A series of novel 1,2,3-benzotriazin-4-ones I (R = H, Cl, MeO, F, 3-CF3O; n = 2, 3) were prepd. and evaluated as ligands for 5-HT receptors. Radioligand binding assays proved that the majority of I behaved as good to excellent ligands at the 5-HT1A receptor, some of which were selective with respect 5-HT2A and 5-HT2C receptors. Six analogs were selected and further evaluated for their binding affinities on D1, D2 dopaminergic, and a1-, a2-adrenergic receptors. I (R = 2-MeO, n = 3) bound at 5-HT1A sites with subnanomolar affinity and showed high selectivity over all considered receptors and may offer a new lead for the development of therapeutically efficacious agents.
Synthesis of new 1,2,3-benzotriazin-4-one-arylpiperazine derivatives as 5-HT1A serotonin receptor ligands / Caliendo, Giuseppe; Fiorino, Ferdinando; Grieco, Paolo; Perissutti, Elisa; Santagada, Vincenzo; Severino, Beatrice; Bruni, G; Romeo, M. R.. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - STAMPA. - 8:3(2000), pp. 533-538.
Synthesis of new 1,2,3-benzotriazin-4-one-arylpiperazine derivatives as 5-HT1A serotonin receptor ligands.
CALIENDO, GIUSEPPE;FIORINO, FERDINANDO;GRIECO, PAOLO;PERISSUTTI, ELISA;SANTAGADA, VINCENZO;SEVERINO, BEATRICE;
2000
Abstract
A series of novel 1,2,3-benzotriazin-4-ones I (R = H, Cl, MeO, F, 3-CF3O; n = 2, 3) were prepd. and evaluated as ligands for 5-HT receptors. Radioligand binding assays proved that the majority of I behaved as good to excellent ligands at the 5-HT1A receptor, some of which were selective with respect 5-HT2A and 5-HT2C receptors. Six analogs were selected and further evaluated for their binding affinities on D1, D2 dopaminergic, and a1-, a2-adrenergic receptors. I (R = 2-MeO, n = 3) bound at 5-HT1A sites with subnanomolar affinity and showed high selectivity over all considered receptors and may offer a new lead for the development of therapeutically efficacious agents.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
