Adenosine receptor agonist

FIGURE 4.18 Affinity of adenosine receptor agonists in whole cells (dark bars) and membranes (cross-hatched bars, high-affinity binding site). Data shown for (1) 2-phenylaminoadenosine, (2) 2-chloro adenosine, (3) 5 -N-ethylcarboxamidoadenosine, (4) N6-cyclohexyladenosine, (5) (-)-(R)-N6-phenylisopropyladenosine, and (6) N6-cyclopentyladenosine. Data redrawn from [15],... 

FIGURE 9.14 Effects of adenosine receptor agonist 2-chloro-adenosine on vascular perfusion pressure of isolated perfused rat kidneys. Minor effects seen in untreated kidneys (filled circles) and pronounced vasoconstriction while vasodilatation in kidneys coperfused with subthreshold concentrations of a-adrenoceptor vasoconstrictor methoxamine and vasodilatatory activation of adenylyl cyclase with forskolin (open circles). Redrawn from [49]. 

Abscissae, 254f Absolute stoichiometry, 180 Adenosine receptor agonists, 70 Adenylate cyclase, 23, 25f 62-Adrenoceptor antagonists, 4 6-Adrenoceptors, 82 Adsorption process... 

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

Fig. 1.1 Interaction between allergen and adenosine receptor agonists with respect to histamine release from guinea-pig chopped lung (left) or bronchoconstriction in the guinea pig in vivo (right). Tissues and animals were passively sensitized to ovalbumin. In the histamine release assay, a threshold response to allergen is augmented concentration-dependently by NECA. In the whole animal, a single intravenous injection of APNEA markedly enhances the bronchoconstrictor response to allergen (J.R. Fozard and H.J. Pfannkuche, unpublished observations 1994)...

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... 

Ochaion A, Bar-Yehuda S, Cohen S, Amital H, Jacobson KA, Joshi BV, Gao ZG, Barer F, Patoka R, Del Valle L, Perez-Liz G, Fishman P (2008) The A3 adenosine receptor agonist CF502 inhibits the PI3K, PKB/Akt and NF-kappaB signaling pathway in synoviocytes from rheumatoid arthritis patients and in adjuvant-induced arthritis rats. Biochem Pharmacol... 

Wan TC, Ge ZD, Tampo A, Mio Y, Bienengraeber MW, Tracey WR, Gross GJ, Kwok WM, Auchampach JA (2008) The A3 adenosine receptor agonist CP-532, 903 [N6-(2, 5-dichlorobenzyl)-3 -aminoadenosine-5 -N-methylcarboxamide] protects against myocardial ischemia/reperfusion injury via the sarcolemmal ATP-sensitive potassium channel. J Pharmacol Exp Ther 324(l) 234-243... 

A3 Adenosine Receptor Agonists History and Future Perspectives... 

Auchampach JA, Ge ZD, Wan TC, Moore J, Gross GJ (2003) A3 adenosine receptor agonist IB-MECA reduces myocardial ischemia-reperfusion injury in dogs. Am J Physiol-Heart Circ Physiol 285(2) H607-613... 

Bar-Yehuda S, Stemmer SM, Madi L, Castel D, Ochaion A, Cohen S, Barer F, Zabutti A, Perez-Liz G, Del Valle L, Fishman P (2008) The A, adenosine receptor agonist CF102 induces apoptosis of hepatocellular carcinoma via de-regulation of the Wnt and NF-kappaB signal transduction pathways. Int J Oncol 33(2) 287-295... 

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... 

Jacobson KA, von Lubitz DKJE, Daly JW, Fredholm BB (1996) Adenosine receptor ligands differences with acute and chronic treatment. Trends Pharmacol Sci 17(3) 108-113 Jacobson KA, Ji X-D, Li AH, Melman N, Siddiqui MA, Shin KJ, Marquez VE, Ravi RG (2000) Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists. J Med Chem 43(ll) 2196-2203... 

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