Abstract
There are currently no known agents that display selectivity between homomeric 5-hydroxytryptamine type 3A (5-HT3A) and heteromeric 5-HT3A/3B receptors. In the present study, we show that the CNS convulsant picrotoxin selectively interacts with 5-HT3A receptors. In whole-cell patch clamp recordings, the inhibitory effect of PTX was reduced 100-fold in heteromeric mouse 5-HT3A/3B receptors, compared to homomeric 5-HT3A receptors. Picrotoxin should prove to be a useful probe for determining the presence of homomeric vs. heteromeric 5-HT3 receptors in both native tissue and recombinant receptor preparations.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Cell Line
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Dose-Response Relationship, Drug
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Down-Regulation / drug effects
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Down-Regulation / genetics
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Drug Tolerance / genetics
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GABA Antagonists / pharmacology*
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Humans
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Ion Channel Gating / drug effects
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Ion Channel Gating / genetics
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Ligands
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Mice
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Picrotoxin / pharmacology*
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Protein Subunits / antagonists & inhibitors
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Protein Subunits / genetics
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Protein Subunits / metabolism
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Receptors, Serotonin, 5-HT3 / genetics
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Receptors, Serotonin, 5-HT3 / metabolism
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Serotonin / metabolism
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Serotonin / pharmacology
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Serotonin 5-HT3 Receptor Antagonists*
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Synaptic Transmission / drug effects
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Synaptic Transmission / genetics
Substances
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GABA Antagonists
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Ligands
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Protein Subunits
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Receptors, Serotonin, 5-HT3
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Serotonin 5-HT3 Receptor Antagonists
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Picrotoxin
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Serotonin