Synthesis of the tritium labeled SCH 58261, a new non-xanthine A2A adenosine receptor antagonist

✍ Scribed by Pier Giovanni Baraldi; Barbara Cacciari; Silvio Dionisotti; Judith Egan; Giampiero Spalluto; Cristina Zocchi

• Publisher: John Wiley and Sons
• Year: 1996
• Tongue: French
• Weight: 375 KB
• Volume: 38
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/(sici)1099-1344(199608)38:8<725::aid-jlcr885>3.0.co;2-g

✦ Synopsis

The tritium labeled form of 5-amino-7-(2-phenylethyl)-2-(2-furyl)pyrazolo[4,3-e] 1,2,4-triazolo[l,5-c]pyrimidine (3H-SCH 58261) was obtained by reduction of 5-amino-7-[2-(2',4',5'-tribromo)phenylethyl]-2-(2-furyl)-pyrazolo[4,3-e] 1,2,4-triazolo[ 1,5clpyrimidine with tritium gas in the presence of 10% Pd-C. Final product was purified by HPLC to give the title 3H-SCH 58261 with radiochemical purity of 99% and specific activity of 68.6 Ci/mmol. 3H-SCH 58261 bound A ~A receptors in rat striatal membranes (specific binding > 90%) with Kd and Bmax value of 0.70 nM and 971 fmoYmg of protein, respectively. 3H-SCH 58261 represents a useful tool for a further characterization of A ~A adenosine receptor sub type.