Synthesis and preliminary biological evaluation of [3H]-MRE 3008-F20: the first high affinity radioligand antagonist for the human A3 adenosine receptors

✍ Scribed by Pier Giovanni Baraldi; Barbara Cacciari; Romeo Romagnoli; Katia Varani; Stefania Merighi; Stefania Gessi; Pier Andrea Borea; Edward Leung; Sarah L Hickey; Giampiero Spalluto

• Publisher: Elsevier Science
• Year: 2000
• Tongue: English
• Weight: 123 KB
• Volume: 10
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/s0960-894x(99)00674-5

✦ Synopsis

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.