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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. Copyright © 2014 Elsevier Ltd. All rights reserved.


Yeon Sun Lee, David Rankin, Sara M Hall, Cyf Ramos-Colon, Jose Juan Ortiz, Robert Kupp, Frank Porreca, Josephine Lai, Victor J Hruby. Structure-activity relationships of non-opioid [des-Arg(7)]-dynorphin A analogues for bradykinin receptors. Bioorganic & medicinal chemistry letters. 2014 Nov 01;24(21):4976-9

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PMID: 25282551

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