Frontal 5-HT 2A receptors studied in depressive patients during chronic treatment by selective serotonin reuptake inhibitors

Massou, J. M.; Trichard, Christian; Attar-Levy, D.; Féline, A.; Corruble, Emmanuelle; Beaufils, B.; Martinot, Jean‐Luc

doi:10.1007/s002130050377

Cited by 92 publications

(39 citation statements)

References 14 publications

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“…13 This implies that chronic fluoxetine can enhance 5-HT 2 -coupled activation of PLC and possibly other 5-HT receptor-coupled effectors such as PLA 2 . Like fluoxetine, the SSRI fluvoxamine increased rat cortex total PLA 2 activity after 7 days but not after 1 day of administration.…”

Section: Discussionmentioning

confidence: 99%

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Chronic fluoxetine upregulates activity, protein and mRNA levels of cytosolic phospholipase A2 in rat frontal cortex

et al. 2006

Pharmacogenomics J

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Chronic lithium and carbamazepine, which are effective against mania in bipolar disorder, decrease the activity of cytosolic phospholipase A 2 (cPLA 2 ) and the turnover rate of arachidonic acid in phospholipids in rat brain. Assuming that stages of bipolar disorder are related to brain arachidonic acid metabolism, we hypothesized that drugs effective in depression would increase cPLA 2 activity. To test this hypothesis, adult male CDF-344 rats were administered fluoxetine (10 mg/kg intraperitoneally (i.p.) or saline (control) (i.p.) chronically for 21 days. Frontal cortex cPLA 2 protein, phosphorylated cPLA 2 , activity and mRNA levels were increased after chronic fluoxetine. Transcription factors (activator protein-1, activator protein-2, glucocorticoid response element, polyoma enhancer element-3 and nuclear factor-kappa B ) that are known to regulate cPLA 2 gene expression were not significantly changed by chronic fluoxetine, but nuclear AU-rich element/poly(U)-binding/degradation factor-1 RNA-stabilizing protein was increased significantly. The results suggest that chronic fluoxetine increases brain cPLA 2 gene expression post-transcriptionally by increasing cPLA 2 mRNA stabilization. Chronic fluoxetine's effect on cPLA 2 expression was opposite to the effect reported with chronic lithium or carbamazepine administration, and may be part of fluoxetine's mode of action.

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Section: Discussionmentioning

confidence: 99%

“…13 Despite the many cellular and molecular targets of fluoxetine, its mechanism of action is not agreed upon. Arachidonic acid (20:4n-6) is a nutritionally essential polyunsaturated fatty acid predominately found in the stereospecifically numbered-2 (sn-2) position of membrane phospholipids.…”

Section: Consistent With the Above [mentioning

confidence: 99%

Chronic fluoxetine upregulates activity, protein and mRNA levels of cytosolic phospholipase A2 in rat frontal cortex

et al. 2006

Pharmacogenomics J

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“…These effects could be related to the long-lasting antidepressant-like actions of estrogens in the FST. It is notable that the 5-HT 2A receptor is also associated with antidepressant effects (Barnes and Sharp, 1999;Einat et al, 2001;Li et al, 1997b;Lucki et al, 1994;Massou et al, 1997;Raap and Van de Kar, 1999). The other proposed mechanism implies adaptive changes on the serotonergic and noradrenergic receptors that increase the cAMP response element binding protein (CREB) and the brain-derived neurotrophic factor (BDNF).…”

Section: Discussionmentioning

confidence: 99%

Antidepressant-Like Effect of Different Estrogenic Compounds in the Forced Swimming Test

Estrada‐Camarena

Fernández‐Guasti

López‐Rubalcava

2002

Neuropsychopharmacol

180

124

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The present study evaluated the possible antidepressant-like action of the natural estrogen 17b-estradiol (E 2 , 2.5-10 mg/rat), the synthetic steroidal estrogen ethinyl-estradiol (EE 2 , 1.25-10.0 mg/rat), and the nonsteroidal synthetic estrogen, diethyl-stilbestrol (DES, 0.25-1.0 mg/ rat) in ovariectomized adult female Wistar rats using the forced swimming test (FST). The behavioral profile induced by the estrogens was compared with that induced by the antidepressants fluoxetine (FLX, 2.5-10 mg/kg) and desipramine (DMI, 2.5-10 mg/kg). In addition, the temporal course of the antidepressant-like action of the estrogenic compounds was analyzed. FLX and DMI induced an antidepressant-like effect characterized by a reduced immobility and increased swimming for FLX and decreased immobility and increased climbing for DMI. Both E 2 and EE 2 produced a decrease in immobility and an increase in swimming, suggesting an antidepressant-like action. DES did not affect the responses in this animal model of depression at any dose tested. The time course analysis of the actions of E 2 (10 mg/rat) and EE 2 (5 mg/rat) showed that both compounds induced an antidepressant-like effect observed 1 h after their injection lasting for 2-3 days.

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“…This latency may be due to drug-induced changes in serotonin receptors and their signaling pathways. SSRIs produce long-term neuroadaptive changes in the serotonin 2 (5-HT 2 ) receptors (Cadogan et al, 1993;Li et al, 1993;Tilakaratne et al, 1995;Massou et al, 1997). Understanding these adaptive changes that occur in 5-HT 2A receptor signaling may lead to novel antidepressants with a shorter latency of therapeutic action.…”

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confidence: 99%

Chronic Fluoxetine Differentially Affects 5-Hydroxytryptamine_2A Receptor Signaling in Frontal Cortex, Oxytocin- and Corticotropin-Releasing Factor-Containing Neurons in Rat Paraventricular Nucleus

Damjanoska

Kar²,

Kindel³

et al. 2003

J Pharmacol Exp Ther

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Differential adaptive changes in serotonin 2A 2A ] receptor signaling during treatment may be one mechanism involved in the latency of therapeutic improvement with antidepressants, such as fluoxetine. We examined the effects of fluoxetine (2, 3, 7, 21, or 42 days) on hypothalamic 5-HT 2A receptor signaling. The hormone responses to an injection of the 5-HT 2A receptor agonist (Ϯ)-1-(2,5-dimethoxy-4-iodophenyl)-2-amino-propane HCl (DOI) were used as an index of hypothalamic 5-HT 2A receptor function. Treatment with fluoxetine for 21 or 42 days produced diminished adrenocorticotropic hormone (ACTH) and oxytocin (but not corticosterone) responses to DOI injections (2.5 mg/kg i.p.; 15 min postinjection). Regulators of G protein signaling 4 and G ␣q protein levels in the hypothalamic paraventricular nucleus were not altered during fluoxetine treatment. Because previous studies indicate that treatment with fluoxetine for 21 days resulted in increased hormone responses to DOI when measured at 30 min after injection, we examined the effect of fluoxetine (21 days) on DOI-induced increase hormone levels at 15, 30, and 60 min after DOI injection. Fluoxetine decreased the oxytocin response at 15 but not at 30 min post-DOI injection, and potentiated the ACTH and corticosterone responses at 30 min post-DOI injection. For comparison, we examined the effect of fluoxetine on 5-HT 2A receptor-mediated increase in phospholipase C (PLC) activity in the frontal cortex. 5-HT-stimulated, but not guanosine 5Ј-O-(3-thio)triphosphate-stimulated PLC activity was increased after 21 days of fluoxetine-treatment. Overall, these results indicate that chronic fluoxetine treatment can potentiate 5-HT 2A receptor signaling in frontal cortex but differentially alters 5-HT 2A receptor signaling in oxytocin-containing neurons and corticotropin-releasing factor-containing neurons in the paraventricular nucleus.

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Frontal 5-HT 2A receptors studied in depressive patients during chronic treatment by selective serotonin reuptake inhibitors

Cited by 92 publications

References 14 publications

Chronic fluoxetine upregulates activity, protein and mRNA levels of cytosolic phospholipase A2 in rat frontal cortex

Chronic fluoxetine upregulates activity, protein and mRNA levels of cytosolic phospholipase A2 in rat frontal cortex

Antidepressant-Like Effect of Different Estrogenic Compounds in the Forced Swimming Test

Chronic Fluoxetine Differentially Affects 5-Hydroxytryptamine_2A Receptor Signaling in Frontal Cortex, Oxytocin- and Corticotropin-Releasing Factor-Containing Neurons in Rat Paraventricular Nucleus

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Frontal 5-HT 2A receptors studied in depressive patients during chronic treatment by selective serotonin reuptake inhibitors

Cited by 92 publications

References 14 publications

Chronic fluoxetine upregulates activity, protein and mRNA levels of cytosolic phospholipase A2 in rat frontal cortex

Chronic fluoxetine upregulates activity, protein and mRNA levels of cytosolic phospholipase A2 in rat frontal cortex

Antidepressant-Like Effect of Different Estrogenic Compounds in the Forced Swimming Test

Chronic Fluoxetine Differentially Affects 5-Hydroxytryptamine2A Receptor Signaling in Frontal Cortex, Oxytocin- and Corticotropin-Releasing Factor-Containing Neurons in Rat Paraventricular Nucleus

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Chronic Fluoxetine Differentially Affects 5-Hydroxytryptamine_2A Receptor Signaling in Frontal Cortex, Oxytocin- and Corticotropin-Releasing Factor-Containing Neurons in Rat Paraventricular Nucleus