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名称

Asenapine hydrochloride

别名

盐酸阿塞那平

英文名称

Asenapine hydrochloride

货号

A656371-1ml

包装规格

1ml

浓度

10mM in DMSO

储存温度

干燥,-80℃储存

运输条件

超低温冰袋运输

产品介绍

Asenapine hydrochloride, an antipsychotic, is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and Dopamine (D 2 , D 3 , D 4 ) receptor antagonist with K i values of 0.03-4.0 nM for 5-HT and 1.3, 0.42, 1.1 nM for Dopamine receptor , respectively. In Vitro Relative to its D2 receptor affinity, Asenapine has a higher affinity for 5-HT 2C , 5-HT 2A , 5-HT 2B , 5-HT 7 , 5-HT 6 , 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-HT 6 (8.0), 5-HT 7 (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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:sPLA2 2.5 nM (Ki) 5-HT 2A Receptor 0.06 nM (Ki) 5-HT 2C Receptor 0.03 nM (Ki) 5-HT 7 Receptor 0.13 nM (Ki) D 2 Receptor 1.3 nM (Ki) D 3 Receptor 0.42 nM (Ki) D 4 Receptor 1.1 nM (Ki)

生化机理

盐酸阿塞那平是一种抗精神病药，是 5-羟色胺（1A、1B、2A、2B、2C、5A、6、7）和多巴胺（D 2、D 3、D 4）受体拮抗剂，5-羟色胺受体的 K i 值分别为 0.03-4.0 nM，多巴胺受体的 K i 值分别为 1.3、0.42、1.1 nM。

CAS号

1412458-61-7(DMSO)

分子式

C17H17Cl2NO

分子量

322.23 g/mol

Smiles

[H]Cl.ClC1=CC2=C(C=C1)OC3=C(C=CC=C3)[C@](C4)([H])[C@]2([H])CN4C

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

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「No related articles yet」

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