Effects of the novel selective κ-opioid receptor agonist NP-5497-KA on morphine-induced reward-related behaviors.

ABSTRACT: Opioid addiction and the opioid overdose epidemic are becoming more serious, and the development of therapeutic agents is essential for the pharmacological treatment of substance use disorders. The κ-opioid receptor (KOP) is a member of the opioid receptor system that has been gaining attention as a promising molecular target for the treatment of numerous human disorders, including pain, depression, anxiety, and drug addiction. Here, we biologically and pharmacologically evaluated a novel azepane-derived ligand, NP-5497-KA, as a selective KOP agonist. NP-5497-KA had 1000-fold higher selectivity for the KOP over the μ-opioid receptor (MOP), which was higher than nalfurafine (KOP/MOP: 65-fold), and acted as a selective KOP full agonist in the 3',5'-cyclic adenosine monophosphate assay. The o

SUBMITTER: Ide S 

PROVIDER: S-EPMC10598265 | biostudies-literature | 2023 Oct

REPOSITORIES: biostudies-literature