Probes for narcotic receptor mediated phenomena. 7. Synthesis and pharmacological properties of irreversible ligands specific for. mu. or. delta. opiate receptors

TR Burke Jr, BS Bajwa, AE Jacobson…

Index: Burke Jr.; Bajwa; Jacobson; Rice; Streaty; Klee Journal of Medicinal Chemistry, 1984 , vol. 27, # 12 p. 1570 - 1574

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Citation Number: 74

Abstract

Syntheses of affinity reagents for opiate receptors based on the fentanyl, endo- ethenotetrahydrooripavine, and etonitazene carbon-nitrogen skeletons are described. The isothiocyanate, bromoacetamido, and methylfumaramido alkylating functions were employed in these compounds, some of which had previously been shown to be p specific (12, BIT) and 6 specific (8, FIT and 19, FAO) in vitro. Antinociceptive activity of the title ...