Abstract
A series of 2-(3,5-dimethylphenyl)tryptamine derivatives was prepared and evaluated on a rat gonadotropin releasing hormone receptor assay. Some para-substituents on the 4-phenylbutyl side chain attached to the tryptamine nitrogen led to compounds with potent GnRH receptor binding. The study has helped define structural requirements for GnRH receptor binding for the 2-aryltryptamine GnRH antagonists.
MeSH terms
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Animals
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Binding Sites / physiology
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Drug Design
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Female
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Hormone Antagonists / chemistry
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Hormone Antagonists / metabolism*
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Hormone Antagonists / pharmacology*
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Humans
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Inhibitory Concentration 50
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Molecular Structure
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Rats
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Receptors, LHRH / metabolism*
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Tryptamines / chemical synthesis*
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Tryptamines / chemistry
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Tryptamines / metabolism*
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Tryptamines / pharmacology*
Substances
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2-(3,5-dimethylphenyl)tryptamine
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Hormone Antagonists
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Receptors, LHRH
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Tryptamines
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tryptamine