This paper reports the microwave-assisted synthesis and the binding assays on the 5-HT1A, 5-HT2A and 5-HT2C receptors of new benzotriazinone derivatives, in order to identify selective ligands for the 5-HT1A subtype receptor. Conventional and microwave heating of the reactions were compared. Good yields and short reaction times are the main advantages of our synthetic route. More active compounds were selected and further evaluated for their binding affinities on D1, D2 dopaminergic and a1, a2 adrenergic receptors. The 3-(2-(4-(naphthalen-1-yl)piperazin-1-yl)ethyl) benzo[d][1,2,3]triazin-4(3H)-one 5 with Ki = 0.000178 nM was the most active and selective derivative for the 5-HT1A receptor with respect to other serotonin receptors and the most selective derivative compared to dopaminergic and adrenergic receptors.

Fiorino, F., Severino, B., DE ANGELIS, F., Perissutti, E., Frecentese, F., Massarelli, P., et al. (2008). Synthesis and in-vitro pharmacological evaluation of new 5-HT1A receptor ligands containing a benzotriazinone nucleus. ARCHIV DER PHARMAZIE, 341(1), 20-27 [10.1002/ardp.200700151].

Synthesis and in-vitro pharmacological evaluation of new 5-HT1A receptor ligands containing a benzotriazinone nucleus

MASSARELLI, PAOLA;BRUNI, GIANCARLO;
2008

Abstract

This paper reports the microwave-assisted synthesis and the binding assays on the 5-HT1A, 5-HT2A and 5-HT2C receptors of new benzotriazinone derivatives, in order to identify selective ligands for the 5-HT1A subtype receptor. Conventional and microwave heating of the reactions were compared. Good yields and short reaction times are the main advantages of our synthetic route. More active compounds were selected and further evaluated for their binding affinities on D1, D2 dopaminergic and a1, a2 adrenergic receptors. The 3-(2-(4-(naphthalen-1-yl)piperazin-1-yl)ethyl) benzo[d][1,2,3]triazin-4(3H)-one 5 with Ki = 0.000178 nM was the most active and selective derivative for the 5-HT1A receptor with respect to other serotonin receptors and the most selective derivative compared to dopaminergic and adrenergic receptors.
Fiorino, F., Severino, B., DE ANGELIS, F., Perissutti, E., Frecentese, F., Massarelli, P., et al. (2008). Synthesis and in-vitro pharmacological evaluation of new 5-HT1A receptor ligands containing a benzotriazinone nucleus. ARCHIV DER PHARMAZIE, 341(1), 20-27 [10.1002/ardp.200700151].
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11365/17875
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