Premium
Synthesis and In‐vitro Pharmacological Evaluation of New 5‐HT 1A Receptor Ligands Containing a Benzotriazinone Nucleus
Author(s) -
Fiorino Ferdinando,
Severino Beatrice,
De Angelis Francesca,
Perissutti Elisa,
Frecentese Francesco,
Massarelli Paola,
Bruni Giancarlo,
Collavoli Elga,
Santagada Vincenzo,
Caliendo Giuseppe
Publication year - 2008
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200700151
Subject(s) - receptor , chemistry , 5 ht receptor , dopaminergic , chemical synthesis , stereochemistry , serotonin , in vitro , derivative (finance) , affinities , radioligand assay , biochemistry , dopamine , endocrinology , biology , economics , financial economics
This paper reports the microwave‐assisted synthesis and the binding assays on the 5‐HT 1A , 5‐HT 2A and 5‐HT 2C receptors of new benzotriazinone derivatives, in order to identify selective ligands for the 5‐HT 1A 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 D 1 , D 2 dopaminergic and α 1 , α 2 adrenergic receptors. The 3‐(2‐(4‐(naphthalen‐1‐yl)piperazin‐1‐yl)ethyl)benzo[ d ][1,2,3]triazin‐4(3 H )‐one 5 with K i = 0.000178 nM was the most active and selective derivative for the 5‐HT 1A receptor with respect to other serotonin receptors and the most selective derivative compared to dopaminergic and adrenergic receptors.