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

作者：Dale Clare L; Hill Stephen J^*; Kellam Barrie

来源：Medchemcomm, 2012, 3(3): 333-338.

DOI：10.1039/c2md00247g

New, short-linker BODIPY 630/650 (TM) 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 N-6-amino group of NECA and the fluorophore are preferred with the best ligand (15b, aminopropyl linker) displaying the greatest potency (Log IC50 (G(i)) = -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.

• 出版日期2012-3