Binding of isotryptamines and indenes at h5-HT6 serotonin receptors

To determine if the indolic nitrogen atom is required for the binding of N(1)-benzyltryptamines at h5-HT(6) serotonin receptors, several isotryptamines and indene analogs were examined. The affinity of 3-benzyl-N(1)-(N,N-dimethylaminoethyl)indole (5, K(i)=32nM) and 1-benzyl-3-(N,N-dimethylaminoethyl...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2005-04, Vol.15 (8), p.1987-1991
Main Authors: KOLANOS, Renata, SIRIPURAPU, Uma, PULLAGURLA, Manik, RIAZ, Mohamed, SETOLA, Vince, ROTH, Bryan L, DUKAT, Małgorzata, GLENNON, Richard A
Format: Article
Language:English
Subjects:
Binding Sites
Biological and medical sciences
Humans
Indenes - chemistry
Indenes - metabolism
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Protein Binding
Receptors, Serotonin - chemistry
Receptors, Serotonin - metabolism
Serotoninergic system
Tryptamines - chemistry
Tryptamines - metabolism
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Summary:To determine if the indolic nitrogen atom is required for the binding of N(1)-benzyltryptamines at h5-HT(6) serotonin receptors, several isotryptamines and indene analogs were examined. The affinity of 3-benzyl-N(1)-(N,N-dimethylaminoethyl)indole (5, K(i)=32nM) and 1-benzyl-3-(N,N-dimethylaminoethyl)indene (11, K(i)=3nM) indicates that the indolic nitrogen atom is not essential for binding.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2005.02.070