Asenapine hydrochloride

Asenapine hydrochloride, an antipsychotic, is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and Dopamine (D 2 , D 3 , D 4 ) 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-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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Asenapine has anxiolytic-like effects in the EPM and the defensive marble burying tests in mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target: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)

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