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 1.650.10 nM and Bmax value of 364 fmol/mg protein. [3H]-MRE2029-F20 represents a useful tool for the pharmacol. characterization of human A2B adenosine receptor subtype
[H-3]-MRE 2029-F20, a selective antagonist radioligand for the human A(2B) adenosine receptors
BARALDI, Pier Giovanni;AGHAZADEH TABRIZI, Mojgan;PRETI, Delia;BOVERO, Andrea;FRUTTAROLO, Francesca;ROMAGNOLI, Romeo;GESSI, Stefania;MERIGHI, Stefania;VARANI, Katia;BOREA, Pier Andrea
2004
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 1.650.10 nM and Bmax value of 364 fmol/mg protein. [3H]-MRE2029-F20 represents a useful tool for the pharmacol. characterization of human A2B adenosine receptor subtypeFile in questo prodotto:
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