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是组胺受体和胆碱受体抑制剂。
| 基本信息 | |
| CAS | No.3978-86-7 |
| 中文名称 | 马来酸阿扎他定 |
| 英文名称 | Azatadine dimaleate |
| 别名 | Azatadine Maleate;SCH10649 |
| 分子式 | C20H22N2·2C4H4O4 |
| 分子量 | 522.55 |
| 溶解性 | Soluble in Water/DMSO |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 货期 | 1-2个工作日 |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| EC | EINECS 223-615-8 |
| MDL | MFCD00242593 |
| SMILES | O=C(O)/C=CC(O)=O.O=C(O)/C=CC(O)=O.CN1CC/C(CC1)=C2C3=CC=CC=C3CCC4=CC=CN=C42 |
| InChIKey | SGHXFFAHXTZRQM-SPIKMXEPSA-N |
| InChI | 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- |
| PubChem CID | 5281066 |
| 靶点 | Histamine Receptor |
| 通路 | GPCR & G Protein;Neuronal Signaling;Immunology & Inflammation |
| 背景说明 | 是组胺受体和胆碱受体抑制剂。 |
| 生物活性 | Azatadine (SCH10649) 是一种抗组胺和抗胆碱能药物，IC50分别为6.5nM和10nM。[1] |
| IC50 | Histamine receptor: 6.5nM;Cholinergic :10nM[1] |
| 细胞实验 | 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%. [2] Azatadine(1 mg twice daily for 14 days)is effective in relieving the histamine-mediated symptoms of seasonal allergic rhinitis. [3] |
| 数据来源文献 | [1] Tozzi S， et al. Agents Actions， 1974， 4(4)， 264-270. [2] Simons FE， et al. Clin Pharmacokinet， 1991， 21(5)， 372-393. [3] Katelaris C， et al. Asian Pac J Allergy Immunol， 1990， 8(2)， 103-107 |
| 单位 | 支 |