Abstract
The 5-HT1A and 5-HT2 receptor affinity of 2- and 3-substituted 1,2,3,4-tetrahydro-beta-carbolines 1-8, 10 and 12-15 has been determined. It has been found that the specific 5-HT1A affinity of the protonated form (KiAH+) 2-n-hexyl derivatives 4, 8, 14 and (+)-LSD is of the same order. It has been shown by means of molecular modelling methods that pharmacophores of all the active compounds can adopt a common position at the 5-HT1A receptor model. The model also offers an explanation for the observed stereoselectivity chiral compounds.
MeSH terms
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8-Hydroxy-2-(di-n-propylamino)tetralin / pharmacology
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Animals
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Binding, Competitive / drug effects
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Brain Chemistry / drug effects
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Carbolines / chemical synthesis*
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Carbolines / pharmacology
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Cerebral Cortex / drug effects
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Cerebral Cortex / metabolism
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Hippocampus / drug effects
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Hippocampus / metabolism
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In Vitro Techniques
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Ketanserin / pharmacology
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Rats
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Receptors, Serotonin / drug effects*
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Serotonin / pharmacology
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Carbolines
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Receptors, Serotonin
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Serotonin
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tryptoline
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8-Hydroxy-2-(di-n-propylamino)tetralin
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Ketanserin