Bioorganic and Medicinal Chemistry Letters p. 3638 - 3640 (2008)
Update date:2022-07-30
Topics:
Mercer, Susan L.
Cunningham, Christopher W.
Eddington, Natalie D.
Coop, Andrew
Numerous studies have shown that many clinically employed opioid analgesics are substrates for P-glycoprotein (P-gp), suggesting that up-regulation of P-gp may contribute to the development of central tolerance to opioids. The studies herein focus on the development of SAR for P-gp substrate activity in the meperidine series of opioids. Addition of a 3-OH to meperidine and the ketone analog of meperidine yielding bemidone and ketobemidone, respectively, significantly increased P-gp substrate affinity. The results of this study have implications in the development of novel analgesics to be utilized as tools to study the contribution of P-gp on the development of central tolerance to opioids.
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