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

MedChemComm Pub Date: 2011-11-30 DOI: 10.1039/C2MD00247G

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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