Abstract
The time course of fluoxetine-induced supersensitivity of hypothalamic 5-HT2A/2C receptors was examined. Daily injections of fluoxetine (7 or 14 days) significantly increased agonist ([125I]DOI)-labeled high-affinity-state 5-HT2A/2C receptors in the hypothalamus, but not frontal cortex. No change was observed in the density of [3H]ketanscrin-labeled 5-HT2A receptors in either brain region. The levels of Gq- and G11- proteins in the hypothalamus and cortex were not altered by fluoxetine. These results suggest that fluoxetine gradually increases the G-protein coupling of 5-HT2A/2C receptors without altering the levels of Gq- or G11-proteins.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Amphetamines / antagonists & inhibitors*
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Amphetamines / pharmacology
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Animals
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Cerebral Cortex / drug effects
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Cerebral Cortex / metabolism
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Fluoxetine / pharmacology*
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GTP-Binding Proteins / metabolism*
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Hypothalamus / drug effects
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Hypothalamus / metabolism*
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Immunoblotting
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Ketanserin / pharmacology
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Male
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Rats
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Rats, Sprague-Dawley
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Receptors, Serotonin / drug effects*
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Selective Serotonin Reuptake Inhibitors / pharmacology*
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Serotonin Antagonists / pharmacology
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Serotonin Receptor Agonists / pharmacology*
Substances
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Amphetamines
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Receptors, Serotonin
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Serotonin Antagonists
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Serotonin Receptor Agonists
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Serotonin Uptake Inhibitors
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Fluoxetine
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Ketanserin
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GTP-Binding Proteins
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4-iodo-2,5-dimethoxyphenylisopropylamine