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 B(max) 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. (C) 2000 Elsevier Science Ltd. All rights reserved.
Synthesis and preliminary biological evaluation of [H-3]-MRE 3008-F20: the first high affinity radioligand antagonist for the human A(3) adenosine receptors
BARALDI, Pier Giovanni;CACCIARI, Barbara;ROMAGNOLI, Romeo;VARANI, Katia;MERIGHI, Stefania;GESSI, Stefania;
2000
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 B(max) 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. (C) 2000 Elsevier Science Ltd. All rights reserved.File in questo prodotto:
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