17419-72-6Relevant academic research and scientific papers
Synthesis of new 1,2,3-benzotriazin-4-one-arylpiperazine derivatives as 5-HT(1A) serotonin receptor ligands
Caliendo, Giuseppe,Fiorino, Ferdinando,Grieco, Paolo,Perissutti, Elisa,Santagada, Vincenzo,Severino, Beatrice,Bruni, Giancarlo,Romeo, Maria Rosaria
, p. 533 - 538 (2007/10/03)
A series of novel 1,2,3-benzotriazin-4-one derivatives was prepared and evaluated as ligands for 5-HT receptors. Radioligand binding assays proved that the majority of the novel compounds behaved as good to excellent ligands at the 5-HT(1A) receptor, some of which were selective with respect 5-HT(2A) and 5-HT(2C) receptors. Six analogues (1a, 2a, 2b, 2c, 2e and 2i) were selected and further evaluated for their binding affinities on D1, D2 dopaminergic and α1-, α2-adrenergic receptors. A o-OCH3 derivative (2e) bound at 5-HT(1A) sites with subnanomolar affinity (IC50=0.059 nM) and shows high selectivity over all considered receptors and may offer a new lead for the development of therapeutically efficacious agents. Copyright (C) 2000 Elsevier Science Ltd.
Synthesis and biological activity of benzotriazole derivatives structurally related to trazodone
Caliendo, G.,Carlo, R. Di,Greco, G.,Meli, R.,Novellino, E.,et al.
, p. 77 - 84 (2007/10/02)
This paper outlines the synthesis and the pharmacological screening of a series of novel 1- and 2-ethyl>benzotriazoles and 1-propoxy>benzotriazoles, which are structurally related to trazodone.Antiserotonergic, antiadrenergic and antihistaminic in vitro activity and in vivo analgesic action are described.Some of the investigated compounds show overall pharmacological profiles similar to that of the antidepressant trazodone. benzotriazole / antiserotonergic activity / antiadrenergic activity / antihistaminic activity / analgesic activity
