BU08073 a buprenorphine analogue with partial agonist activity at μ-receptors in vitro but long-lasting opioid antagonist activity in vivo in mice

BACKGROUND AND PURPOSE: Buprenorphine is a potent analgesic with high affinity at μ, δ and κ and moderate affinity at nociceptin opioid (NOP) receptors. Nevertheless, NOP receptor activation modulates the in vivo activity of buprenorphine. Structure activity studies were conducted to design buprenor...

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Vydáno v:Br J Pharmacol
Hlavní autoři: Khroyan, T V, Wu, J, Polgar, W E, Cami-Kobeci, G, Fotaki, N, Husbands, S M, Toll, L
Médium: Artigo
Jazyk:Inglês
Vydáno: Blackwell Publishing Ltd 2015
Témata:
Themed Section: Opioids: New Pathways to Functional Selectivity
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC4292977/
https://ncbi.nlm.nih.gov/pubmed/24903063
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1111/bph.12796
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