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A novel series of potent and selective agonists at the opioid kappa-receptor
G F Costello1, B G Main, J J Barlow
1Bioscience Department, ICI Pharmaceuticals Division, Macclesfield, Cheshire, U.K.
European Journal of Pharmacology
|July 14, 1988
Abstract:
Three novel opioid agonists are described. These compounds were found to bind with high affinity and selectivity to the kappa-opioid receptor. Isolated tissue studies using the field-stimulated mouse vas deferens and guinea-pig ileum preparations confirmed the high agonist potency and naloxone-reversibility of these agents. All three compounds exhibited potent antinociceptive activity in the mouse abdominal constriction model. These compounds should prove useful as tools to investigate kappa-receptor function.