Design and synthesis of naltrexone-derived affinity labels with nonequilibrium opioid agonist and antagonist activities. Evidence for the existence of different. mu. …

LM Sayre, DL Larson, AE Takemori…

Index: Sayre, L. M.; Larson, D. L.; Takemori, A. E.; Portoghese, P. S. Journal of Medicinal Chemistry, 1984 , vol. 27, # 10 p. 1325 - 1335

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Citation Number: 46

Abstract

A series of@-funaltrexamine (2,@-FNA) analogues (3-14) were synthesized that contain a variety of electrophilic groups attached at the 6@-position of the opiate. The opioid agonist and antagonist activities of these ligands were evaluated in the guinea pig ileum (GPI) and mouse vas deferens (MVD) in vitro assays. Several of the compounds behaved like@-FNA in that they exhibited reversible agonist activity at K opioid receptors and irreversible ...