Adenosine receptor subtype

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

Stiles GL. Adenosine receptor subtypes new insights from cloning and functional studies. In Jacobson KA, Jarvis MF, eds. Purinergic Approaches in Experimental Therapeutics. New York Wiley-Liss, 1997 29-37. 

Marks, G. A., Shaffery, J. P., Speciale, S. G. Birabil, C. G. (2003). Enhancement of rapid eye movement sleep in the rat by actions at Al and A2A adenosine receptor subtypes with a differential sensitivity to atropine. Neuroscience 116, 913-20. 

The P-site of adenylyl cyclase inhibits cyclic AMP accumulation 308 There are four adenosine receptor subtypes 308 Xanthines block P2 but not P2 receptors 309... 

There are four adenosine receptor subtypes. There are four subtypes of adenosine (Pj) receptor that have... 

Okada M, Kawata Y, Murakami T, Wada K, Mizuno K, Kondo T, Kaneko S. (1999). Differential effects of adenosine receptor subtypes on release and reuptake of hippocampal serotonin. EurJ Neurosci. 11(1) 1-9. 

As mentioned above, a key factor in excluding a role for three out of the four recognised adenosine receptor subtypes was that the subtype selective agonists, CPA (Aj), CGS 21680 (A2A) and 2-CI-IB-MECA (A3), unlike the non-selective agonists,... 

Hinschen AK, Rose Meyer RB, Headrick JP (2003) Adenosine receptor subtypes mediating coronary vasodilatation in rat hearts. J Cardiovasc Pharmacol 41 73-80 Holgate ST (2005) The identification of the adenosine A2B receptor as a novel therapeutic target in asthma. Br J Pharmacol 145 1009-1015... 

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 )...

Salvatore et al. 1993). While the existence of the A2B adenosine receptor was anticipated from pharmacological data much earlier (Bruns 1980), the A3 subtype turned out to be an entirely new adenosine receptor which was initially identified as an orphan receptor in rat testis (Meyerhof et al. 1991). Later it was cloned from various tissue and species (Zhou et al. 1992 Salvatore et al. 1993 Linden et al. 1993 Hill et al. 1997). Expression in cellular systems revealed the unique pharmacological characteristics and species differences of the A3 adenosine receptor. For details about adenosine receptor subtypes see Fredholm et al. 2001a. 

Table 3.1 Sequence identities (%) between human adenosine receptor subtypes. Data are taken from the GPCRDB All against all pairwise identity matrix (http //www.gpcr.org/7tm old/seq/001/ 001.PCTID.html)...

Both the generation of mice overexpressing A3 adenosine receptors and targeted deletion of the A3 receptor gene have added important knowledge to the understanding of various functions of this adenosine receptor subtype. In particular its role in cardiovascular function was confirmed in numerous studies with genetically modified animals. 

Avila MY, Stone RA, Civan MM (2002) Knockout of A3 adenosine receptors reduces mouse intraocular pressure. Invest Ophthalmol Vis Sci 43 3021-26 Baraldi PG, Cacciari B, Borea PA, Varani K, Pastorin G, Da Ros T, Spalluto G (2002a) Pyrazolo-triazolo-pyrimidine derivatives as adenosine receptor antagonists a possible template for adenosine receptor subtypes Curr Pharm Des 8 99-110... 

Me Olah, Stiles GL (1995) Adenosine receptor subtypes characterization and therapeutic regulation. Annu Rev Pharmacol Toxicol 35 581-606 Ongini E, Dionisotti S, Gessi S, Irenius E, Fredholm BB (1999) Comparison of CGS 15943, ZM 241385 and SCH 58261 as antagonists at human adenosine receptors. Naunyn Schmiedebergs Arch Pharmacol 359 7-10... 

Okada M, Kawata Y, Kiryu K, Mizuno K, Wada K, Tasaki H, Kaneko S (1997) Effects of adenosine receptor subtypes on hippocampal extracellular serotonin level and serotonin reuptake activity. J Neurochem 69(6) 2581-2588... 

Yoon MH, Bae HB, Choi JI (2005) Antinociception of intrathecal adenosine receptor subtype agonists in rat formalin test. Anesth Analg 101 (5) 1417—1421... 

Auchampach JA, Bolli R (1999) Adenosine receptor subtypes in the heart Therapeutic opportunities and challenges. Am J Physiol 276 3 Pt 2 H1113-H1116... 

Gan XT, Rajapurohitam V, Haist JV, Chidiac P, Cook MA, Karmazyn M (2005) Inhibition of phenylephrine-induced cardiomyocyte hypertrophy by activation of multiple adenosine receptor subtypes. J Pharmacol Exp Ther 312(1) 27—34 Gardner NM, Yates L, Broadley KJ (2004) Effects of endogenous adenosine and adenosine receptor agonists on hypoxia-induced myocardial stunning in guinea-pig atria and papillary muscles. J Cardiovasc Pharmacol 43(3) 358-368... 

Rose Meyer RB, Hope W (1990) Evidence that A2 purinoceptors are involved in endothelium-dependent relaxation of the rat thoracic aorta. Br J Pharmacol 100(3) 576-580 Rubio R, Ceballos G (2003) Sole activation of three luminal adenosine receptor subtypes in different parts of coronary vasculature. Am J Physiol 284(1) H204-H214 Safran N, Shneyvays V, Balas N, Jacobson KA, Nawrath H, Shainberg A (2001) Cardioprotective effects of adenosine A3 and A3 receptor activation during hypoxia in isolated rat cardiac myocytes. Mol Cell Biochem 217(1-2) 143-152 Salvatore CA, Tilley SL, Latour AM, Fletcher DS, Roller BH, Jacobson MA (2000) Disruption of the A3 adenosine receptor gene in mice and its effect on stimulated inflammatory cells. J Biol Chem 275(6) 4429-4434... 

The accumulation of evidence implicating a role for adenosine in the pathogenesis of airway inflammation has led to investigations into all adenosine receptor subtypes as potential therapeutic targets for the treatment of asthma and COPD. To this end, the efficacy of A3AR in the clinical setting has been inconclusive. However, inhibition of Aj and A2B receptors and/or activation of the A2A pathway may serve as an alternative therapeutic approach (Brown et al. 2008b). 

Other Adenosine Receptor Subtypes Involved in Lung Reperfusion Injury... 

Collis MG, Hourani SM (1993) Adenosine receptor subtypes. Trends Pharmacol Sci 14(10) 360-366... 

Feoktistov I, Biaggioni I (1998) Pharmacological characterization of adenosine A2B receptors studies in human mast cells coexpressing A2A and A2B adenosine receptor subtypes. Biochem Pharmacol 55(5) 627-633... 

Polosa R (2002) Adenosine-receptor subtypes their relevance to adenosine-mediated responses in asthma and chronic obstructive pulmonary disease. Eur Respir 1 20(2) 488-496... 

The presence and functional roles of other adenosine receptor subtypes... 

---