Home Neuronal Signaling Histamine Receptor inhibitor Azatadine dimaleate For research use only.

Azatadine dimaleate

Synonyms: SCH10649,Azatadine Maleate

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

Azatadine dimaleate Chemical Structure

Azatadine dimaleate Chemical Structure

CAS: 3978-86-7

Selleck's Azatadine dimaleate has been cited by 1 publication

Purity & Quality Control

Batch: Purity: 99.93%
99.93

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Biological Activity

Description Azatadine (SCH10649,Azatadine Maleate) is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.
Targets
Histamine receptor [1] Cholinergic [1]
6.5 nM 10 nM
In vitro
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. [2]
In Vivo
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. [1] Following a single oral dose of Azatadine (4 mg) in fasted volunteers, a Cmax 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%. [3] Azatadine (1 mg twice daily for 14 days) is effective in relieving the histamine-mediated symptoms of seasonal allergic rhinitis. [4]

Chemical lnformation & Solubility

Molecular Weight 522.55 Formula

C20H22N2.2C4H4O4
CAS No. 3978-86-7 SDF Download Azatadine dimaleate SDF
Smiles CN1CCC(=C2C3=CC=CC=C3CCC4=C2N=CC=C4)CC1.C(=CC(=O)O)C(=O)O.C(=CC(=O)O)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 105 mg/mL ( (200.93 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 105 mg/mL

Ethanol : Insoluble


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