Asenapine (maleate)

Asenapine (Org 5222) maleate, a brain-penetrant atypical antipsychotic, is an antagonist of serotonin receptors (pK_i: 8.4-10.5), adrenoceptors (pK_i: 8.9-9.5), dopamine receptors (pK_i: 8.9-9.4) and histamine receptors (pK_i: 8.2-9.0). Asenapine maleate can be used in the research of schizophrenia and bipolar disorder^{[1][2][3][4][5]}. IC50 & Target:Ki: 0.03-4.0 nM (5-HT), 1.3 nM (D2)^[1]. 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-HT1A (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 maleate 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 maleate has anxiolytic-like effects in the EPM and the defensive marble burying tests in mice^[3][4].