Opioids and efflux transporters. Part 3: P-glycoprotein substrate activity of 3-hydroxyl addition to meperidine analogs
SL Mercer, CW Cunningham, ND Eddington…
Index: Mercer, Susan L.; Cunningham, Christopher W.; Eddington, Natalie D.; Coop, Andrew Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 12 p. 3638 - 3640
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Citation Number: 11
Abstract
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 ...
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