Azatadine dimaleate - 10mM in DMSO , Histamine H1 receptor antagonist, CAS No.3978-86-7, Histamine H1 receptor antagonist

CAS: 3978-86-7 Cat. No.: A409069 Molecular Weight: 522.55 EC Number: 223-615-8 PubChem CID: 5281066

GRADE & PURITY 10mM in DMSO

Synonyms

SCH10649 | 5H-Benzo[5,6]cyclohepta[1,2-b]pyridine, 6,11-dihydro-11-(1-methyl-4-piperidinylidene)-, (2Z)-2-butenedioate (1:2)

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Azatadine dimaleate Azatadine (SCH10649) is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.
In vitro

95% of Azatadine is biotransformed in Sabouraud dextrose broth within 72 hours treatment with two major metabolites, 7-hydroxyazatadine (25%) and 8-hydroxyazatadine (50%), and two minor metabolites, N-desmethylazatadine and 9-hydroxyazatadine.

In vivo

Azatadine delays the onset of dyspnea-induced by aerosolized histamine, acetylcholine and serotonin in the conscious guinea-pig with PD50 of 0.01 mg/kg, 0.739 mg/kg and 0.86 mg/kg. Azatadine protects conscious guinea-pigs against death induced by the intravenous injection of histamine with oral PD50 of 0.009 mg/kg in guinea-pig and 0.22 mg/kg in mice. Following a single oral dose of Azatadine (4 mg) in fasted volunteers, a C_max of 3 μg/L has been measured by RIA 4.2 hours after administration. Azatadine is almost completely metabolised by hydroxylation, demethylation and formation of zwitterion isomers by oxidative ring opening. Azatadine (8.8 mg oral) in healthy volunteers results in a Csub>max of 5.9 μg/L at 5.3 hours after treatment and bioavailability of 80%. Azatadine (1 mg twice daily for 14 days) is effective in relieving the histamine-mediated symptoms of seasonal allergic rhinitis.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥98%

Specifications

Synonyms

SCH10649 | 5H-Benzo[5, 6]cyclohepta[1, 2-b]pyridine, 6, 11-dihydro-11-(1-methyl-4-piperidinylidene)-, (2Z)-2-butenedioate (1:2)

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

Azatadine (SCH10649) is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

ANTAGONIST

Mechanism of action

Histamine H1 receptor antagonist

Names and Identifiers

• Isomeric SMILES: CN1CCC(=C2C3=C(C=CC=N3)CCC4=CC=CC=C24)CC1.C(=C\C(=O)O)\C(=O)O.C(=C\C(=O)O)\C(=O)O
• PubChem CID: 5281066
• Molecular Weight: 522.55