[3H]-MRE 2029-F20, a selective antagonist radioligand for the human A2B adenosine receptors.
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.
Baraldi
Pier Giovanni
PG
Dipartimento di Scienze Farmaceutiche, Università di Ferrara, 44100 Ferrara, Italy.
Tabrizi
Mojgan Aghazadeh
MA
Preti
Delia
D
Bovero
Andrea
A
Fruttarolo
Francesca
F
Romagnoli
Romeo
R
Moorman
Allan R
AR
Gessi
Stefania
S
Merighi
Stefania
S
Varani
Katia
K
Borea
Pier Andrea
PA
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
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