| Literature DB >> 15177484 |
Pier Giovanni Baraldi1, Mojgan Aghazadeh Tabrizi, Delia Preti, Andrea Bovero, Francesca Fruttarolo, Romeo Romagnoli, Allan R Moorman, Stefania Gessi, Stefania Merighi, Katia Varani, Pier Andrea Borea.
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.Entities:
Mesh：
Substances：
Year: 2004 PMID： 15177484 DOI： 10.1016/j.bmcl.2004.03.084
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823