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Published on: September 20, 2016
Structure-activity relationships of non-opioid [des-Arg(7)]-dynorphin A analogues for bradykinin receptors
Yeon Sun Lee1, David Rankin2, Sara M Hall1
1Department of Chemistry and Biochemistry, University of Arizona, Tucson, AZ 85721, USA.
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.
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