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Comparison of pharmacological activities of buprenorphine and norbuprenorphine: norbuprenorphine is a potent opioid agonist.
The binding of norBUP to opioid and nociceptin/orphanin FQ (ORL1) receptors, and its effects on [(35)S]guanosine-5'-O-(gamma-thio)triphosphate ([(35]S]GTP gamma S) binding mediated by opioid or ORL1 receptors are described and highlighted.
2-Methoxymethyl-Salvinorin B Is a Potent κ Opioid Receptor Agonist with Longer Lasting Action in Vivo Than Salvinorin A
MOM-Sal B is a potent and efficacious KOPR agonist with longer lasting in vivo effects than Sal A, and was more potent than U50,488H in both tests and more efficacious in the hot-plate test.
Comparison of Pharmacological Activities of Three Distinct κ Ligands (Salvinorin A, TRK-820 and 3FLB) on κ Opioid Receptors in Vitro and Their Antipruritic and Antinociceptive Activities in Vivo
In vitro pharmacological activities on receptors expressed in Chinese hamster ovary cells and in vivo antiscratch and antinociceptive activities in mice are investigated and salvinorin A, TRK-820, and 3FLB caused internalization of the human KOR in a dose-dependent manner.
GEC1 interacts with the kappa opioid receptor and enhances expression of the receptor.
GEC1 interacted with N-ethylmaleimide-sensitive factor (NSF) in pull-down assays and co-immunoprecipitated with NSF in rat brain extracts and the interaction is important for trafficking of the receptor in the biosynthesis pathway.
Mouse model of OPRM1 (A118G) polymorphism has sex-specific effects on drug-mediated behavior
This work derived a mouse model possessing the equivalent nucleotide/amino acid substitution in the Oprm1 gene and found sex-specific reductions in the rewarding properties of morphine and the aversive components of naloxone-precipitated morphine withdrawal.
The association of NHERF adaptor proteins with g protein-coupled receptors and receptor tyrosine kinases.
This review summarizes the emerging data on the biochemical mechanisms, physiologic outcomes, and potential clinical implications of the assembly and disassembly of receptor/NHERF complexes.