Title of article :
Synthesis of 3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles, displaying combined 5-HT uptake inhibiting and α2-adrenoceptor antagonistic activities: a novel series of potential antidepressants
Author/Authors :
J. Ignacio Andrés، نويسنده , , Jes?s Alc?zar، نويسنده , , José M. Alonso-Meijide، نويسنده , , Rosa M. Alvarez، نويسنده , , José M. Cid، نويسنده , , Ana I. De Lucas، نويسنده , , Javier Fernandez-Suarez، نويسنده , , Sonia Mart?nez، نويسنده , , Carmen Nieto، نويسنده , , Joaqu?n Pastor، نويسنده , , Margot H. Bakker، نويسنده , , Ilse Biesmans، نويسنده , , Lieve I. Heylen، نويسنده , , Anton A. Megens، نويسنده ,
Abstract :
The synthesis of a series of novel 3-piperazinylmethyl-3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles as novel dual 5-HT reuptake inhibitors and α2-adrenoceptor antagonists is described. Their affinity at the three different human α2-adrenoceptor subtypes and the 5-HT transporter site is reported. The in vivo activity of the compounds was measured in two different assays: (1) inhibition of pCA-induced excitation, which evaluates the ability to block the central 5-HT transporter, and (2) inhibition of xylazine-induced loss of righting, which evaluates the ability to block central α2-adrenoceptors.
