Abstract
Parthenolide displaces [3H]ketanserin from 5HT2A receptors from rat and rabbit brain and cloned 5HT2A receptors. Ki's are in the 100-250 microM range. These results suggest that parthenolide may be a low-affinity antagonist at 5HT receptors; it is unlikely that the entire mechanism of action can be explained by its modest 5HT2A receptor affinity.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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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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Cells, Cultured
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In Vitro Techniques
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Ketanserin / pharmacokinetics
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Kinetics
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Rabbits
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Rats
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Receptors, Serotonin / drug effects
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Receptors, Serotonin / metabolism*
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Serotonin Antagonists / pharmacology*
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Sesquiterpenes / pharmacology*
Substances
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Receptors, Serotonin
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Serotonin Antagonists
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Sesquiterpenes
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parthenolide
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Ketanserin