Further studies on the binding of N1-substituted tryptamines at h5-HT6 receptors
| Autor: | Renata Kolanos, Bryan L. Roth, Richard A. Glennon, Abner N. Nyandege |
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| Rok vydání: | 2007 |
| Předmět: |
DNA
Complementary Magnetic Resonance Spectroscopy Stereochemistry Clinical Biochemistry Pharmaceutical Science Biochemistry Chemical synthesis Structure-Activity Relationship chemistry.chemical_compound Drug Discovery MS-245 Humans Moiety Molecular Biology Alkyl Sulfonyl chemistry.chemical_classification Aryl Organic Chemistry Tryptamines chemistry Receptors Serotonin Benzyl group Molecular Medicine Indicators and Reagents Chromatography Thin Layer |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 17:1691-1694 |
| ISSN: | 0960-894X |
| Popis: | N1-Arylsulfonyl-substituted analogs of N,N-dimethyltryptamine bind at 5-HT6 receptors. Replacement of the aryl moiety with similarly hydrophobic alkyl substituents results in decreased affinity, as does replacement of a benzenesulfonyl moiety with a benzyl group. Current findings indicate that an aryl (or substituted aryl) sulfonyl (rather than alkylsulfonyl or benzyl) moiety is optimal for high-affinity binding, and further suggest that the N1-benzenesulfonyl- and their corresponding N1-benzyltryptamine counterparts bind in a different fashion. |
| Databáze: | OpenAIRE |
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