Evidence that A 2 purinoceptors are involved in endothelium‐dependent relaxation of the rat thoracic aorta

1 The effect of adenosine and some adenosine analogues on the isolated thoracic aorta from rats was compared with the effect of adenosine 5′‐triphosphate (ATP) and adenosine 5′‐diphosphate (ADP). 2 Both ATP and adenosine analogues caused relaxation of the noradrenaline (30 n m )‐contracted thoracic aorta. 3 The order of potency for adenosine analogues was 5′‐(N‐ethyl) carboxamidoadenosine (NECA) > l ‐N 6 ‐phenylisopropyladenosine ( l ‐PIA), adenosine 5′‐monophosphate (AMP), adenosine indicating the presence of adenosine A 2 receptors. 4 Removal of the endothelium or prior treatment with haemoglobin (10 μ m ) attenuated relaxant responses to both ATP and NECA, attenuation being greater for ATP than NECA. 5 8‐Phenyltheophylline (10 μ m ) reduced relaxant responses to NECA but not to ATP in the intact tissue. 6 These results provide evidence that there are two components to relaxation of the rat thoracic aorta induced by purinoceptor agonists. The first is an endothelium‐dependent mechanism involving release of endothelium‐derived relaxant factor (EDRF) and the second is due to a direct effect on smooth muscle.