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Opioid receptor agonists and antagonists act on mu, delta and kappa receptors and the related nociceptin receptor. All four are G protein-coupled receptors that respond to endogenous peptides such as endorphins, enkephalins and dynorphins. Expression cloning of the delta opioid receptor in 1992 opened the family to molecular study. The nociceptin/orphanin FQ peptide (NOP) receptor, first called opioid receptor-like 1 (ORL1), was matched to its endogenous peptide agonist in 1995. Dynorphin A (1-13) Acetate is a peptide agonist at the kappa receptor, and JDTic is a kappa antagonist. SR-17018 acts as a mu agonist, while alvimopan is a peripherally acting opioid antagonist. MCOPPB trihydrochloride is a NOP agonist, and BAN ORL 24 blocks the same receptor.
N-Desmethyl-loperamide is a significant metabolite of loperamide, primarily targeting μ-opioid receptors with a Ki value of 0.16 nM. This compound exhibits activity as a substrate for the ATP-dependent efflux transporter P-glycoprotein. It is useful for studies examining peripheral μ-opioid receptor activation and the role of P-glycoprotein in drug transport.
