阿塞那平盐酸盐性质、用途与生产工艺
Asenapine hydrochloride，一种抗精神病药物，同时是 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) 和 Dopamine (D2，D3，D4) 受体的拮抗剂，对 5-HT 受体的 Ki 值分别为 0.03-4.0 nM，多巴胺受体的 Ki 值分别为 1.3，0.42，1.1 nM。
|
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)
|
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.
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.
阿塞那平盐酸盐
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