Preprint
Article
Development of Bicyclo[3.1.0]hexane-based A3 Receptor Ligands – Closing the Gaps in the Structure-affinity Relationships
Submitted:
09 March 2022
Posted:
10 March 2022
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Abstract
In this paper, a series of bicyclo[3.1.0]hexane-based nucleosides were synthesized and evaluated for their P1 receptor affinities in radioligand binding studies. The most potent derivative 30 displayed moderate A3AR affinity (Ki of 0.38 μM) and high A3R selectivity. A subset of compounds varied at 5’-position was further evaluated in functional P2Y1R assays displaying no off-target activity.
Keywords:
Adenosine receptors
; methanocarba
; bicyclo[3.1.0]hexane
; A3 receptors
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Copyright: This open access article is published under a Creative Commons CC BY 4.0 license, which permit the free download, distribution, and reuse, provided that the author and preprint are cited in any reuse.
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