A adenosine agonists

Macdonald, R. L., Skerritt, J. H., Werz, M. A. Adenosine agonists reduce voltage-dependent calcium conductance of mouse sensory neurones in cell culture, J. Physiol. 1986, 370, 75-90. 

There are not yet any agonists that are truly selective for the A2BAR, known as the low affinity adenosine A2 receptor. A novel agonist, the 2-(6-bromotryptophol) ether derivative MRS3997 16, is a full agonist with mixed selectivity at A2a and A2BARs. 

Mathot RAA, van Schaick EA, Langemeijer MWE, Soudijn W, Breimer DD, Ijzerman AP, Danhof M. Pharmacokinetic-pharmacodynamic relationship of the cardiovascular effects of the adenosine A receptor agonist A -cyclopentyladenosine (CPA) in the rat. J Pharmacol Exp Ther 1994 268 616-624. 

Townsend-Nicholson A, Schofield PR. A threonine residue in the seventh transmembrane domain of the human A, adenosine receptor mediates specific agonist binding. J Biol Chem 1994 269 2373-2376. 

Hong, Z. Y., Huang, Z. L., Qu, W. M. et al. (2005). An adenosine A receptor agonist induces sleep by increasing GABA release in the tuberomammillary nucleus to inhibit histaminergic systems in rats. J. Neurochem. 92 (6), 1542-9. 

Clark, R.L., Eschbach, K., Cusick, W.A. and Heyse, J.F. (1987). Interactions between caffeine and adenosine agonists in producing embryo resorptions and malformations in mice. Toxicol. Appl. Pharmacol. 91 371-385. 

Changes in the activity of adenosine receptors have been implicated in the stimulant effects of drugs like caffeine. Carbamazepine exhibits a partial agonist effect on adenosine receptors, and experimental evidence suggests that the reduced reuptake and release of noradrenaline caused by the drug are due to its interaction with these receptors. The precise relevance of these findings to its anticonvulsant and psychotropic effects is presently unclear. 

Research on compounds that interact with adenosine A1 receptors has focused on agonists with structures based on adenosine itself as agents that will overcome responses due to inappropriate excitation such as tachycardia and some arrhythmias. Replacement of one of the hydrogen atoms on the exocyclic amine in adenosine by a tetrahydrofuryl group provides an effective A1 adenosine agonist. Preparation of this fragment as a single enantiomer starts with a modem version of the Curtius reaction. 

Palmer TM, Stiles GL (2000) Identification of threonine residues controlling the agonist-dependent phosphorylation and desensitization of the rat A, adenosine receptor. Mol Pharmacol 57(3) 539-545... 

Von Lubitz DK, Lin RC, Boyd M, Bischofberger N, Jacobson KA (1999) Chronic administration of adenosine A receptor agonist and cerebral ischemia neuronal and glial effects. Eur J Pharmacol 367(2-3) 157-63... 

A, Adenosine Receptor Agonists History and Future Perspectives... 

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