Asenapine hydrochloride
Names
[ CAS No. ]:
1412458-61-7
[ Name ]:
Asenapine hydrochloride
[Synonym ]:
cs-1053
Asenapine (hydrochloride)
Biological Activity
[Description]:
Asenapine maleate, an antipsychotic, is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and Dopamine (D2, D3, D4) receptor antagonist with Ki values of 0.03-4.0 nM for 5-HT and 1.3, 0.42, 1.1 nM for Dopamine receptor, respectively.
[Related Catalog]:
[Target]
5-HT1A Receptor:2.5 nM (Ki)
5-HT2A Receptor:0.06 nM (Ki)
5-HT2C Receptor:0.03 nM (Ki)
5-HT7 Receptor:0.13 nM (Ki)
D2 Receptor:1.3 nM (Ki)
D3 Receptor:0.42 nM (Ki)
D4 Receptor:1.1 nM (Ki)
[In Vitro]
Relative to its D2 receptor affinity, Asenapine has a higher affinity for 5-HT2C, 5-HT2A, 5-HT2B, 5-HT7, 5-HT6, α2B and D3 receptors, suggesting stronger engagement of these targets at therapeutic doses. Asenapine behaves as a potent antagonist (pKB) at 5-HT1A (7.4), 5-HT1B (8.1), 5-HT2A (9.0), 5-HT2B (9.3), 5-HT2C (9.0), 5-HT6 (8.0), 5-HT7 (8.5), D2 (9.1), D3 (9.1), α2A (7.3), α2B (8.3), α2C (6.8) and H1 (8.4) receptors[2].
[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[3]. Asenapine has anxiolytic-like effects in the EPM and the defensive marble burying tests in mice[4].
[References]
[Related Small Molecules]
Chemical & Physical Properties
[ Molecular Formula ]:
C17H17Cl2NO
[ Molecular Weight ]:
322.22900
[ Exact Mass ]:
321.06900
[ PSA ]:
12.47000
[ LogP ]:
4.99840
[ Storage condition ]:
2-8℃