Abstract
A series of 6-substituted tricyclic ergoline partial structures has been synthesized and found to possess very strong serotonin agonist activity. A methoxy group at the 6-position greatly enhances activity, but at the expense of compound stability. Substituting the 6-position with protophyllic groups that are also electron-withdrawing in character enhances both activity and stability.
MeSH terms
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Animals
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Brain / drug effects
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Brain / metabolism
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Chemical Phenomena
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Chemistry
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Corticosterone / blood
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Hydroxyindoleacetic Acid / metabolism
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Indoles / chemical synthesis
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Indoles / metabolism
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Indoles / pharmacology*
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Male
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Rats
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Rats, Inbred Strains
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Receptors, Serotonin / drug effects*
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Receptors, Serotonin / metabolism
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Serotonin / metabolism
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Structure-Activity Relationship
Substances
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Indoles
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Receptors, Serotonin
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Serotonin
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Hydroxyindoleacetic Acid
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Corticosterone