Adenosine receptor agonists and antagonists

Adenosine Receptors. Table 2 Affinity of commonly used adenosine receptor agonists and antagonists for defining pharmacologically adenosine receptor subtypes... 

Ma, H., Green, R.D., 1992. Modulation of cardiac cyclic AMP metabolism by adenosine receptor agonists and antagonists. Mol. Pharmacol. 42, 831-837. 

Taken together, using a mouse model of hindlimb skeletal muscle injury, all three adenosine receptor subtypes could each individually induce protection from ischemia-reperfusion injury in skeletal muscle. Due to the lack of a highly selective A2B receptor agonist and antagonist, its role in mediating an anti-ischemic effect in skeletal muscle remains to be determined. 

Table 3. Agonists and Antagonists of Adenosine Triphosphate and Receptors...

Presently, only adenosine itself is approved for clinical use. It is used widely in the treatment of supraventricular tachycardia and in cardiac stress imaging to assess coronary artery disease [5]. Other agonists and antagonists and an allosteric modulator of the Ai receptor are in clinical trials for a variety of indications. 

PI (adenosine) receptors were explored as therapeutic targets before P2 receptors. Adenosine was identified early and is in current use to treat supraventricular tachycardia. A2a receptor antagonists are being investigated for the treatment of Parkinson s disease and patents have been lodged for the application of PI receptor subtype agonists and antagonists for myocardial ischaemia and reperfusion injury, cerebral ischaemia, stroke, intermittent claudication and renal insufficiency. 

Kourounakis A, Visser C, de Groote M, Ijzerman AP. Differential effects of the allosteric enhancer PD81,723 on agonist and antagonist binding and function at the human wild type and a mutant (T277A) adenosine At receptor. Biochem Pharmacol 2000 61 137-144. 

Dalpiaz A, Townsend-Nicholson A, Beukers MW, Schofield P, Ijzerman AP. Thermodynamics of full agonist, partial agonist and antagonist binding to wild type and mutant adenosine Ai receptors. Biochem Pharmacol 1998 56 1437-1445. 

TABLE 17-2 Subtypes of adenosine receptor, their effectors and selective agonists and antagonists ... 

FIGURE 17-7 The structures of selective agonists and antagonists of adenosine receptors. 

Fig. 2.1 van t Hoff plots showing the effect of temperature on the equilibrium binding association constants, KA, for [3H]-MRE 3008F20 in various cell lines examined (a) and for six adenosine receptor agonists (b) and antagonists (c) studied. All plots are essentially linear (r in the range 0.91-0.99) in the temperature range of 0-30°C... 

Blay J, White TD, Hoskin DW (1997) The extracellular fluid of solid carcinomas contains immunosuppressive concentrations of adenosine. Cancer Res 57(13) 2602-2605 Bruns RF (1980) Adenosine receptor activation in human fibroblasts nucleoside agonists and antagonists. Can J Physiol Pharmacol 58(6) 673-691 Cerniway RJ, Yang Z, Jacobson MA, Linden J, Matherne GP (2001) Targeted deletion of A3 adenosine receptors improves tolerance to ischemia-reperfusion injury in mouse myocardium. Am J Physiol 281(4) H1751-H1758... 

Freissmuth M, Selzer E, Schtitz W (1991) Interactions of purified bovine brain Al-adenosine receptors with G-proteins. Reciprocal modulation of agonist and antagonist binding. Biochem J 275(Pt 3) 651-656... 

Cosyn L, Palaniappan KK, Kim SK, Duong HT, Gao ZG, Jacobson KA, Van Calenbergh S (2006b) 2-Triazole-substituted adenosines a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists. J Med Chem 49(25) 7373-7383... 

Triazole-substituted adenosines a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists. J Med Chem 49 7373-7383... 

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