| Title | Structure-activity relationships of non-opioid [des-Arg(7)]-dynorphin A analogues for bradykinin receptors. |
| Publication Type | Journal Article |
| Year of Publication | 2014 |
| Authors | Lee YSun, Rankin D, Hall SM, Ramos-Colon C, Ortiz JJuan, Kupp R, Porreca F, Lai J, Hruby VJ |
| Journal | Bioorg Med Chem Lett |
| Volume | 24 |
| Issue | 21 |
| Pagination | 4976-9 |
| Date Published | 2014 Nov 01 |
| ISSN | 1464-3405 |
| Keywords | Animals, Brain, Dynorphins, Neurotransmitter Agents, Rats, Receptors, Bradykinin, Structure-Activity Relationship |
| Abstract | In our earlier studies, bradykinin receptors (BRs) were identified as a potential target for the neuroexcitatory effects of dynorphin A (Dyn A) in the central nervous system (CNS), and [des-Arg(7)]-Dyn A-(4-11) (6) was discovered as a lead ligand to modulate Dyn A-(2-13) induced neuroexcitatory effects in the CNS as an antagonist. In an effort to gain insights into key structural features of the Dyn A for the BRs, we pursued further structure-activity relationships (SAR) study on the [des-Arg(7)]-Dyn A analogs and confirmed that all of the [des-Arg(7)]-Dyn A analogues showed good binding affinities at the BRs. |
| DOI | 10.1016/j.bmcl.2014.09.033 |
| Alternate Journal | Bioorg. Med. Chem. Lett. |
| PubMed ID | 25282551 |
| PubMed Central ID | PMC4250343 |
| Grant List | P01 DA006284 / DA / NIDA NIH HHS / United States R01 DA013449 / DA / NIDA NIH HHS / United States NIDA P01DA006284 / / PHS HHS / United States R01DA013449 / DA / NIDA NIH HHS / United States |
Faculty Member Reference:
Frank Porreca, PhD