Effect of anchoring 4-anilidopiperidines to opioid peptides.

TitleEffect of anchoring 4-anilidopiperidines to opioid peptides.
Publication TypeJournal Article
Year of Publication2013
AuthorsPetrov RR, Lee YSun, Vardanyan RS, Liu L, Ma S-W, Davis P, Lai J, Porreca F, Vanderah TW, Hruby VJ
JournalBioorg Med Chem Lett
Date Published2013 Jun 1
KeywordsAnimals, Cell Line, Fentanyl, Humans, Kinetics, Mice, Opioid Peptides, Piperidines, Protein Binding, Receptors, Opioid, delta, Receptors, Opioid, mu, Structure-Activity Relationship

We report here the design, synthesis, and in vitro characterization of new opioid peptides featuring a 4-anilidopiperidine moiety. Despite the fact that the chemical structures of fentanyl surrogates have been found suboptimal per se for the opioid activity, the corresponding conjugates with opioid peptides displayed potent opioid activity. These studies shed an instructive light on the strategies and potential therapeutic values of anchoring the 4-anilidopiperidine scaffold to different classes of opioid peptides.

Alternate JournalBioorg. Med. Chem. Lett.
PubMed ID23623418
PubMed Central IDPMC3942532
Grant ListDA-06284 / DA / NIDA NIH HHS / United States
DA-12394 / DA / NIDA NIH HHS / United States
R01 DA013449 / DA / NIDA NIH HHS / United States
Faculty Member Reference: 
Victor Hruby, Ph.D.
Josephine Lai , Ph.D.
Frank Porreca, PhD
Todd Vanderah, PhD