Pharmacological and biochemical characterization of purified A2a adenosine receptors in human platelet membranes by [3H]-CGS 21680 binding

British Journal of Pharmacology

Volumn 117, Issue 8, 1996, Pages 1693-1701

  Varani, Katia ^a   Gessi, Stefania ^a   Dalpiaz, Alessandro ^a   Borea, Pier Andrea ^a  

^a UNIVERSITY OF FERRARA   (Italy)

Author keywords

Cyclic AMP assays; Human platelet membranes; Purified A2a adenosine receptors; Thermodynamic analysis; 3H CGS 21680 binding

Indexed keywords

2 [4 (2 CARBOXYETHYL)PHENETHYLAMINO]ADENOSINE 5' (N ETHYLCARBOXAMIDE); 3 [(3 CHOLAMIDOPROPYL)DIMETHYLAMMONIO] 1 PROPANESULFONIC ACID; ADENOSINE A2 RECEPTOR; ADENOTIN; ADENYLATE CYCLASE; RADIOLIGAND;

ARTICLE; DRUG POTENCY; HUMAN; HUMAN CELL; NORMAL HUMAN; PRIORITY JOURNAL; RECEPTOR AFFINITY; THROMBOCYTE MEMBRANE;

ADENOSINE; BINDING, COMPETITIVE; BLOOD PLATELETS; CELL MEMBRANE; CYCLIC AMP; HUMANS; PHENETHYLAMINES; RECEPTORS, PURINERGIC P1;

EID: 0029987991     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1476-5381.1996.tb15341.x     Document Type: Article

References (41)

1. 2a receptor ligands. Biochem. Pharmacol., 49, 461-469.
2. BRADFORD, M.M. (1976). A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein dye-binding. Anal. Biochem., 72, 248.
3. BROWN, B.L., ALBANO, J.D.M., EKINS, R.I. & SGHERZI, A.M. (1971). A simple and sensitive saturation assay method for the measurement of adenosine 3′ : 5′-cyclic monophosphate. Biochem. J., 121, 561-562.
4. BRUNS, R.F., LAWSON-WENDING, K. & PUGSLEY, T.A. (1983). A rapid filtration assay for soluble receptors using polyethylemine-treated filters. Anal. Biochem., 132, 74-81.
5. 3H] NECA in rat striatal membranes. Mol. Pharmacol., 29, 331-346.
6. 1 adenosine receptors. J. Pharmacol. Exp. Ther., 266, 1463-1474.
7. 50) of an enzymatic reaction. Biochem. Pharmacol., 22, 3099-3108.
8. COOPER, J.A., HILL, S.J., ALEXANDER, S.P.H., RUBIN, P.C. & HORN, E.H. (1995). Adenosine receptor-induced cyclic AMP generation and inhibition of 5-hydroxytryptamine release in human platelets. Br. J. Pharmacol., 40, 43-50.
9. CRISTALLI, G., VITTORI, S., THOMPSON, R.D., PADGETT, W.L., SHI, D., DALY, J.W. & OLSSON, R.A. (1994a). Inhibition of platelet aggregation by adenosine receptor agonists. Naunyn. Schmied. Arch. Pharmacol., 349, 644-650.
10. 2 adenosine receptor agonist with potent inhibitory activity on platelet aggregation. J. Med. Chem., 37, 1720-1726.
11. 2 adenosine receptor antagonist 8FB-PTP, an 8 substituted pyrazolo-triazolo-pyrimidine, on in vitro functional models. Br. J. Pharmacol., 112, 659-665.
12. DIONISOTTI, S., ZOCCHI, C., VARANI, K., BOREA, P.A. & ONGINI, E. (1992). Effects of adenosine derivatives on human and rabbit platelet aggregation. Naunyn. Schmied. Arch. Pharmacol., 346, 673-676.
13. FEIN, T., SCHULZE, E., BAR, J. & SCHWABE, U. (1994). Purification and characterization of an adenotin-like adenosine binding protein from human platelets. Naunyn. Schmied. Arch Pharmacol., 349, 374-380.
14. FINNEY, D.J. (1978). Statistical Methods in Biological Assay. pp. 80-82. London: Griffin & Co..
15. FREDHOLM, B.B., ABBRACCHIO, M.P., BURNSTOK G, DALY, J.W., HARDEN, T.K., JACOBSON, K.A., LEFF, P. & WILLIAMS, M. (1994). Nomenclature and classification of purinoceptors. Pharmacol. Rev., 46, 143-156.
16. 2 receptor interaction in the striatum as a basis for adenosine/dopamine interactions in the central nervous system. Drug Dev. Res., 28, 374-380.
17. 2 receptor antagonist, reduces cerebral ischemic injury in the Mongolian gerbil. Life Sci., 55, 61-65.
18. GILLI, P., FERRETTI, V., GILLI, G. & BOREA, P.A. (1994). Enthalpyentropy compensation in drug-receptor binding. J. Phys. Chem., 98, 1515-1518.
19. HUTCHISON, K.A., NERVIS, B., PERINI, F. & FOX, I.H. (1990). Soluble and membrane-associated human low-affinity adenotin binding protein (adenotin)l: properties and homology with mammalian and avian stress proteins. Biochemistry, 29, 5138-5144.
20. 3H] adenosine binding in relation to adenylate cyclase activity. Naunyn. Schmied. Arch. Pharmacol., 325, 226-233.
21. 2-adenosine antagonists in vitro and in vivo. FEBS Lett., 323, 141-144.
22. 2 receptors in rat brain. J. Pharmacol. Exp. Ther., 251, 888-893.
23. 2 receptor. Biochem. Pharmacol., 21, 3827-3833.
24. KORTH, R., NUNEZ, D., BIDAULT, J. & BENVENISTE, J. (1988). Comparison of three paf-acether receptor antagonist ginkgolides. Eur. J. Pharmacol., 152, 101-110.
25. LINDEN, J., JACOBSON, M.A., HUTCHINS, C. & WILLIAMS, M. (1994). Adenosine receptors. In Handbook of Receptors and Channels. ed. Peroutka, S.J. Vol 1, pp.29-44. Boca Raton, FL: CRC Press.
26. 3H] NECA binding sites by gel filtration. Naunyn Schmied. Arch. Pharmacol., 337, 64-68.
27. LORENZEN, A., GRUN, S., VOGT, H. & SCHWABE, U. (1992). Identification of a novel high affinity adenosine binding protein from bovine striatum. Naunyn Schmied. Arch. Pharmacol., 346, 63-68.
28. 2a adenosine receptor agonist CGS 21680C in conscious normotensive rats. Br. J. Pharmacol., 114, 761-768.
29. MUNSON, P.J. & RODBARD, D. (1980). Ligand: a versatile computerized approach for the characterization of ligand binding systems. Anal. Biochem., 107, 220-239.
30. NAKATA, H. & FUJISAWA, H. (1988). Adenosine binding sites of rat pheochromocytoma PC 12 cell membranes: partial characterizations and solubilization. J. Biochem., 104, 457-460.
31. NORDSTEDT, C. & FREDHOLM, M.M. (1990). A modification of a protein-binding method for rapid quantification of cAMP in cell culture supernatants and body fluids. Anal. Biochem., 189, 231-234.
32. 2a receptor antagonists. In Adenosine and adenine nucleotides: from molecular biology to integrative physiology. ed. Belardinelli L, & Pelleg, A. pp.241-248. Boston, U.S.A.: Kluwer Academic Publishers.
33. OSBORNE, J.P., PALUMBO, G., BREWER, H.B. & EDELHOCH, H. (1976). The thermodynamics of the self-association of the reduced and carboxymethylated form of Apo A-II from the human high density lipoprotein complex. Biochemistry, 15, 317-320.
34. 3H] UK-14,304: regulation by Gpp(NH)p and cations. Naunyn Schmied. Arch. Pharmacol., 336, 48-59.
35. SCHWABE, U., FEIN, T. & LORENZEN, A. (1993). Pharmacological properties of adenosine receptors and adenosine binding properties. Drug Dev. Res., 28, 220-225.
36. VAN CALKER, D., MULLER, M. & HAMPRECHT, B. (1979). Adenosine regulates via two different types of receptors the accumulation of cyclic AMP in cultured brain cells. J. Neurochem., 33, 999-1005.
37. 3H] CGS21680 to human platelet membranes. Biochem. Pharmacol., 48, 1658-1661.
38. 2 receptor agonist. Cardiovasc. Drug Rev., 10, 26-53.
39. 3H]-5′-N-ethylcarboxamidoadenosine binds to both Ra and Ri adenosine receptors in rat striatum. Naunyn Schmied. Arch. Pharmacol., 325, 218-222.
40. 2a adenosine receptor antagonist. J. Pharmacol. Exp. Ther., (in press).
41. 2-like binding protein. Mol. Pharmacol., 37, 554-559.