University of Hertfordshire

From the same journal

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

Research output: Contribution to journalArticlepeer-review

  • Gerta Cami-Kobeci
  • Willma E. Polgar
  • Taline V. Khroyan
  • Lawrence Toll
  • Stephen M. Husbands
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Original languageEnglish
Pages (from-to)6531-6537
Number of pages7
JournalJournal of Medicinal Chemistry
Publication statusE-pub ahead of print - 25 Aug 2011


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.


© 2011 American Chemical Society

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