1,2,3-TRIAZOLO[1,5-A]QUINOXALINES - SYNTHESIS AND BINDING TO BENZODIAZEPINE AND ADENOSINE RECEPTORS

This paper reports the synthesis and binding assays toward benzodiazep ine and adenosine A(1) and A(2A) receptors of new 1,2,3-triazolo[1,5-a ]quinoxalin-4-one derivatives. The prepared compounds show good affini ty toward the benzodiazepine receptor (K-i 53-314 nM); the GABA ratio values suggest an inverse agonist activity for the N(5) unsubstituted compounds 6b-d and an agonist activity for the N(5) methylated compoun ds 7a-c. Some derivatives of both series show good affinity (Ki < 100 nM) and selectivity toward the adenosine A(1) receptorial subtype. (C) Elsevier, Paris.