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Azatadine dimaleate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Azatadine dimaleate图片
CAS NO:3978-86-7
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)522.55
FormulaC20H22N2.2C4H4O4
CAS No.3978-86-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 105 mg/mL (200.9 mM)
Water: 105 mg/mL (200.9 mM)
Ethanol: <1 mg/mL
Other info

Chemical Name: 6,11-Dihydro-11-(1-methylpiperidin-4-ylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine dimaleate

InChi Key: SGHXFFAHXTZRQM-SPIKMXEPSA-N

InChi Code: InChI=1S/C20H22N2.2C4H4O4/c1-22-13-10-16(11-14-22)19-18-7-3-2-5-15(18)8-9-17-6-4-12-21-20(17)19;2*5-3(6)1-2-4(7)8/h2-7,12H,8-11,13-14H2,1H3;2*1-2H,(H,5,6)(H,7,8)/b;2*2-1-

SMILES Code: CN1CC/C(CC1)=C2C3=CC=CC=C3CCC4=CC=CN=C4\2.O=C(O)/C=C\C(O)=O.O=C(O)/C=C\C(O)=O

SynonymsSCH 10649; azatadine maleate; SCH10649; SCH-10649; Idulamine; Idulian; Lergocil; Optimine; Zadine
实验参考方法
In Vitro

In vitro activity: 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 VivoAzatadine 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 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%. Azatadine (1 mg twice daily for 14 days) is effective in relieving the histamine-mediated symptoms of seasonal allergic rhinitis.
Animal modelguinea-pig
Formulation & Dosage0.01 mg/kg, 0.739 mg/kg and 0.86 mg/kg
References

Agents Actions. 1974 Oct;4(4):264-70; Clin Pharmacokinet. 1991 Nov;21(5):372-93.