LY2795050

LY2795050 is a selective, short-acting antagonist of the kappa-opioid receptor (KOR), developed primarily as a radiotracer for positron emission tomography (PET) imaging in the brain. It exhibits high affinity and selectivity for KOR over mu-opioid and delta-opioid receptors (Ki values of approximately 0.72 nM for KOR, with much lower affinity for MOR and DOR)[2][8]. In preclinical studies and clinical PET imaging applications, [11C]LY2795050 has demonstrated favorable pharmacokinetics with rapid brain uptake and specific binding to regions rich in KOR[1][4][6]. The compound was originally developed by Eli Lilly & Co., mainly as a diagnostic tool to study neuropsychiatric conditions involving the kappa-opioid system such as depression and post-traumatic stress disorder[5]. Its mechanism of action is antagonism at the kappa-opioid receptor.

Other names

[11C]LY2795050