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 A(2A) receptors in rat striatal membranes (specific binding > 90%) with K(d) and B(max) value of 0.70 nM and 971 fmol/mg of protein, respectively. 3H-SCH 58261 represents a useful tool for a further characterization of A(2A) adenosine receptor subtype.
Synthesis of the tritium labeled SCH 58261, a new non-xanthine A(2A) adenosine receptor antagonist
BARALDI, Pier Giovanni;CACCIARI, Barbara;
1996
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 A(2A) receptors in rat striatal membranes (specific binding > 90%) with K(d) and B(max) value of 0.70 nM and 971 fmol/mg of protein, respectively. 3H-SCH 58261 represents a useful tool for a further characterization of A(2A) adenosine receptor subtype.I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
