565460-15-3
基本信息
[1,1'-聯(lián)苯]-3-基氨基甲酸環(huán)己酯
N-[1,1'-Biphenyl]-3-yl-
URB602 ada@tuskwei.com whatsapp
cyclohexyl biphenyl-3-ylcarbaMate
Cyclohexyl [1,1'-biphenyl]-3-ylcarbaMate
Monoacylglycerol Lipase Inhibitor, URB602
Biphenyl-3-yl Carbamic Acid, Cyclohexyl Ester
[1,1’-Biphenyl]-3-yl-carbamic acid cyclohexyl ester
應(yīng)用領(lǐng)域
常見(jiàn)問(wèn)題列表
IC50: 28±4 μM (rat brain MGL)
Without URB602, the apparent Michaelis constant (K m ) of MGL for 2-AG is 24±1.7 μM and the maximum velocity (V max ) is 1814±51 nmol min per mg protein; with URB602, the K m is 20±0.4 μM and the V max is 541±20 nmol min per mg protein (n=4). When organotypic slice cultures of rat forebrain are incubated with URB602 (100 μM), both baseline and Ca 2+ -ionophore-stimulated 2-arachidonoylglycerol (2-AG) concentrations are increased. URB602 is an inhibitor of monoacylglycerol lipase (MGL), a serine hydrolase involved in the biological deactivation of the endocannabinoid 2-arachidonoyl-sn-glycerol (2-AG). URB602 weakly inhibits recombinant MGL (IC 50 =223±63 μM) through a rapid and noncompetitive mechanism.
URB602 at doses of 20 and 40 mg/kg tends to reduce upper GI transit and slow colonic propulsion. When taken together as whole gut transit, URB602 dose dependently inhibits transit (P<0.05) compared with the vehicle control group. The inhibitory action of 40 mg/kg URB602 on whole gut transit is absent in these mice, indicating CB 1 receptor involvement in the inhibitory action. URB602 decreases the AUC of pain behaviour during the early phase of the formalin test with an ED 50 of 0.06±0.028 μg for JZL184 and 120±51.3 μg for URB602 in adult male Sprague-Dawley rats. Both MGL inhibitors also suppresses pain behaviour during the late phase of formalin pain, with an ED 50 of 0.03±0.011 μg for JZL184 and 66±23.9 μg for URB602.