Synthesis of 3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles, displaying combined 5-HT uptake inhibiting and alpha(2)-adrenoceptor antagonistic activities: a novel series of potential antidepressants
| Autor: | Sonia Martı́nez, Javier Fernández, Jesús Alcázar, Lieve I. Heylen, Rosa M. Alvarez, Ilse Biesmans, Anton Megens, Joaquín Pastor, J.Ignacio Andrés, Margot H. Bakker, Ana Isabel de Lucas, José María Cid, Carmen Nieto, J. Alonso |
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| Rok vydání: | 2003 |
| Předmět: |
Xylazine
Stereochemistry Clinical Biochemistry Pharmaceutical Science Nerve Tissue Proteins Biochemistry Chemical synthesis chemistry.chemical_compound Structure-Activity Relationship In vivo Drug Discovery Animals Neurotransmitter Molecular Biology Adrenergic alpha-Antagonists Serotonin Plasma Membrane Transport Proteins Membrane Glycoproteins Molecular Structure Chemistry Organic Chemistry Antagonist Membrane Transport Proteins Transporter Stereoisomerism Isoxazoles In vitro Antidepressive Agents Rats Molecular Medicine Serotonin Reuptake inhibitor Carrier Proteins Selective Serotonin Reuptake Inhibitors |
| Zdroj: | Bioorganicmedicinal chemistry letters. 13(16) |
| ISSN: | 0960-894X |
| Popis: | The synthesis of a series of novel 3-piperazinylmethyl-3a,4-dihydro-3 H -[1]benzopyrano[4,3- c ]isoxazoles as novel dual 5-HT reuptake inhibitors and α 2 -adrenoceptor antagonists is described. Their affinity at the three different human α 2 -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 α 2 -adrenoceptors. |
| Databáze: | OpenAIRE |
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