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

n order to identify selective ligands for the 5-HT1A subtype receptor, the microwave-assisted synthesis and the binding assays on the 5-HT1A, 5-HT2A and 5-HT2C receptors of new benzotriazinone derivs. were reported. Conventional and microwave heating of the reactions were compared. Good yields and short reaction times were the main advantages of our synthetic route. More active compds. 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 I with Ki = 0.000178 nM was the most active and selective deriv. for the 5-HT1A receptor with respect to other serotonin receptors and the most selective deriv. compared to dopaminergic and adrenergic receptors.