title: [3H]-MRE 2029-F20, a selective antagonist radioligand for the human A2B adenosine receptors.
abstract: MRE 2029-F20 [N-benzo[1,3]dioxol-5-yl-2-[5-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-1-methyl-1H-pyrazol-3-yloxy]-acetamide] is a selective antagonist ligand of A2B adenosine receptors. For use as a radioligand, 1,3-diallyl-xanthine, the precursor of [3H]-MRE 2029-F20, was synthesized, and tritiated on the allyl groups. [3H]-MRE 2029-F20 bound to human A2B receptors expressed in CHO cells showed a KD value of 1.65+/-0.10 nM and Bmax value of 36+/-4 fmol/mg protein. [3H]-MRE2029-F20 represents a useful tool for the pharmacological characterization of human A2B adenosine receptor subtype.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Ferrara, 44100 Ferrara, Italy.
authors.forename: Pier Giovanni
authors.initials: PG
authors.lastname: Baraldi
authors.forename: Mojgan Aghazadeh
authors.initials: MA
authors.lastname: Tabrizi
authors.forename: Delia
authors.initials: D
authors.lastname: Preti
authors.forename: Andrea
authors.initials: A
authors.lastname: Bovero
authors.forename: Francesca
authors.initials: F
authors.lastname: Fruttarolo
authors.forename: Romeo
authors.initials: R
authors.lastname: Romagnoli
authors.forename: Allan R
authors.initials: AR
authors.lastname: Moorman
authors.forename: Stefania
authors.initials: S
authors.lastname: Gessi
authors.forename: Stefania
authors.initials: S
authors.lastname: Merighi
authors.forename: Katia
authors.initials: K
authors.lastname: Varani
authors.forename: Pier Andrea
authors.initials: PA
authors.lastname: Borea
mesh_terms: D000081:Acetamides / Q000138:chemical synthesis* / Q000494:pharmacology; D058917:Adenosine A2 Receptor Antagonists; D000498:Allyl Compounds / Q000737:chemistry; D000818:Animals; D016227:Benzoquinones / Q000737:chemistry; D001667:Binding, Competitive; D016466:CHO Cells; D006224:Cricetinae; D006801:Humans; D011687:Purines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011869:Radioligand Assay; D043704:Receptor, Adenosine A2B / Q000378:metabolism; D014316:Tritium / Q000737:chemistry; D019820:Xanthine / Q000737:chemistry
chemical_list: D000081:Acetamides; D058917:Adenosine A2 Receptor Antagonists; D000498:Allyl Compounds; D016227:Benzoquinones; C495752:N-benzo(1,3)dioxol-5-yl-2-(5-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-1-methyl-1H-pyrazol-3-yloxy)-acetamide; D011687:Purines; D011720:Pyrazoles; D043704:Receptor, Adenosine A2B; D014316:Tritium; D019820:Xanthine