[3H]-SCH 58261 labelling of functional A(2A) adenosine receptors in human neutrophil membranes

British Journal of Pharmacology

Volumn 123, Issue 8, 1998, Pages 1723-1731

  Varani, Katia ^a   Gessi, Stefania ^a   Dionisotti, Silvio ^b   Ongini, Ennio ^b   Borea, Pier Andrea ^a  

^a UNIVERSITY OF FERRARA   (Italy)

^b Schering Plough Research Institute   (Italy)

Author keywords

3H SCH 58261 binding; Adenosine A(2A) receptor ligands; Adenosine A(2A) receptors; Cyclic AMP assays; Human neutrophil membranes; Superoxide anion production; Thermodynamic analysis

Indexed keywords

5 AMINO 2 (2 FURYL) 7 (2 PHENYLETHYL)PYRAZOLO[4,3 E][1,2,4]TRIAZOLO[1,5 C]PYRIMIDINE; ADENOSINE A2A RECEPTOR; ADENOSINE RECEPTOR BLOCKING AGENT; ADENOSINE RECEPTOR STIMULATING AGENT; ADENYLATE CYCLASE; CYCLIC AMP; SUPEROXIDE; ADENOSINE 5' (N ETHYLCARBOXAMIDE); ADENOSINE RECEPTOR; FORMYLMETHIONYLLEUCYLPHENYLALANINE; PYRIMIDINE DERIVATIVE; TRIAZOLE DERIVATIVE;

ARTICLE; BINDING SITE; CELL MEMBRANE; CONTROLLED STUDY; CORPUS STRIATUM; DRUG POTENCY; ENTHALPY; ENTROPY; HUMAN; HUMAN CELL; ISOTOPE LABELING; NEUTROPHIL; NORMAL HUMAN; PRIORITY JOURNAL; RECEPTOR AFFINITY; RECEPTOR BINDING; THERMODYNAMICS; DRUG ANTAGONISM; DRUG EFFECT; DRUG POTENTIATION; IN VITRO STUDY; KINETICS; METABOLISM;

ADENOSINE-5'-(N-ETHYLCARBOXAMIDE); CELL MEMBRANE; CYCLIC AMP; ENTROPY; HUMANS; KINETICS; N-FORMYLMETHIONINE LEUCYL-PHENYLALANINE; NEUTROPHILS; PYRIMIDINES; RECEPTORS, PURINERGIC P1; SUPEROXIDES; TRIAZOLES;

EID: 0031596853     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0701758     Document Type: Article

References (41)

1. 2A adenosine receptor antagonists. Bioorg. Med. Chem. Lett., 4, 2539-2544.
2. 3H]-SCH 58261 to coronary artery membranes. Circ. Res., 79, 1153-1160.
3. BONG, G.W., ROSENGREN, S. & FIRESTEIN, G.S. (1996). Spinal cord adenosine stimulation in rats inhibits peripheral neutrophil accumulation. The role of N-methyl-D-aspartate receptors. J. Clin. Invest., 12, 2779-2785.
4. 2A receptor ligands. Biochem. Pharmacol., 49, 461-469.
5. 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.
6. 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.
7. 2 receptors. Naunyn-Schmiedeberg's Arch. Pharmacol., 335, 64-69.
8. 50) of an enzymatic reaction. Biochem. Pharmacol., 22, 3099-3108.
9. CRONSTEIN, B.N. (1994). Adenosine, an endogenous anti-inflammatory agent. J. Appl. Physiol., 76, 5-13.
10. 2 generation, respectively. J. Clin. Invest., 85, 1150-1157.
11. CRONSTEIN, B.N., HAINES, K.A., KOLASINSKI, S. & REIBMAN, J. (1992). Occupancy of G alpha s-linked receptors uncouples chemoattractant receptors from their stimulus-transduction mechanisms in the neutrophil. Blood, 80, 1052-1057.
12. CRONSTEIN, B.N. & HIRSCHHORN, R. (1990). Adenosine and host defense. Modulation through metabolism and receptor-mediated mechanisms. In Adenosine and Adenosine Receptors. Ed. Williams, M. New Jersey: The Humana Press Inc.
13. 2 receptor on human neutrophils. J. Immunol., 135, 1366-1371.
14. 3H]-SCH 58261. J. Pharmacol Exp. Ther., 298, 726-732.
15. 3H]-SCH 58261. Br. J. Pharmacol., (in press).
16. FINNEY, D.J. (1978). Statistical Methods in Biological Assay. ed. Grin. pp. 80-82. London: Griffin & Co.
17. FREDHOLM, B.B., ABBRACCHIO, M.P., BURNSTOCK, 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.
18. 2A receptors mediate the inhibitory effect of adenosine on formyl-Met-Leu-Phe-stimulated respiratory burst in neutrophil leukocytes. Naunyn-Schmiedeberg's Arch. Pharmacol., 354, 262-267.
19. GILLI, P., FERRETTI, V., GILLI, G. & BOREA, P.A. (1994). Enthalpyentropy compensation in drug-receptor binding. J. Phys. Chem., 98, 1515-1518.
20. HUSSAIN, T. & MUSTAFA, S.J. (1993). Regulation of the adenosine receptor system in coronary artery: functional studies and cAMP. Am. J. Physiol., 33, H 441.
21. HUTCHISON, K.A., NERVIS, B., PERINI, F. & FOX, I.H. (1990). Soluble and membrane-associated human low-affinity adenotin binding protein (adenotin): properties and homology with mammalian and avian stress proteins. Biochemistry, 29, 5138-5144.
22. LIANG, B.T. (1992). Adenosine receptors and cardiovascular function. Trends Cardiovasc. Med., 2, 100.
23. 3H]-CGS 21680 in the rat brain. Naunyn-Schmiedeberg's Arch. Pharmacol., 354, 539-541.
24. 3H] NECA binding sites by gel nitration. Naunyn-Schmiedeberg's Arch. Pharmacol., 337, 64-68.
25. - production by human neutrophils. The preparation and assay of NADPH oxidase-containing particles from human neutrophils. Methods Enzymol., 105, 358-365.
26. MUNSON, P.J. & RODBARD, D. (1980). Ligand: a versatile computerized approach for the characterization of ligand binding systems. Anal. Biochem., 107, 220-239.
27. 2 adenosine receptor: guanine nulceotide modulation of agonist binding is enhanced by proteolysis. Mol. Pharmacol., 39, 130-135.
28. 2-adenosine receptor. J. Receptor Res., 13, 961-973.
29. 2 receptor antagonist, to rat brain membranes. Mol. Pharmacol., 46, 817-822.
30. 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.
31. OLAH, M.E. & STILES, G.L. (1995). Adenosine receptor subtypes: Characterization and Therapeutic Regulation. Ann. Rev. Pharmacol. Toxicol., 35, 581-588.
32. 2A receptors. Trends Pharmacol. Sci., 17, 364-372.
33. RUDOLPHI, K.A., SCHUBERT, P., PARKINSON, F.E. & FREDHOLM, B.B. (1992). Neuroprotective role of adenosine in cerebral ischemia. Trends Pharmacol. Sci., 13, 439-445.
34. SCATCHARD, G. (1949). The attractions of protein for small molecules and ions. Ann. New York Acad. Sci., 51, 660-672.
35. SCHRIER, D.J. & IMRE, K.M. (1986). The effects of adenosine on human neutrophil function. J. Immunol., 137, 3284-3288.
36. SPISANI, S., GIULIANI, A.L., CAVALLETTI, T., ZACCARINI, M., MILANI, L., GAVIOLI, R. & TRANIELLO, S. (1992). Effect of cyclic AMP level reduction on human neutrophil responses to formylated peptides. Inflammation, 16, 147-158.
37. 3H] CGS 21680 binding. Br. J. Pharmacol., 117, 1693-1701.
38. 3H] SCH 58261 binding. Br. J. Pharmacol., 122, 386-392.
39. ZHANG, Y. & FREDHOLM, B.B. (1994). Propentophylline enhancement of the actions of adenosine on neutrophil leukocytes. Biochem. Pharmacol., 48, 2025-2032.
40. 2A adenosine receptor antagonist. J. Pharmacol. Exp. Ther., 276, 398-404.
41. 2A adenosine receptor antagonist, to rat striatal membranes. Br. J. Pharmacol., 117, 1381-1386.