Novel selective antagonist radioligands for the pharmacological study of A(2B) adenosine receptors.
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]triazin-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-purin-8-yl)-phenoxy]acetamide ([(3)H]MRS 1754), N-(2-(2-Phenyl-6-[4-(2,2,3,3-tetratritrio-3-phenylpropyl)-piperazine-1-carbonyl]-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.
Gessi
Stefania
S
Department of Clinical and Experimental Medicine, Pharmacology Unit and "Interdisciplinary Center for the Study of Inflammation (ICSI),", Ferrara, Italy.
Varani
Katia
K
Merighi
Stefania
S
Leung
Edward
E
Mac Lennan
Stephen
S
Baraldi
Pier Giovanni
PG
Borea
Pier Andrea
PA