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. 1988 Jul 14;151(3):475-8.
doi: 10.1016/0014-2999(88)90546-8.

A novel series of potent and selective agonists at the opioid kappa-receptor

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A novel series of potent and selective agonists at the opioid kappa-receptor

G F Costello et al. Eur J Pharmacol. .

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.

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