Butyrophenone analogues in the carbazole series as potential atypical antipsychotics: synthesis and determination of affinities at D(2), 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors
| Autor: | José Brea, Christian F. Masaguer, María Isabel Loza, Enrique Raviña, Helena Tristan, José Angel Fontenla |
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| Rok vydání: | 2000 |
| Předmět: |
Male
Tertiary amine Butyrophenone Stereochemistry medicine.drug_class Carbazoles Aorta Thoracic Chemical synthesis Piperazines Aminoketone Rats Sprague-Dawley chemistry.chemical_compound Fischer indole synthesis Drug Discovery medicine Animals Receptor Pharmacology Carbazole Receptors Dopamine D2 Organic Chemistry Cell Membrane General Medicine Isoxazoles Affinities Butyrophenones Frontal Lobe Rats chemistry Receptors Serotonin Choroid Plexus Cattle Serotonin Antagonists Antipsychotic Agents |
| Zdroj: | European journal of medicinal chemistry. 35(1) |
| ISSN: | 0223-5234 |
| Popis: | We describe practical and efficient routes for synthesis of 2-aminomethyl-1,2,3,9-tetrahydro-4 H -carbazol-4-ones using the Fischer indole synthesis or palladium-catalysed cyclization methodologies, as well as their affinities for D 2 , 5-HT 2A and 5-HT 2C receptors, and their activity at the 5-HT 2B receptor. The most active compounds, 4b (QF 2003B) and 4c (QF 2004B), with a p K i (5-HT 2A /D 2 ) ratio of 1.28 show a potential antipsychotic profile according to Meltzer's classification. |
| Databáze: | OpenAIRE |
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