11C-MK-3168是一种有效的，选择性的，可透过血脑屏障的脂肪酸酰胺水解酶(FAAH)抑制剂，对人，大鼠和恒河猴FAAH的IC50值分别为1.0，1.7和5.5nM。
11C-MK-3168 is a potent, reversible and blood/brain barrier penetrated fatty acid amide hydrolase (FAAH) inhibitor, with IC50s of 1.0, 1.7 and 5.5 nM for human, rat and rhesus FAAH, respectively.
11C-MK-3168 is a potent and reversible fatty acid amide hydrolase (FAAH) inhibitor, with IC50s of 1.0, 1.7 and 5.5 nM for human, rat and rhesus FAAH, respectively. 11C-MK-3168 also shows selectivity over hERG (IC50 = 37 μM) and DLZ (IC50 = 16 μM); CYP 3A4 (IC50 > 50 μM); and the two cannabinoid receptors, CB1 (IC50 = 30 μM) and CB2 (IC50 = 150 μM)[1].
[1]. Liu P, et al. Discovery of MK-3168: A PET Tracer for Imaging Brain Fatty Acid Amide Hydrolase. ACS Med Chem Lett. 2013 Apr 20;4(6):509-13.
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