[11C]MePPEP

[11C]MePPEP is a radioligand developed for positron emission tomography (PET) imaging of cannabinoid CB1 receptors in the brain. It is characterized by high brain uptake, high specific binding to CB1 receptors, and adequately fast washout from the brain that allows quantification of receptor density. The chemical structure contains a carbon-11 isotope in its methoxy group, which gives it its radioactive properties necessary for PET imaging. This radioligand has shown good to excellent reproducibility for quantifying CB1 receptor availability using several kinetic models and model-free analyses. It has been used in research to investigate CB1-receptor mediated neurotransmission in both healthy subjects and those with psychiatric disorders. The regional uptake of [11C]MePPEP in the brain is consistent with the known distribution of CB1 receptors, with high radioactivity observed in the striatum and cerebellum and low levels in the thalamus and pons. Studies have confirmed that the majority (>89%) of brain uptake in regions with high receptor densities is specific and reversibly bound to CB1 receptors. The compound acts as an inverse agonist at cannabinoid CB1 receptors, making it valuable for studying the endocannabinoid system in various neurological and psychiatric conditions.

Other names

(3R,5R)-5-(3-[11C]methoxy-phenyl)-3-((R)-1-phenyl-ethylamino)-1-(4-trifluoromethyl-phenyl)-pyrrolidin-2-one