85650-56-2马来酸阿森那平

马来酸阿森那平
分子式：C17H16ClNO.C4H4O4
分子量：401.84
产品描述
Asenapine 是adrenergic receptor (α1, α2A, α2B, α2C) 拮抗剂，Ki为0.25-1.2 nM，也是5-HT receptor拮抗剂，(1A, 1B, 2A, 2B, 2C, 5A, 6, 7) Ki为0.03-4.0 nM。

靶点

IC50
生物活性
Asenapine is a new atypical antipsychotic developed for the treatment of schizophrenia and acute mania associated with bipolar disorder.Asenapine shows high affinity (pKi) for numerous receptors, including the serotonin 5-HT1A (8.6), 5-HT1B (8.4), 5-HT2A (10.2), 5-HT2B (9.8), 5-HT2C (10.5), 5-HT5A (8.8), 5-HT6 (9.5), and 5-HT7 (9.9) receptors, the adrenergic α1 (8.9), α2A (8.9), α2B (9.5), and α2C (8.9) receptors, the dopamine D1 (8.9), D2 (8.9), D3 (9.4), and D4 (9.0) receptors, and the histamine H1 (9.0) and H2 (8.2) receptors. Asenapine behaves as an antagonist at all receptors.溶解性DMSO 80 mg/mL，水 <1 mg/mL，乙醇<1 mg/mL
稳定性
2年 -20°C粉状，6月-80°C溶于DMSO