Abstract
The ring-closed phenylethylamine analogue 6-hydroxy-3-n-propyl-2,3,4,5-tetrahydro-1H-3-benzazepine (1) is a 5-HT1A receptor agonist of moderate potency, according to both in vivo biochemical data and in vitro binding data. The active compounds of this series also induce the 5-HT behavioral syndrome. Molecular modeling studies were performed with molecular mechanics calculations, and a tentative explanation for the relatively low potency of these serotonergic benzazepines is provided.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Benzazepines / chemistry*
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Benzazepines / pharmacology*
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Binding, Competitive
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Brain / drug effects
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Brain / metabolism
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Dopamine / biosynthesis
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Feedback
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In Vitro Techniques
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Male
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Models, Molecular
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Molecular Conformation
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Motor Activity / drug effects
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Norepinephrine / biosynthesis
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Radioligand Assay
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Rats
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Rats, Sprague-Dawley
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Receptors, Serotonin / drug effects
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Receptors, Serotonin / metabolism
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Serotonin / biosynthesis
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Serotonin Receptor Agonists / chemistry*
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Serotonin Receptor Agonists / pharmacology*
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Structure-Activity Relationship
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Thermodynamics
Substances
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Benzazepines
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Receptors, Serotonin
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Serotonin Receptor Agonists
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Serotonin
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Dopamine
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Norepinephrine