Analgesic Activity of the Kappa Opioid Receptor Agonist RU-1205 in Rats

Orvinols with Mixed Kappa/Mu Opioid Receptor Agonist Activity

Dual-acting kappa opioid receptor (KOR) agonist and mu opioid receptor (MOR) partial agonist ligands have been put forward as potential treatment agents for cocaine and other psychostimulant abuse. Members of the orvinol series of ligands are known for their high binding affinity to both KOR and MOR, but efficacy at the individual receptors has not been thoroughly evaluated. In this study, it i...

GR89,696 is a kappa-2 opioid receptor agonist and a kappa-1 opioid receptor antagonist in the guinea pig hippocampus.

Receptor binding studies and electrophysiological studies demonstrated the existence of at least two kappa opioid receptors, which have been designated kappa-1 and kappa-2. Several agonists and antagonists are selective for the kappa-1 receptor whereas no known ligands are selective for the kappa-2 receptor. In this study, the kappa opioid GR89,696 was tested in the guinea pig hippocampal slice...

Prolonged opportunity for ischemic neuroprotection with selective kappa-opioid receptor agonist in rats.

BACKGROUND AND PURPOSE We have previously demonstrated that pretreatment with selective kappa-opioid agonist BRL 52537 hydrochloride [(+/-)-1-(3,4-dichlorophenyl) acetyl-2-(1-pyrrolidinyl) methylpiperidine], provides ischemic neuroprotection following transient focal ischemia in rats. The present study was undertaken to a) define "therapeutic opportunity" for ischemic neuroprotection with BRL 5...

Opioid Kappa Receptor Selective Agonist TRK-820 (Nalfurafine Hydrochloride)

Spinally mediated analgesic interaction between γ-aminobutyric acid B receptor agonist and glutamate receptor antagonists in rats

Background.  Many mechanisms are involved in pain transmission in the spinal cord.  Therefore, combination of drugs acting on different kinds of mechanisms might be useful for analgesia.  We investigated the interaction betweenγ-aminobutyric acid （GABA）B receptor agonist, baclofen, and N-methyl-D-aspartate （NMDA） receptor antagonist, AP-5, orα-amino-3-hydroxy-5-methylisoxazole-4-propionic acid ...