Abstract
This study demonstrates quantification of A2A adenosine receptors (A2AAdoRs) in membranes prepared from porcine coronary arteries, porcine striatum, and PC12 cells. Radioligand binding assays were performed using the new selective A2AAdoR antagonist radioligand [3H]-5-amino-7-(2-phenylethyl)-2-(2-furyl)-pyrazolo [4,3-epsilon]-1,2,4-triazolo[1,5-c)pyrimidine ([3H]SCH58261). Binding of the radioligand to membranes was rapid, reversible, and saturable. The densities of A2AAdoRs in membranes prepared from porcine coronary arteries, porcine striatum, and PC12 cells were 900 +/- 61, 892 +/- 35, and 959 +/- 76 fmol/mg protein, respectively. Equilibrium dissociation constants (Kd values) calculated from results of saturation binding assays were 2.19, 1.20, and 0.81 nmol/L, and Kd values calculated from results of association and dissociation assays were 2.42, 1.01, and 0.40 nmol/L for [3H]SCH58261 binding to membranes prepared from porcine coronary arteries, porcine striatum, and PC12 cells, respectively. The specific binding of [3H]SCH58261 as a percentage of total binding at a radioligand concentration equal to the Kd value was 65% to 90% in the three membrane preparations. The order of ligand potencies determined by assay of competi...Continue Reading
References
Jan 1, 1992·Journal of Receptor Research·X D JiK A Jacobson
Jul 1, 1990·Physiological Reviews·R A Olsson, J D Pearson
Apr 21, 1986·FEBS Letters·D UkenaJ W Daly
Feb 1, 1987·Journal of Neurochemistry·M WilliamsL Noronha-Blob
Dec 1, 1973·Biochemical Pharmacology·Y Cheng, W H Prusoff
May 17, 1994·European Journal of Pharmacology·H NonakaH Kase
Apr 1, 1996·British Journal of Pharmacology·C ZocchiS Dionisotti
Citations
Jul 3, 2013·Naunyn-Schmiedeberg's Archives of Pharmacology·Mayumi SakiTomoyuki Kanda
Jan 27, 1999·Biochemical Pharmacology·B KullB B Fredholm
Oct 17, 1998·European Journal of Pharmacology·J W PhillisM H O'Regan
Nov 19, 1997·Neuropharmacology·G ArslanB B Fredholm
Dec 1, 2001·Pharmacology & Therapeutics·R Tabrizchi, S Bedi
Dec 28, 1999·Brain Research. Brain Research Reviews·J L Moreau, G Huber
Jul 29, 1998·Bioorganic & Medicinal Chemistry·S A Poulsen, R J Quinn
Oct 30, 2013·Journal of Medicinal Chemistry·Manuel de Lera RuizJunying Zheng
Jun 18, 1999·British Journal of Pharmacology·B K Kemp, T M Cocks
Feb 29, 2000·British Journal of Pharmacology·S GessiP A Borea
Jul 6, 2000·British Journal of Pharmacology·K S ErgaL Belardinelli
Apr 27, 2002·British Journal of Pharmacology·Katia VaraniPier Andrea Borea
Mar 21, 1998·Journal of Veterinary Pharmacology and Therapeutics·J Elliott, F E Brady
Mar 5, 2013·Archives of Pharmacal Research·Rudolf GesztelyiArpad Tosaki
Oct 6, 1997·British Journal of Pharmacology·K VaraniP A Borea
May 30, 1998·British Journal of Pharmacology·K VaraniP A Borea
Jun 1, 1997·British Journal of Pharmacology·S DionisottiB B Fredholm
Jun 24, 2009·European Journal of Pharmacology·Wiebke SihverMarcus H Holschbach
Aug 13, 2015·Human Molecular Genetics·Feng-Lan ChiuHung-Chih Kuo
Feb 26, 2000·Anesthesiology·C N SeubertD M Dennis
Aug 28, 2012·The Journal of Pharmacology and Experimental Therapeutics·Stefano ToldoAntonio Abbate
Feb 15, 2000·Journal of Cardiovascular Pharmacology·A Z Arif HasanS J Mustafa
Jul 1, 1999·Clinical and Experimental Pharmacology & Physiology·M J Lew, S W Kao
Nov 25, 1997·Annals of the New York Academy of Sciences·E OnginiR Bertorelli
Oct 7, 1998·Neurochemistry International·B CostaC Martini
Mar 27, 1998·Biochemical Pharmacology·I Feoktistov, I Biaggioni