Opioids and efflux transporters. Part 1: P-Glycoprotein substrate activity of N-substituted analogs of meperidine

…, HE Hassan, CW Cunningham, ND Eddington…

Index: Mercer, Susan L.; Hassan, Hazem E.; Cunningham, Christopher W.; Eddington, Natalie D.; Coop, Andrew Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 5 p. 1160 - 1162

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Citation Number: 19

Abstract

P-Glycoprotein (P-gp) is an efflux transporter which is up-regulated at the blood–brain barrier in both morphine-and oxycodone-tolerant rats. Numerous studies have shown that many clinically employed opioid analgesics are substrates for 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 ...