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Tricyclic isoxazolines: Identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and α2-adrenoceptor antagonism by J. Ignacio Andrés; Jesús Alcázar; José M. Alonso; Rosa M. Alvarez; Margot H. Bakker; Ilse Biesmans; José M. Cid; Ana I. De Lucas; Wilhelmus Drinkenburg; Javier Fernández; Luis M. Font; Laura Iturrino; Xavier Langlois; Ilse Lenaerts; Sonia Martínez; Anton A. Megens; Joaquín Pastor; Shirley Pullan; Thomas Steckler is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Tricyclic isoxazolines: Identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and α2-adrenoceptor antagonism about?
In previous articles we have described the discovery of a new series of tricyclic isoxazolines combining central serotonin (5-HT) reuptake inhibition with a 2 -adrenoceptor antagonistic activity. We report now on the synthesis, the in vitro binding potency and the primary in vivo activity of six enantiomers within this series, one of which was selected for further pharmacological evaluation and assigned as R226161. Some additional in vivo studies in rats are described with this compound, which proved to be centrally and orally active as a combined 5-HT reuptake inhibitor and a 2 -adrenoceptor antagonist.
Who reads Tricyclic isoxazolines: Identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and α2-adrenoceptor antagonism?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- J. Ignacio Andrés; Jesús Alcázar; José M. Alonso; Rosa M. Alvarez; Margot H. Bakker; Ilse Biesmans; José M. Cid; Ana I. De Lucas; Wilhelmus Drinkenburg; Javier Fernández; Luis M. Font; Laura Iturrino; Xavier Langlois; Ilse Lenaerts; Sonia Martínez; Anton A. Megens; Joaquín Pastor; Shirley Pullan; Thomas Steckler
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)
- Published
- 2007
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)