This paper reports the synthesis and binding assays toward benzodiazepine 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 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 (Ki < 100 nM) and selectivity toward the adenosine A(1) receptorial subtype. (C) Elsevier, Paris.
1,2,3-Triazolo[1,5-a]quinoxalines: synthesis and binding to benzodiazepine and adenosine receptors
GIORGI, IRENE;MANERA, CLEMENTINA;BETTI, LAURA;GIANNACCINI, GINO;TRINCAVELLI, MARIA LETIZIA;
1998-01-01
Abstract
This paper reports the synthesis and binding assays toward benzodiazepine 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 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 (Ki < 100 nM) and selectivity toward the adenosine A(1) receptorial subtype. (C) Elsevier, Paris.File in questo prodotto:
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