1412458-61-7
1412458-61-7 結(jié)構(gòu)式
基本信息
Saphris hydrochloride
Asenapine (hydrochloride)
(3AS,12BS)-5-CHLORO-2-METHYL-2,3,3A,12B-TETRAHYDRO-1H-DIBENZO[2,3:6,7]OXEPINO[4,5-C]PYRROLE HYDROCHLORIDE
(3aS,12bS)-5-Chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole hydrochloride (1:1)
物理化學(xué)性質(zhì)
常見(jiàn)問(wèn)題列表
|
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.