1,2,3-Triazolo[1,5-a]quinoxalines: Synthesis and binding to benzodiazepine and adenosine receptors

Article abstract of DOI:10.1016/S0223-5234(98)80036-6

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) < 100 nM) and selectivity toward the adenosine A₁ receptorial subtype.