A highly selective κ-opioid receptor agonist with low addictive potential and dependence liability

Hee Sock Park, Hee Yoon Lee, Yong Hae Kim, Jin Kyu Park, Edwin E. Zvartau, Heeseung Lee

Research output: Contribution to journalArticlepeer-review

13 Scopus citations

Abstract

Buprenorphine analogs have been synthesized. In the studies of analgesic and addictive effects in mice and [35S]GTPγS binding assay in human brain tissue, an analog of buprenorphine where the tert-butyl is replaced by a cyclobutyl moiety (16) has been identified as a selective κ-partial agonist which gives antinociceptive effects, but has low abuse potential. The results may lead to lower degrees of dysphoria than full κ-agonists.

Original languageEnglish
Pages (from-to)3609-3613
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number13
DOIs
StatePublished - 1 Jul 2006

Keywords

  • κ-partial agonist
  • Addiction
  • Buprenorphine
  • Opioid

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