Binding of adenosine receptor ligands to brain of adenosine receptor knock-out mice: evidence that CGS 21680 binds to A1 receptors in hippocampus

Naunyn-Schmiedeberg's Archives of Pharmacology
L HalldnerB B Fredholm

Abstract

The adenosine receptor agonist 2-[ p-(2-carboxyethyl)phenylethylamino]-5'- N-ethylcarboxamidoadenosine (CGS 21680) is generally considered to be a selective adenosine A(2A) receptor ligand. However, the compound has previously been shown to exhibit binding characteristics that are not compatible with adenosine A(2A) receptor binding, at least in brain regions other than the striatum. We have examined binding of [(3)H]CGS 21680 and of antagonist radioligands with high selectivity for adenosine A(1) or A(2A) receptors to hippocampus and striatum of mice lacking either adenosine A(1) (A1R((-/-))) or A(2A) (A2AR((-/-))) receptors. Both receptor autoradiography and membrane binding techniques were used for this purpose and gave similar results. There were no significant changes in the binding of the A(1) receptor antagonist [(3)H]DPCPX in mice lacking A(2A) receptors, or in the binding of the A(2A) receptor antagonists [(3)H]SCH 58261 and [(3)H]ZM 241385 in mice lacking A(1) receptors. Furthermore, [(3)H]CGS 21680 binding in striatum was abolished in the A2AR((-/-)), and essentially unaffected in striatum from mice lacking A(1) receptors. In hippocampus, however, binding of [(3)H]CGS 21680 remained in the A2AR((-/-)), whereas bindin...Continue Reading

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Citations

Feb 21, 2007·Naunyn-Schmiedeberg's Archives of Pharmacology·Ming YangJohn C Shryock
Jul 31, 2009·Psychopharmacology·Ryan K Bachtell, David W Self
Sep 5, 2008·The Journal of Neuroscience : the Official Journal of the Society for Neuroscience·Susana MingoteJohn D Salamone
Nov 28, 2006·European Journal of Pharmacology·Timo RiegVolker Vallon
Sep 18, 2007·Biochemical Pharmacology·Stina M JohanssonAbram Katz
Jul 16, 2011·European Journal of Pharmacology·Daniela ImpellizzeriSalvatore Cuzzocrea
Aug 6, 2011·The International Journal of Neuropsychopharmacology·Robyn M BrownAndrew J Lawrence
Sep 7, 2005·American Journal of Physiology. Heart and Circulatory Physiology·Eugene I TikhJames G Dobson
Apr 12, 2005·Annual Review of Pharmacology and Toxicology·Bertil B FredholmJean-Marie Vaugeois
May 29, 2018·The Journal of Headache and Pain·Kristian A HaanesAntoinette MaassenVanDenBrink

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