Binaltorphimine-related bivalent ligands and their. kappa. opioid receptor antagonist selectivity

PS Portoghese, H Nagase, AW Lipkowski…

Index: Portoghese, P. S.; Nagase, H.; Lipkowski, A. W.; Larson, D. L.; Takemori, A. E. Journal of Medicinal Chemistry, 1988 , vol. 31, # 4 p. 836 - 841

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Citation Number: 142

Abstract

In an effort to develop selective antagonists for K opioid receptors, bivalent ligands that contain opioid antagonist pharmacophores derived from naltrexone or other morphinans were synthesized and tested on the guinea pig ileum (GPI) and mouse vas deferens (MVD) preparations. The minimum requirements for K selectivity are at least one free phenolic OH group and one N-cyclopropyl or N-allyl substituent. Several compounds (3, 8, 10) with K ...