Bioorganic and Medicinal Chemistry Letters p. 2719 - 2725 (2003)
Update date:2022-08-04
Topics:
Andres, J. Ignacio
Alcazar, Jesus
Alonso, Jose M.
Alvarez, Rosa M.
Cid, Jose M.
De Lucas, Ana I.
Fernandez, Javier
Martinez, Sonia
Nieto, Carmen
Pastor, Joaquin
Bakker, Margot H.
Biesmans, Ilse
Heylen, Lieve I.
Megens, Anton A.
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.
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