[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 synthesize...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2004-07, Vol.14 (13), p.3607-3610
Hauptverfasser:	BARALDI, Pier Giovanni, TABRIZI, Mojgan Aghazadeh, BOREA, Pier Andrea, PRETI, Delia, BOVERO, Andrea, FRUTTAROLO, Francesca, ROMAGNOLI, Romeo, MOORMAN, Allan R, GESSI, Stefania, MERIGHI, Stefania, VARANI, Katia
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetamides - chemical synthesis Acetamides - pharmacology Adenosine A2 Receptor Antagonists Allyl Compounds - chemistry Animals Benzoquinones - chemistry Binding, Competitive Biological and medical sciences CHO Cells Contrast media. Radiopharmaceuticals Cricetinae Humans Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Purines - chemical synthesis Purines - chemistry Purines - pharmacology Pyrazoles - chemical synthesis Pyrazoles - chemistry Pyrazoles - pharmacology Radioligand Assay Receptor, Adenosine A2B - metabolism Tritium - chemistry Xanthine - chemistry
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2004.03.084