Further studies on the binding of N1-substituted tryptamines at h5-HT6 receptors

N(1)-Arylsulfonyl-substituted analogs of N,N-dimethyltryptamine bind at 5-HT(6) 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 a...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2007-03, Vol.17 (6), p.1691-1694
Main Authors: NYANDEGE, Abner, KOLANOS, Renata, ROTH, Bryan L, GLENNON, Richard A
Format: Article
Language:English
Subjects:
Biological and medical sciences
Chromatography, Thin Layer
DNA, Complementary - biosynthesis
DNA, Complementary - genetics
Humans
Indicators and Reagents
Magnetic Resonance Spectroscopy
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Receptors, Serotonin - metabolism
Serotoninergic system
Structure-Activity Relationship
Tryptamines - chemistry
Tryptamines - metabolism
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Summary:N(1)-Arylsulfonyl-substituted analogs of N,N-dimethyltryptamine bind at 5-HT(6) 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 N(1)-benzenesulfonyl- and their corresponding N(1)-benzyltryptamine counterparts bind in a different fashion.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.12.089