High impact information on [(1S)-5,6-dichloroindan-1-yl]-[(3R)-3-(pyrrolidin-1-ylmethyl)thiomorpholin-4-yl]methanone

• Effects of R-84760, a selective kappa-opioid receptor agonist, on nociceptive reflex in isolated neonatal rat spinal cord [1].
• R-84760 at 10 nM decreased the slow ventral root potential to 35% of the control, leaving the monosynaptic reflex unaffected [1].
• Pharmacological properties of R-84760, a novel kappa-opioid receptor agonist [2].

Analytical, diagnostic and therapeutic context of [(1S)-5,6-dichloroindan-1-yl]-[(3R)-3-(pyrrolidin-1-ylmethyl)thiomorpholin-4-yl]methanone

• On oral administration, R-84760 was 20-2077 times more potent than the same reference drugs [2].
• Rapid, real-time sampling of R-84760 in blood by in vivo microdialysis with tandem mass spectrometry [3].
• Quantitative analysis of R-84760, a selective kappa-opioid receptor agonist, in plasma by liquid chromatography with electrospray ionization tandem mass spectrometry [4].
• Intracerebroventricular and intrathecal injection, as well as subcutaneous administration of naloxone antagonized the antinociceptive effect of R-84760, suggesting the sites of action of R-84760 were at the spinal and supraspinal levels [5].

References