A3 adenosine receptor

The synthesis and biological studies of a new series of pyrazolo[4,3-e][l,2,4]triazolo[l,5-cjpyrimidines as antagonists of the human A3 adenosine receptor have been reported <06JMC1720>. 

A2a adenosine receptors are highly expressed in the basal ganglia 314 A2b adenosine receptors regulate vascular permeability 314 A3 adenosine receptors are few in the central nervous system 314... 

Macek, T. A., Schaffhauser, H., and Conn, P. J. (1998) Protein kinase C and A3 adenosine receptor activation inhibit presynaptic metabotropic glutamate receptor (mGluR) function and uncouple mGluRs from GTP-binding proteins. J. Neurosci. 18, 6138-6146. 

Palmer, T. M., Benovic, J. L., and Stiles, G. L. (1995) Agonist-dependent phosphorylation and desensitization of the rat A3 adenosine receptor. Evidence for a G-protein-conpled receptor kinase- mediated mechanism. J. Biol. Chem. 270, 29607-29613. 

Gao Z-G, Jacobson KA (2004) Partial agonists for A3 adenosine receptors. Curr Topics Med Chem 4 855-862... 

Gao Z, Li BS, Day YJ, Linden J (2001) A3 adenosine receptor activation triggers phosphorylation of protein kinase B and protects rat basophilic leukemia 2H3 mast cells from apoptosis. Mol Pharmacol 59 76-82... 

Gao Z-G, Kim S-K, Biadatti T, Chen W, Lee K, Barak D, Kim S-G, Johnson CR, Jacobson KA (2002) Structural determinants of A3 adenosine receptor activation nucleoside ligands at the agonist/antagonist boundary. J Med Chem 445 4471-4484 Gao Z-G, Blaustein JB, Gross AS, Melman N, Jacobson KA (2003) M -Substituted adenosine derivatives selectivity, efficacy, and species differences at A3 adenosine receptors. Biochem Pharmacol 65 1675-1684... 

Kohno Y, Ji X, Mawhorter SD, Koshiba M, Jacobson KA (1996) Activation of A, adenosine receptors on human eosinophils elevates intracellular calcium. Blood 88 3569 Linden J, Taylor HE, Robeva AS, Tucker AL, Stehle JH, Rivkees SA, Fink JS, Reppert SM (1993) Molecular cloning and functional expression of a sheep A3 adenosine receptor with widespread tissue distribution. Mol. Pharmacol. 44 524-532. 

Salvatore CA, Tilley SL, Latour AM, Fletcher DS, Koller BH, Jacobson MA (2000) Disruption of the A3 adenosine receptor gene in mice and its effect on stimulated inflammatory cells. J Biol Chem 275 4429 1434... 

Shneyvays V, Jacobson KA, Li AH, Nawrath H, Zinman T, Isaac A, Shainberg A (2000) Induction of apoptosis in rat cardiocytes by A3 adenosine receptor activation and its suppression by isoproterenol. Exp Cell Res 257 111-126... 

Thermodynamic Analysis in Drug-Receptor Binding The A3 Adenosine Receptor... 

Table 2.2 Thermodynamic parameters for pH]-MRE 3008F20 saturation binding experiments to different cell lines expressing A3 adenosine receptors...

Fig. 2.2 Scatter plot of -TAS° versus AH° values for the adenosine A3 receptor ligands (n = 11) studied obtained in hA3 CHO cells (a). Scatter plot of a typical series of adenosine compounds (n = 85) for the A, A2A, A2B and A3 adenosine receptor subtypes (b). Full and open symbols indicate antagonists and agonists, respectively. All points lie on a same regression line. The two dashed lines indicate the loci of the points representing possible combinations of AH° and -TAS° values giving rise to the two different equilibrium constants indicated (KA = 104 and KA = 1011 M )...

Gessi S, Varani K, Merighi S, Morelli A, Ferrari D, Leung E, Baraldi PG, Spalluto G, Borea PA (2001) Pharmacological and biochemical characterization of A3 adenosine receptors in Jurkat T cells. Br J Pharmacol 134(1) 116-126... 

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