Chapter 31. Adenosine Receptors as Pharmacological Targets

摘要: Publisher Summary This chapter discusses several studies as well the recent literature on adenosine receptor structure–function and pharmacology associated with adenosinergic compounds. Despite therapeutic potential of compounds, only drugs currently marketed are itself for treatment supraventricular tachycardia transport blocker dipyridamole an adjunct to warfarin prevention postoperative thromboembolic events after heart valve surgery. The overall lack success date stems from ubiquitous nature receptors, profound evoked upon activation, absence compounds that activate receptors expressed target tissue. Adenosine a part G-protein coupled superfamily based molecular cloning sequencing studies. Sequence homology other protein-coupled indicates have classical seven transmembrane-helix topology, extracellular amino terminus, cytoplasmic carboxyl containing phosphorylation sites, domain could interact G-protein. Five subtypes been identified— namely, A 1, A2a, A2b, A3 A4 —based ligand-binding, signal transduction pathway, sequence criteria. first cloned were A1 A2a. agonists lower blood pressure by depressing cardiac conductance contractility through activation nodal cells myocytes. In context role protection results receptors. Activation A2a platelets prevents platelet subsequent aggregation, and, therefore, provides myocardial inhibiting intracoronary thrombosis. is believed function endogenous anti-inflammatory agent its ability inhibit cellular adhesion superoxide anion generation. Tissue damage induced inflammation in migration neutrophils sites followed release membrane-damaging oxygen radicals.