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Issue 3, 2012
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New potent, short-linker BODIPY-630/650™ labelled fluorescent adenosine receptor agonists

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Abstract

New, short-linker BODIPY 630/650™ fluorescent conjugates of the adenosine receptor ligand N-ethylcarboxamido-adenosine (NECA) have been synthesised and pharmacologically evaluated. These novel conjugates confirm that short linkers between the N6-amino group of NECA and the fluorophore are preferred with the best ligand (15b, aminopropyl linker) displaying the greatest potency (Log IC50 (Gi) = −9.31) at the human adenosine A1-receptor. Imaging studies with this compound confirmed it can be employed to selectively label the human adenosine A1-receptor in single living cells, with receptor-associated binding prevented by preincubation with the nonfluorescent antagonist DPCPX.

Graphical abstract: New potent, short-linker BODIPY-630/650™ labelled fluorescent adenosine receptor agonists

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Publication details

The article was received on 30 Sep 2011, accepted on 25 Nov 2011 and first published on 30 Nov 2011


Article type: Concise Article
DOI: 10.1039/C2MD00247G
Med. Chem. Commun., 2012,3, 333-338

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    New potent, short-linker BODIPY-630/650™ labelled fluorescent adenosine receptor agonists

    C. L. Dale, S. J. Hill and B. Kellam, Med. Chem. Commun., 2012, 3, 333
    DOI: 10.1039/C2MD00247G

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