Abstract
N1-Arylsulfonyltryptamines have been identified as 5-HT6 receptor ligands. In particular, N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine (11q) is a high affinity, potent full agonist (5-HT6 Ki = 2 nM, EC50 = 6.5 nM, Emax = 95.5%). Compound 11q is selective in a panel of over 40 receptors and ion channels, has good pharmacokinetic profile, has been shown to increase GABA levels in the rat frontal cortex, and is active in the schedule-induced polydipsia model for obsessive compulsive disorders.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Administration, Oral
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Animals
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Biological Availability
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CHO Cells
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Cricetinae
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Cricetulus
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Dogs
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Frontal Lobe / metabolism
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Haplorhini
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Humans
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In Vitro Techniques
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Mice
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Microdialysis
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Microsomes, Liver / metabolism
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Radioligand Assay
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Rats
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Receptors, Serotonin / metabolism*
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Serotonin Receptor Agonists / chemical synthesis*
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Serotonin Receptor Agonists / pharmacokinetics
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Serotonin Receptor Agonists / pharmacology
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Solubility
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Structure-Activity Relationship
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Thiazoles / chemistry*
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Thiazoles / pharmacokinetics
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Thiazoles / pharmacology
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Tryptamines / chemical synthesis*
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Tryptamines / chemistry
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Tryptamines / pharmacokinetics
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Tryptamines / pharmacology
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gamma-Aminobutyric Acid / metabolism
Substances
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N(1)-(6-chloroimidazo(2,1-b)(1,3)thiazole-5-sulfonyl)tryptamine
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Receptors, Serotonin
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Serotonin Receptor Agonists
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Thiazoles
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Tryptamines
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serotonin 6 receptor
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gamma-Aminobutyric Acid