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 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 1.650.10 nM and Bmax value of 364 fmol/mg protein. [3H]-MRE2029-F20 represents a useful tool for the pharmacol. characterization of human A2B adenosine receptor subtype
Baraldi, Pier Giovanni; AGHAZADEH TABRIZI, Mojgan; Preti, Delia; Bovero, Andrea; Fruttarolo, Francesca; Romagnoli, Romeo; Moorman, Ar; Gessi, Stefania; Merighi, Stefania; Varani, Katia; Borea, Pier Andrea
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/516836
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