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 language | English |
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Pages (from-to) | 3609-3613 |
Number of pages | 5 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 16 |
Issue number | 13 |
DOIs | |
State | Published - 1 Jul 2006 |
Keywords
- κ-partial agonist
- Addiction
- Buprenorphine
- Opioid