Asenapine hydrochloride,1412458-61-7

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YZ剂描述：

产品名称：Asenapine hydrochloride

产品别名：Saphris hydrochloride

英文别名：Saphris hydrochloride

靶点：5-HT Receptor

CAS：1412458-61-7

纯度：>98%

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Asenapine hydrochloride inhibits adrenergic receptor (??1, ??2A, ??2B, ??2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, , 6, 7) with Ki of 0.03-4.0 nM.

溶解性：10 mM in DMSO

体外研究：

Relative to its D2 receptor affinity, Asenapine has a higher affinity for 5-HT_2C, 5-HT_2A, 5-HT_2B, 5-HT₇, 5-HT₆, α_2B and D3 receptors, suggesting stronger engagement of these targets at therapeutic doses. Asenapine behaves as a potent antagonist (pK_B) at 5-HT_1A (7.4), 5-HT1B (8.1), 5-HT_2A (9.0), 5-HT_2B (9.3), 5-HT_2C (9.0), 5-HT₆ (8.0), 5-HT₇ (8.5), D2 (9.1), D3 (9.1), α_2A (7.3), α_2B (8.3), α_2C (6.8) and H1 (8.4) receptors.

体内研究：

Asenapine is an atypical antipsychotic that is currently available for the treatment of schizophrenia and bipolar I disorder. Asenapine may have superior therapeutic effect on anxiety symptoms than other agents in rats. Asenapine has anxiolytic-like effects in the EPM and the defensive marble burying tests in mice.

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