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ABSTRACT: Three novel opioid agonist are described. These compounds were found to bind with high affinity and selectivity to the κ-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 κ-receptor function.
European Journal of Pharmacology. 01/1988;