LY2795050 is a novel specific κ-Opioid Receptor antagonist (IC50: 0.72 nM).

κ opioid receptor:0.72 nM

LY2795050 displays full antagonist activity and high binding affinity and selectivity for κ-opioid Receptor (Ki: 0.72 nM) [1].

In the brain, (11)C-LY2795050 displayed fast uptake kinetics (regional activity peak times of <20 min) and an uptake pattern consistent with the distribution of κ-Opioid Receptor (KOR) in primates [1]. The LY2795050 ED50 at MOR was 119 μg/kg based on a 1-site model for 11C-carfentanil. The 1-site binding model was also deemed sufficient to describe the specific binding of 11C-LY2795050 at KOR. The ED50 at KOR estimated from the 1-site model was 15.6 μg/kg. Thus, the ED50 ratio for MOR:KOR was 7.6 [2].