Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 1
| Autor: | Encarna Matesanz, José Manuel Alonso, Jesús Alcázar, Pilar Gil, Laura Iturrino, J. Ignacio Andres, Javier Fernández, Victor Sipido, Theo F. Meert, Anton Megens, Adolfo Dı́az |
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| Rok vydání: | 2002 |
| Předmět: |
Male
Tertiary amine Stereochemistry Clinical Biochemistry Pharmaceutical Science CHO Cells Biochemistry Chemical synthesis chemistry.chemical_compound Structure-Activity Relationship Cricetinae Drug Discovery Receptor Serotonin 5-HT2C Structure–activity relationship Animals Receptor Serotonin 5-HT2A Azepine Serotonin Antagonists Rats Wistar Receptor Molecular Biology Chemistry Organic Chemistry Azepines Affinities Rats Receptors Serotonin Molecular Medicine |
| Zdroj: | Bioorganicmedicinal chemistry letters. 12(2) |
| ISSN: | 0960-894X |
| Popis: | The synthesis of a series of novel 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives as well as their 5-HT(2A/2C) and H(1) receptor binding affinities are described. The in vivo activity as potential anxiolytics of the synthesised compounds was measured in a mCPP challenge test. One of the compounds, 2a, proved to be a potent 5-HT(2A/2C) receptor antagonist showing as well oral activity and therefore could be considered as a potential anxiolytic/antidepressant agent. |
| Databáze: | OpenAIRE |
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