tcsc1053 Asenapine (hydrochloride)

Asenapine maleate, an antipsychotic, is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and Dopamine (D₂, D₃, D₄) 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-HT₇, 5-HT₆, 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-HT₆ (8.0), 5-HT₇ (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^[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].