Adenosine receptor agonists, and

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

In a search for more potent and selective Ai adenosine receptor agonists, and taking in mind that at Ai receptor the most active analogues were substituted adenosines, a series of N -cycloalkyl-1-deazaadenosine derivatives were synthesized and evaluated in radioligand binding studies and adenylate cyclase assays [13]. N -Cyclopentyl-2-chloro-1-deazaadenosine (1-deazaCCPA) showed the highest affinity at Ai receptor with more than two fold higher Ai selectivity than N -cyclopentyladenosine (CPA). 

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

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]. 

Sawynok J. (1995). Pharmacological rationale for the clinical use of caffeine. Drugs. 49(1) 37-50. Sawynok J. (1998). Adenosine receptor activation and nociception. Eur J Pharmacol. 347(1) 1-11. Schlaepfer TE, Strain EC, Greenberg BD, Preston KL, Lancaster E, Bigelow GE, Barta PE, Pearlson GD. (1998). Site of opioid action in the human brain mu and kappa agonists subjective and cerebral blood flow effects. Am J Psychiatry. 155(4) 470-73. 

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... 

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... 

A3 Adenosine Receptor Agonists History and Future Perspectives... 

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