The synthesis by microwave irradn. and the binding tests on the 5-HT1A, 5-HT2A and 5-HT2C receptors of new substituted piperazines in order to identify selective ligands for 5-HT1A subtype receptor are reported. Conventional heating and microwave irradn. of the reactions was compared. Synthesis by microwave irradn. gave the desired compds. in better yields than those obtained by conventional heating. The overall times for the syntheses were considerably reduced. Some resulting active compds.were characterized by a good selectivity profile for the 5-HT1A subtype receptor. The more active compds. were selected and further evaluated for their binding affinities on D1, D2 dopaminergic and a1, a2 adrenergic receptors. The compd. with higher affinity and selectivity for the 5-HT1A over all the considered receptors was (-)-3-{4-[4-(1,2,3,4-tetrahydronaphthyl)-1-piperazinyl]butyl}benzotriazinone (5-HT1A Ki=36 nM, other receptors not active).
Synthesis by microwave irradiation and binding properties of novel 5-HT1A receptor ligands / Caliendo, Giuseppe; Fiorino, Ferdinando; Perissutti, Elisa; Severino, Beatrice; Gessi, S; Cattabriga, E; Borea, P. A.; Santagada, Vincenzo. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - STAMPA. - 36:11-12(2001), pp. 873-886.
Synthesis by microwave irradiation and binding properties of novel 5-HT1A receptor ligands.
CALIENDO, GIUSEPPE;FIORINO, FERDINANDO;PERISSUTTI, ELISA;SEVERINO, BEATRICE;SANTAGADA, VINCENZO
2001
Abstract
The synthesis by microwave irradn. and the binding tests on the 5-HT1A, 5-HT2A and 5-HT2C receptors of new substituted piperazines in order to identify selective ligands for 5-HT1A subtype receptor are reported. Conventional heating and microwave irradn. of the reactions was compared. Synthesis by microwave irradn. gave the desired compds. in better yields than those obtained by conventional heating. The overall times for the syntheses were considerably reduced. Some resulting active compds.were characterized by a good selectivity profile for the 5-HT1A subtype receptor. The more active compds. were selected and further evaluated for their binding affinities on D1, D2 dopaminergic and a1, a2 adrenergic receptors. The compd. with higher affinity and selectivity for the 5-HT1A over all the considered receptors was (-)-3-{4-[4-(1,2,3,4-tetrahydronaphthyl)-1-piperazinyl]butyl}benzotriazinone (5-HT1A Ki=36 nM, other receptors not active).I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.