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-Arg7]-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-Arg7]-Dyn A analogs and confirmed that all of the [des-Arg7]-Dyn A analogues showed good binding affinities at the BRs.
Original language | English (US) |
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Pages (from-to) | 4976-4979 |
Number of pages | 4 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 24 |
Issue number | 21 |
DOIs | |
State | Published - Nov 1 2014 |
Keywords
- Bradykinin receptors
- Chronic pain
- Non-opioid dynorphin A
- Structure-activity relationship
- pH sensitivity
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry