Synthesis and preliminary biological evaluation of [H-3]-MRE 3008-F20: thefirst high affinity radioligand antagonist for the human A(3) adenosine receptors

Authors
Baraldi, PG Cacciari, B Romagnoli, R Varani, K Merighi, S Gessi, S Borea, PA Leung, E Hickey, SL Spalluto, G
Citation
Pg. Baraldi et al., Synthesis and preliminary biological evaluation of [H-3]-MRE 3008-F20: thefirst high affinity radioligand antagonist for the human A(3) adenosine receptors, BIOORG MED, 10(3), 2000, pp. 209-211
Citations number
22
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
3
Year of publication
2000
Pages
209 - 211
Database
ISI
SICI code
0960-894X(20000207)10:3<209:SAPBEO>2.0.ZU;2-2
Abstract
The synthesis and the preliminary biological evaluation of the first high a ffinity radioligand antagonist for the human A(3) adenosine receptor, named [H-3]-MRE 3008-F20 are reported. [H-3]-MRE 3008-20 bound human A(3) recept ors expressed in CHO cells with K-D and B-max value of 0.82 +/- 0.08 nM and 297 +/- 28 fmol/mg of protein, respectively. [H-3]-MRE 3008-F20 represents a useful tool for a further characterization of A(3) adenosine receptor su btype. (C) 2000 Elsevier Science Ltd. All rights reserved.