Abstract
A series of heterocyclic 2-(3,5-dimethylphenyl)tryptamine derivatives was prepared and evaluated on a rat gonadotropin releasing hormone receptor assay. The carbon tether length and heterocyclic ring attached to the amino group of 2-(3,5-dimethylphenyl)tryptamine were varied. Several of these derivatives were potent GnRH antagonists with the most potent compound having an IC50 of 16 nM.
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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Heterocyclic Compounds / chemical synthesis*
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Hormone Antagonists / chemistry
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Hormone Antagonists / metabolism*
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Inhibitory Concentration 50
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Rats
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Receptors, LHRH / metabolism*
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Tryptamines / chemical synthesis*
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Tryptamines / metabolism*
Substances
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Heterocyclic Compounds
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Hormone Antagonists
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Receptors, LHRH
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Tryptamines
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tryptamine