Characterization of human A2A adenosine receptors with the antagonist radioligand [3H]-SCH 58261

British Journal of Pharmacology
S DionisottiB B Fredholm

Abstract

1. We have characterized the binding of the new potent and selective antagonist radioligand [3H]-5-amino-7-(2-phenylethyl)-2-(2-furyl)-pyrazolo[4,3-e]-1,2,4-triazol o[1,5- c]pyrimidine, [3H]-SCH 58261, to human cloned A2A adenosine receptors. 2. In Chinese hamster ovary (CHO) cells transfected with the human cloned A2A receptor, [3H]-SCH 58261 specific binding (about 70%) was rapid, saturable, reversible and proportional to protein concentration. The kinetic KD value was 0.75 nM. Saturation experiments showed that [3H]-SCH 58261 labelled a single class of recognition sites with high affinity (KD = 2.3 nM) and limited capacity (apparent Bmax = 526 fmol mg-1 protein). 3. Competition experiments revealed that binding of 0.5 nM [3H]-SCH 58261 was displaced by adenosine receptor agonists with the following order of potency: 2-hexynyl-5'-N-ethylcarboxamidoadenosine (2HE-NECA) > 5'-N-ethylcarboxamidoadenosine (NECA) = 2-phenylaminoadenosine (CV 1808) > 2-[4-(2-carboxyethyl)-phenethylamino]-5'-N-ethylcarboxamidoadenosi ne (CGS 21680) > R-N6-phenylisopropyladenosine (R-PIA) > or = N6-cyclohexyladenosine (CHA) > S-N6-phenylisopropyladenosine (S-PIA). 4. Adenosine receptor antagonists inhibited [3H]-SCH 58261 binding with the following or...Continue Reading

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Citations

Feb 21, 2007·Naunyn-Schmiedeberg's Archives of Pharmacology·Ming YangJohn C Shryock
May 30, 1998·British Journal of Pharmacology·K VaraniP A Borea
Feb 29, 2000·British Journal of Pharmacology·S GessiP A Borea
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Jul 1, 2009·Molecular and Cellular Biology·Antonietta Rosella FarinaAndrew Reay Mackay
Sep 24, 2004·The International Journal of Biochemistry & Cell Biology·M WengertC Caruso-Neves
Jul 5, 2006·Journal of Receptor and Signal Transduction Research·Vipa Ravyn, J Robert Bostwick
Jun 25, 2005·Arteriosclerosis, Thrombosis, and Vascular Biology·George HsiaoJoen R Sheu
Feb 13, 2014·British Journal of Pharmacology·Stephen P H AlexanderUNKNOWN CGTP Collaborators
May 13, 2018·Purinergic Signalling·Sonja HinzChrista E Müller
Apr 12, 2011·Reviews in the Neurosciences·Shuang-Shuang Dai, Yuan-Guo Zhou
May 14, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Yuri ParkYoung G Shin
Dec 15, 2020·Purinergic Signalling·Xue YangDaan van der Es

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