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Gessi S, Varani K, Merighi S, Leung E, Mac Lennan S, Baraldi PG, Borea PA: Novel selective antagonist radioligands for the pharmacological study of A (2B) adenosine receptors. Purinergic Signal. 2006 Nov;2(4):583-8. Epub 2006 Jul 8.
The adenosine A (2B) receptor is the least well characterized of the four adenosine subtypes due to the lack of potent and selective agonists and antagonists. Despite the widespread distribution of A (2B) receptor mRNA, little information is available with regard to their function. The characterization of A (2B) receptors, through radioligand binding studies, has been performed, until now, by using low-affinity and non-selective antagonists like 1,3-dipropyl-8-cyclopentylxanthine ([(3) H] DPCPX),(4-(2-[7-amino-2-(2-furyl)-[1,2,4] triazolo-[2,3-a][1,3,5] tri azin-5-ylamino] ethyl)-phenol ([(3) H] ZM 241385) and 3-(3,4-aminobenzyl)-8-(4-oxyacetate) phenyl-1-propyl-xanthine ([(125) I] ABOPX). Recently, high-affinity radioligands for A (2B) receptors, [N-(4-cyanophenyl)-2-[4-(2,3,6,7-tetrahydro-2,6-dioxo-1,3-dipropyl-1H-puri n-8-yl)-phenoxy] acetamide ([(3) H] MRS 1754), N-(2-(2-Phenyl-6-[4-(2,2,3,3-tetratritrio-3-phenylpropyl)-piperazine-1-car bonyl]-7H-pyrrolo [2,3-d] pyrimidin-4-ylamino)-ethyl)-acetamide ([(3) H] OSIP339391) and N-benzo [1,3] dioxol-5-yl-2-[5-(1,3-dipropyl-2,6-dioxo-2,3,6,7-tetrahydro-1H -purin-8-yl)-1-methyl-1H-pyrazol-3-yloxy]-acetamide] ([(3) H] MRE 2029F20), have been introduced. This minireview offers an overview of these recently developed radioligands and the most important applications of drugs towards A (2B) receptors. |
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