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名称

Asenapine hydrochloride

分子类型

小分子

别名

盐酸阿塞那平

英文名称

Asenapine hydrochloride

货号

A650677-50mg

包装规格

50mg

浓度

≥98%

储存温度

2-8°C储存,干燥

运输条件

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. Form:Solid 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

分子式

C17H17Cl2NO

分子量

322.23 g/mol

PubChem编号

163091

Isomeric SMILES

CN1C[C@H]2[C@H](C1)C3=C(C=CC(=C3)Cl)OC4=CC=CC=C24

Smiles

CN1C[C@H]2[C@H](C1)C3=C(C=CC(=C3)Cl)OC4=CC=CC=C24

PubChem CID

163091

溶解性

H2O : 100 mg/mL (310.34 mM; Need ultrasonic) DMSO : 50 mg/mL (155.17 mM; Need ultrasonic)

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

285.092 Da

单同位素质量Monoisotopic Mass

285.092 Da

拓扑极表面积Topological Polar Surface Area

12.500 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

363.000

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

3.800

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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