Abstract
A series of ring-substituted (i.e., methoxy and bromo) 3,4-dihydro- and 1,2,3,4-tetrahydro-beta-carbolines was examined at 5-HT(2A) and 5-HT(2C) serotonin receptors. Whereas most of the methoxy-substituted derivatives typically displayed affinities similar to their unsubstituted parents, certain (particularly 8-substituted) bromo derivatives displayed enhanced affinity. A binding profile was obtained for selected beta-carbolines.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Binding Sites
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Carbolines / chemical synthesis*
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Carbolines / chemistry
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Carbolines / pharmacokinetics*
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Drug Evaluation, Preclinical / methods
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Humans
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Kinetics
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Models, Molecular
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Molecular Conformation
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Protein Binding
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Receptor, Serotonin, 5-HT2A / metabolism
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Receptor, Serotonin, 5-HT2B / metabolism
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Receptor, Serotonin, 5-HT2C / metabolism
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Receptors, Serotonin, 5-HT2 / metabolism*
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Structure-Activity Relationship
Substances
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Carbolines
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Receptor, Serotonin, 5-HT2A
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Receptor, Serotonin, 5-HT2B
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Receptor, Serotonin, 5-HT2C
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Receptors, Serotonin, 5-HT2