Characteristics of P2 (nucleotide) receptors mediating contraction and relaxation of rat aortic strips: possible physiological relevance.

ATP and ADP relaxed rat aortic strips precontracted with noradrenaline by an endothelium-dependent mechanism. 5'-AMP was much less potent and adenosine was essentially without effect. The metabolically stable analogues alpha,beta-methylene ATP and beta,gamma-methylene ATP further contracted precontracted aorta. Aortic strips, which had not been precontracted with noradrenaline, contracted when exposed to either ATP or alpha,beta-methylene ATP, the latter nucleotide being much more potent than the former. Removal of the endothelium increased the contractions to ATP. ANAPP3 had no effect on the endothelium-dependent relaxations produced by ATP but it antagonized contractions produced by alpha,beta-methylene ATP. These results provide evidence for the possible existence of two subtypes of P2 receptors in rat aorta; a P2 receptor mediating contraction residing on smooth muscle which can be antagonized by ANAPP3 and where alpha,beta-methylene ATP is more potent than ATP, and a P2 receptor mediating relaxation located on the endothelium which cannot be antagonized by ANAPP3 and where ATP is much more potent than alpha,beta-methylene ATP.