Peng Huang, Conrad K Ho, Danni Cao, Saadet Inan, Scott M Rawls, Mengchu Li, Boshi Huang, Piyusha P Pagare, E Andrew Townsend, Justin L Poklis, Matthew S Halquist, Matthew Banks, Yan Zhang, Lee-Yuan Liu-Chen
While agonists of mu (MOR) and kappa (KOR) opioid receptors have analgesic effects, they produce euphoria and dysphoria, respectively. Other side effects include respiratory depression and addiction for MOR agonists and sedation for KOR agonists. We reported that 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-{[4'-(2'-cyanopyridyl)]carboxamido}cmorphinan (NCP) displayed potent KOR full agonist and MOR partial agonist activities (58%) with 6.5x KOR-over-MOR selectivity in vitro Herein, we characterized pharmacological effects of NCP in rodents...
February 26, 2024: Journal of Pharmacology and Experimental Therapeutics