Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine

Gerta Cami-Kobeci, W E Polgar, T V Khroyan, L Toll, Stephen M Husbands

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The unique pharmacological profile of buprenorphine has led to its considerable success as an analgesic and as a treatment agent for drug abuse. Activation of nociceptin/orphanin FQ peptide (NOP) receptors has been postulated to account for certain aspects of buprenorphine's behavioral profile. In order to investigate the role of NOP activation further, a series of buprenorphine analogues has been synthesized with the aim of increasing affinity for the NOP receptor. Binding and functional assay data on these new compounds indicate that the area around C20 in the orvinols is key to NOP receptor activity, with several compounds displaying higher affinity than buprenorphine. One compound, 1b, was found to be a mu opioid receptor partial agonist of comparable efficacy to buprenorphine but with higher efficacy at NOP receptors.
Original languageEnglish
Pages (from-to)6531-6537
Number of pages7
JournalJournal of Medicinal Chemistry
Issue number19
Early online date24 Aug 2011
Publication statusPublished - 13 Oct 2011


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