| Title | Effect of anchoring 4-anilidopiperidines to opioid peptides. |
| Publication Type | Journal Article |
| Year of Publication | 2013 |
| Authors | Petrov RR, Lee YSun, Vardanyan RS, Liu L, Ma S-W, Davis P, Lai J, Porreca F, Vanderah TW, Hruby VJ |
| Journal | Bioorg Med Chem Lett |
| Volume | 23 |
| Issue | 11 |
| Pagination | 3434-7 |
| Date Published | 2013 Jun 1 |
| ISSN | 1464-3405 |
| Keywords | Animals, Cell Line, Fentanyl, Humans, Kinetics, Mice, Opioid Peptides, Piperidines, Protein Binding, Receptors, Opioid, delta, Receptors, Opioid, mu, Structure-Activity Relationship |
| Abstract | 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. |
| DOI | 10.1016/j.bmcl.2013.03.065 |
| Alternate Journal | Bioorg. Med. Chem. Lett. |
| PubMed ID | 23623418 |
| PubMed Central ID | PMC3942532 |
| Grant List | DA-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