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 benzodiazepine and adenosine A1 and A(2A) receptors of new 1,2,3-triazolo[1,5-a]quinoxalin-4-one derivatives. The prepared compounds show good affinity 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 compounds 7a-c. Some derivatives of both series show good affinity (K(i) 1 receptorial subtype.