Tranylcypromine (2-PCPA) HCl4548-34-9

Tranylcypromine (2-PCPA) HCl
分子式：C9H11N.HCl   分子量：169.65
 
產品描述
Tranylcypromine (2-PCPA) HCl是一種非選擇性的不可逆的單胺氧化酶(MAO)抑制劑，用作抗抑郁藥和抗焦慮藥。
靶點
 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
穩(wěn)定性
2年 -20°C粉狀，6月-80°C溶于DMSO