Repeated treatment with antidepressants differentially alters 5-HT1A agonist-stimulated [35S]GTPγS binding in rat brain regions

Shen, Changpeng; Li, H; Meller, Emanuel

doi:10.1016/s0028-3908(02)00064-3

Cited by 74 publications

(49 citation statements)

References 30 publications

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“…On the contrary, this SSRI treatment was shown to enhance 5-HT 1A agonist-stimulated [ 35 S]-GTPgS binding in the hippocampus, which is consistent with the increased signaling efficiency of postsynaptic 5-HT 1A receptors already reported by other laboratories with fluoxetine (Elena Castro et al, 2003;Shen et al, 2002). Our data are also consistent with in vitro electrophysiological findings.…”

Section: Discussionsupporting

confidence: 93%

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Acute and chronic effects of citalopram on 5‐HT_1A receptor—Labeling by [¹⁸F]MPPF and—Coupling to receptors‐G proteins

Moulin-Sallanon

Charnay

Ginovart

et al. 2008

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KEY WORDSserotonin ( 18 F]MPPF appears to be an efficient radioligand to quantify specifically 5-HT 1A receptor density in brain imaging. The delayed therapeutic efficacy of citalopram did not appear to be linked to either a downregulation of 5-HT 1A receptors or to a 5-HT 1A receptor-G protein decoupling process in serotonergic neurons, but to increased functional sensitivity of postsynaptic 5-HT 1A receptors.

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Section: Discussionsupporting

confidence: 93%

“…(Elena Castro et al, 2003;Hensler, 2002;Pejchal et al, 2002;Shen et al, 2002) and in 5-HT transporter knock-out mice (Bouali et al, 2003;Fabre et al, 2000;Mannoury la Cour et al, 2001). However, under our conditions, this putative SSRI mechanism of action could not be reproduced with citalopram.…”

Section: Discussionmentioning

confidence: 99%

Acute and chronic effects of citalopram on 5‐HT_1A receptor—Labeling by [¹⁸F]MPPF and—Coupling to receptors‐G proteins

Moulin-Sallanon

Charnay

Ginovart

et al. 2008

Synapse

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“…With chronic SSRI treatment, 5-HT 1A autoreceptors (but not heteroreceptors) desensitize, restoring raphe firing to enhance 5-HT release. By contrast, sensitization of 5-HT 1A heteroreceptors is observed following chronic antidepressant treatment, although the mechanisms involved remain unclear [38][39][40][41][42][43].…”

Section: -Ht 1a Autoreceptors As Brakes For 5-ht Neurotransmissionmentioning

confidence: 99%

Transcriptional regulation of the 5-HT_1Areceptor: implications for mental illness

Albert

2012

Phil. Trans. R. Soc. B

115

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The serotonin-1A (5-HT 1A ) receptor is an abundant post-synaptic 5-HT receptor (heteroreceptor) implicated in regulation of mood, emotion and stress responses and is the major somatodendritic autoreceptor that negatively regulates 5-HT neuronal activity. Based on animal models, an integrated model for opposing roles of pre-and post-synaptic 5-HT 1A receptors in anxiety and depression phenotypes and response to antidepressants is proposed. Understanding differential transcriptional regulation of pre-versus post-synaptic 5-HT 1A receptors could provide better tools for their selective regulation. This review examines the transcription factors that regulate brain region-specific basal and stress-induced expression of the 5-HT 1A receptor gene (Htr1a). A functional polymorphism, rs6295 in the Htr1a promoter region, blocks the function of specific repressors Hes1, Hes5 and Deaf1, resulting in increased 5-HT 1A autoreceptor expression in animal models and humans. Its association with altered 5-HT 1A expression, depression, anxiety and antidepressant response are related to genotype frequency in different populations, sample homogeneity, disease outcome measures and severity. Preliminary evidence from gene Â environment studies suggests the potential for synergistic interaction of stress-mediated repression of 5-HT 1A heteroreceptors, and rs6295-induced upregulation of 5-HT 1A autoreceptors. Targeted therapeutics to inhibit 5-HT 1A autoreceptor expression and induce 5-HT 1A heteroreceptor expression may ameliorate treatment of anxiety and major depression.

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“…In this sense, in vitro and in vivo studies have shown that several SSRIs promote a desensitization of the presynaptic 5-HT 1A receptor subtype (Blier, 2001;Le Poul et al, 1995;Li et al, 1996Li et al, , 1997a, and that facilitates a general enhancement of serotonin levels. These changes in serotonin transmission appear to promote either sensitization (Castro et al, 2003;Shen et al, 2002) or desensitization of the postsynaptic serotonergic 5-HT 1A receptors (Li et al, 1997a;Serres et al, 2000;Shen et al, 2002), depending on the brain area.…”

Section: Introductionmentioning

confidence: 99%

Participation of the 5-HT1A Receptor in the Antidepressant-Like Effect of Estrogens in the Forced Swimming Test

Estrada‐Camarena

Fernández‐Guasti

López‐Rubalcava

2005

Neuropsychopharmacol

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The aim of the present study was to explore the possible participation of the 5-HT 1A receptor in the antidepressant-like action of two estrogenic compounds: 17b-estradiol (E 2 ) and ethynil-estradiol (EE 2 ) in the FST. Ovariectomized female Wistar rats were used in all experiments. As a positive control, the effect of the 5-HT 1A receptor agonist, 8-hydroxy-2-(di-n)-propil-aminotetraline (8-OH-DPAT; 0.0625, 0.125, 0.25 and 0.5 mg/kg) alone or in combination with WAY 100635 (0.5 and 1.0 mg/kg) was analyzed in the FST. In order to analyze the participation of the 5-HT 1A receptor in the antidepressant-like actions of estrogens, the effect of the selective antagonist WAY 100635 (0.5 and 1.0 mg/kg) in combination with E 2 (10 mg/rat) and EE 2 (5 mg/rat) was studied in the FST. In this case, WAY 100635 was administered either simultaneously with the estrogens (48 h before the FST test) or 30 min before the FST. On the other hand, a suboptimal dose of 8-OH-DPAT (0.0625 mg/kg), combined with a noneffective dose of E 2 (2.5 mg/rat) or EE 2 (1.25 mg/rat), was tested in the FST. The results showed that 8-OH-DPAT (0.25 and 0.5 mg/kg), E 2 (10 mg/rat), and EE 2 (5 mg/rat), by themselves, exerted an antidepressant-like action. The antagonist to the 5-HT 1A receptor WAY 100635, when applied together with 8-OH-DPAT or E 2 , blocked their antidepressant-like actions, but not the one induced by EE 2 . Interestingly, when the antagonist was applied 30 min before the FST, it was able to cancel the actions of EE 2 on immobility behavior, and had no effect on the actions of E 2. Finally, when a subthreshold dose of 8-OH-DPAT was combined with a noneffective dose of either E 2 or EE 2 , an antidepressant-like action was observed. The results support the notion that the 5-HT 1A receptor is one of the mediators of the antidepressant-like action of E 2 , and could indirectly contribute to the one induced by EE 2 .

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Repeated treatment with antidepressants differentially alters 5-HT1A agonist-stimulated [35S]GTPγS binding in rat brain regions

Cited by 74 publications

References 30 publications

Acute and chronic effects of citalopram on 5‐HT_1A receptor—Labeling by [¹⁸F]MPPF and—Coupling to receptors‐G proteins

Acute and chronic effects of citalopram on 5‐HT_1A receptor—Labeling by [¹⁸F]MPPF and—Coupling to receptors‐G proteins

Transcriptional regulation of the 5-HT_1Areceptor: implications for mental illness

Participation of the 5-HT1A Receptor in the Antidepressant-Like Effect of Estrogens in the Forced Swimming Test

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Repeated treatment with antidepressants differentially alters 5-HT1A agonist-stimulated [35S]GTPγS binding in rat brain regions

Cited by 74 publications

References 30 publications

Acute and chronic effects of citalopram on 5‐HT1A receptor—Labeling by [18F]MPPF and—Coupling to receptors‐G proteins

Acute and chronic effects of citalopram on 5‐HT1A receptor—Labeling by [18F]MPPF and—Coupling to receptors‐G proteins

Transcriptional regulation of the 5-HT1Areceptor: implications for mental illness

Participation of the 5-HT1A Receptor in the Antidepressant-Like Effect of Estrogens in the Forced Swimming Test

Contact Info

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Resources

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Acute and chronic effects of citalopram on 5‐HT_1A receptor—Labeling by [¹⁸F]MPPF and—Coupling to receptors‐G proteins

Acute and chronic effects of citalopram on 5‐HT_1A receptor—Labeling by [¹⁸F]MPPF and—Coupling to receptors‐G proteins

Transcriptional regulation of the 5-HT_1Areceptor: implications for mental illness