Abstract
The tritium labeled form of 5-amino-7-(2-phenylethyl)-2-(2-furyl)-pyrazolo[4,3-e]1,2,4-triazolo[1,5-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[1,5-c]pyrimidine 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 A2A receptors in rat striatal membranes (specific binding > 90%) with Kd and Bmax value of 0.70 nM and 971 fmol/mg of protein, respectively. 3H-SCH 58261 represents a useful tool for a further characterization of A2A adenosine receptor subtype.
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