly by Wakamoto and Torii Pharmaceuticals.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
histamine secretion by mast cell 3 Target ID: GO:0002553 Sources: http://www.ncbi.nlm.nih.gov/pubmed/9150859	Inhibitor 8504

Conditions

Condition	Modality	Targets	Highest Phase	Product
Asthma 244 Sources: http://meds.qlifepro.com/detail/620006023/tazanolast	Palliative		Approved 8583	Unknown Approved Use Unknown
Unknown 2596

C_max

Value	Dose	Co-administered	Analyte	Population
1.18 μg/mL EXPERIMENT https://en.cnki.com.cn/Article_en/CJFDTotal-LCZZ200103013.htm	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:		ACITAZANOLAST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
2.18 μg × h/mL EXPERIMENT https://en.cnki.com.cn/Article_en/CJFDTotal-LCZZ200103013.htm	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:		ACITAZANOLAST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
2.48 h EXPERIMENT https://en.cnki.com.cn/Article_en/CJFDTotal-LCZZ200103013.htm	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:		ACITAZANOLAST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
4% OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/890016_1319745Q1024_2_009_1F.pdf#page=26			ACITAZANOLAST plasma	Homo sapiens

PubMed

Title	Date	PubMed
Effect of an active metabolite of the antiallergic agent tazanolast on histamine release from rat mast cells.	1997-04	9150859
[Effect of tazanolast on platelet activating factor-induced airway hyperresponsiveness in guinea pigs].	1992-09	1280089

Patents

Sample Use Guides

In Vivo Use Guide

0.01 and 0.033% aerosol inhalation.

Route of Administration: Respiratory

In Vitro Use Guide

WP-871 (Acitazanolast) may inhibit histamine release mainly by preventing the increase in intracellular Ca2+ concentration

Name

Type

Language

ACITAZANOLAST MONOHYDRATE

Common Name

English

ZEPELIN

Preferred Name

English

ACITAZANOLAST HYDRATE

Common Name

English

ACETIC ACID, 2-OXO-2-((3-(2H-TETRAZOL-5-YL)PHENYL)AMINO)-, HYDRATE (1:1)

Common Name

English

Acitazanolast monohydrate [WHO-DD]

Common Name

English

Code System Code Type Description

PUBCHEM

11954321