Synthesis and preliminary biological evaluation of [3H]-MRE 3008-F20: the first high affinity radioligand antagonist for the human A3 adenosine receptors |
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| Authors: | Baraldi P G Cacciari B Romagnoli R Varani K Merighi S Gessi S Borea P A Leung E Hickey S L Spalluto G |
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| Affiliation: | Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Italy. pgb@dns.unife.it |
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| Abstract: | The synthesis and the preliminary biological evaluation of the first high affinity radioligand antagonist for the human A3 adenosine receptor, named [3H]-MRE 3008-F20 are reported. [3H]-MRE 3008-20 bound human A3 receptors expressed in CHO cells with K(D) and Bmax value of 0.82 +/- 0.08 nM and 297 +/- 28 fmol/mg of protein, respectively. [3H]-MRE 3008-F20 represents a useful tool for a further characterization of A3 adenosine receptor subtype. |
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