Tranylcypromine (2-PCPA) HCl4548-34-9
Tranylcypromine (2-PCPA) HCl
分子式:C9H11N.HCl 分子量:169.65
产品描述
Tranylcypromine (2-PCPA) HCl是一种非选择性的不可逆的单胺氧化酶(MAO)抑制剂,用作抗抑郁药和抗焦虑药。
靶点
CYP2A6
IC50
80 nM (Ki)
生物活性
R-(+)-Tranylcypromine, (±)-Tranylcypromine, and S-(−)-Tranylcypromine competitively inhibits CYP2A6-mediated metabolism of nicotine with apparent Ki values of 0.05 μM, 0.08 μM, and 2.0 μM, respectively, in human liver microsomes. Tranylcypromine (500 μg/mL) severely inhibits bradykinin-stimulated arachidonic acid release in calf aortic endothelial cells. Tranylcypromine inhibits CYP2A6 and CYP2E1 activity with IC50 of 0.42 μM and 3 μM, respectively, in human liver microsomes. Tranylcypromine induces type II and cyclopropylbenzene type I difference spectrum in human liver microsomes.
Tranylcypromine injection leads to a large, slow increase in motor activity at 5 mg/kg and 10 mg/kg compared with the saline control in male rats, although 2 mg/kg Tranylcypromine does not induce an increase. Tranylcypromine (10 mg/kg) also causes significant decreases in the number of rearing behaviors in male rats.
溶解性
DMSO 34 mg/mL,水 34 mg/mL,乙醇 34 mg/mL
稳定性
2年 -20°C粉状,6月-80°C溶于DMSO