Structure-activity relationship of 2-(ar) alkoxyadenosines at the adenosine A2 receptor in coronary artery

Add time:07/25/2019    Source:sciencedirect.com

We examined the ability of four 2-(ar)alkoxyadenosines (2-(-phenylethoxy)adenosine, PEA; 2-[2-(2-naphthyl)ethoxy]adenosine, NEA; 2-[2-(4-methylphenyl)ethoxy]adenosine, mPEA; 2-(1-hexyloxy)adenosine, HOA) to relax porcine coronary artery in vitro. All four compounds produced concentration-dependent relaxations in rings contracted with 30 mM KCl. The EC25 values are as follows (× 10−9 mol/1): CGS21680, (2-[p-(2-carboxyetyl)phenethylaminol]-5′-N-ethylcarbonxamidoadenosine) (32.7) ≈ NECA, 5′-N-ethylcarbonxamidoadenosine (51.4) ∼ NEA (74.3) ≈ NEA (160.7) >HOA (855.1) ≈ PEA (1259) ≈ 2-chloroadenosine (1871) >adenosine (9705). However. EC75 values for all the compounds except adenosine were found to be independent converged to a range of 8.16 to 22.86 μM, suggesting a biphasic response. Furthermore, the responses were found to be independent of endothelial integrity. The unselective adenosine receptor antagonist 8-p-sulphophenyltheophylline (100 μM) attenuated the relaxant response to NNEA (EC25 = 1172 nM), suggesting that adenosine receptors mediated relaxation. Structure-activity correlations suggest that the adenosine A2 receptor in porcine coronary artery contains a region of limited bulk tolerance juxtaposed to the region occupied by adenine C-2 and distal to that a large hydrophobic region.

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