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Adenosine receptors: Clinical implications and biochemical mechanisms

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Book cover Progress in Drug Research / Fortschritte der Arzneimittelforschung / Progrès des recherches pharmaceutiques

Abstract

Adenosine receptors comprise a group of cell surface receptors which mediate the physiological effects of adenosine. These receptors were originally classified by Burnstock as P1 and P2 purinergic receptors, depending on their preference for adenosine or adenine nucleotides [1]. The relative potencies for P1 sites are adenosine ≥ AMP ≥ ADP ≥ ATP, while relative potencies for P2 sites are ATP ≥ ADP ≥ AMP ≥ adenosine [1]. Further distinctions between P1 and P2 sites can be made by the use of selective antagonists. For example, methylxan-thines, such as theophylline and 3-isobutyl-1-methylxanthine, are potent inhibitors of P1 receptors, but are without effect on P2 sites. These latter sites are selectively blocked by quinidine and high concentrations of 2-substituted imidazoline compounds such as antazoline and phentolamine, and 2’2-dipyridilisatogen.

G.L.S. is an Established Investigator of the American Heart Association, and is supported in part by National Heart, Lung, and Blood Institute Grant RO1 HL35134, and Grant-in-aid 85612 from the American Heart Association, with funds contributed in part by the North Carolina Affiliate.

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  1. Departments of Medicine and Biochemistry, Duke University Medical Center, Durham, NC, 27710, USA

    Vickram Ramkumar, George Pierson & Gary L. Stiles

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Ramkumar, V., Pierson, G., Stiles, G.L. (1988). Adenosine receptors: Clinical implications and biochemical mechanisms. In: Progress in Drug Research / Fortschritte der Arzneimittelforschung / Progrès des recherches pharmaceutiques. Progress in Drug Research / Fortschritte der Arzneimittelforschung / Progrès des recherches pharmaceutiques, vol 32. Birkhäuser Basel. https://doi.org/10.1007/978-3-0348-9154-7_7

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