Opioids and efflux transporters. Part 4: influence of N-substitution on P-glycoprotein substrate activity of noroxymorphone analogues.
Metcalf MD, Rosicky AD, Hassan HE, Eddington ND, Coop A, Cunningham CW, Mercer SL.
Metcalf MD, et al.
Bioorg Med Chem Lett. 2014 Aug 1;24(15):3592-5. doi: 10.1016/j.bmcl.2014.05.033. Epub 2014 May 22.
Bioorg Med Chem Lett. 2014.
PMID: 24915880
Free PMC article.
Here, we present SAR describing P-gp recognition of a short series of N-modified 4,5-epoxymorphinans. Oxymorphone, naloxone, naltrexone, and nalmexone all failed to demonstrate P-gp substrate activity, indicating these opioid scaffolds contain structural features that prec …
Here, we present SAR describing P-gp recognition of a short series of N-modified 4,5-epoxymorphinans. Oxymorphone, naloxone, naltrexone, and …