meppep

MePPEP is a synthetic small molecule that acts as an inverse agonist and antagonist at the cannabinoid CB1 receptor. It is primarily used as a radioligand in positron emission tomography (PET) imaging to visualize and quantify CB1 receptors in the brain. Radiolabeled with carbon‑11 ([11C]MePPEP), it enables noninvasive assessment of CB1 receptor distribution and density in both preclinical animal models and human subjects. This tool has been applied in research on psychiatric disorders such as alcohol dependence and psychoses, as well as studies of the endocannabinoid system’s role in various physiological processes[2][6][7]. MePPEP demonstrates high affinity for the CB1 receptor (Kd ≈ 0.16 nM), high specific binding signal, favorable brain uptake kinetics for PET quantification, and is not a substrate for P-glycoprotein efflux at the blood-brain barrier[2][7].

Other names

2-pyrrolidinone, 5-(3-methoxyphenyl)-3-(((1R)-1-phenylethyl)amino)-1-(4-(trifluoromethyl)phenyl)-, (3R,5R)-(3R,5R)-5-(3-methoxyphenyl)-3-((R)-1-phenylethylamino)-1-(4-trifluoromethylphenyl)pyrrolidin-2-oneUNII-CS3P21MZK4UNII-CS-3P21MZK4UNII-CS 3P21MZK4UNII-5JL4MD0N76UNII5JL4MD0N76UNII 5JL4MD0N76CS3P21MZK4CS-3P21MZK4CS 3P21MZK41059188–74–71022083–25–5