Toward brain imaging of serotonin 5-HT1A autoreceptor internalization

Zimmer, Luc; Riad, Mustapha; Rbah, Latifa; Belkacem-Kahlouli, A.; Bars, Didier Le; Renaud, Bernard; Descarries, Laurent

doi:10.1016/j.neuroimage.2004.03.020

Cited by 52 publications

(19 citation statements)

References 25 publications

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“…Lanfumey and Hamon, 2004). The 5-HT 1A receptor has been implicated in different pathologies (Jones and Blackburn, 2002) and is thought to play a central role in the action of antidepressants/anxiolytics such as selective serotonin reuptake inhibitors and azapirones (Blier and de Montigny, 1999;Hensler, 2003;Riad et al, 2004;www.elsevier.com/locate/jchemneu Journal of Chemical Neuroanatomy 31 (2006) 226-232 Zimmer et al, 2004). It has also recently been shown that 5-HT 1A receptor agonists possess a strong neuroprotective efficacy in brain ischemia (Mauler and Horvath, 2005).…”

Section: Introductionmentioning

confidence: 99%

A comparison of in vivo and in vitro neuroimaging of 5-HT1A receptor binding sites in the cat brain

Aznavour

Rbah

Léger

et al. 2006

Journal of Chemical Neuroanatomy

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Section: Introductionmentioning

confidence: 99%

A comparison of in vivo and in vitro neuroimaging of 5-HT1A receptor binding sites in the cat brain

Aznavour

Rbah

Léger

et al. 2006

Journal of Chemical Neuroanatomy

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“…One of the mechanisms that cause desensitization of G-protein-coupled receptors is internalization, and studies have demonstrated the internalization (i.e., transfer of the plasmatic membrane in the cytoplasm) of the 5-HT 1A auto-receptors in the dorsal raphe nucleus (DRN) of rats after acute treatment with the specific 8-OH-DPAT agonist to the 5-HT 1A -R, or with recapture inhibitors of the 5-HT (selective inhibitors of serotonin reuptake, SSRIs). Although this phenomenon has not been observed in the hippocampus, we know that in this structure the 5-HT 1A -Rs are located in the soma and dendrites of neurons (heteroreceptors) [14]. The SSRIs in the presynaptic terminals, in turn, increase the release of 5-HT, which binds to the 5-HT 1A -R auto-receptors present in the soma of the raphe neurons, thus inhibiting neuronal firing.…”

Section: Presynaptic and Postsynaptic 5-ht 1a -R And Their Signaling mentioning

confidence: 92%

Association of 5-HT1A Receptors with Affective Disorders

Soria-Fregozo¹,

Vega²,

FranciscoRodríguez-Landa³

et al. 2017

Serotonin - A Chemical Messenger Between All Types of Living Cells

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Serotonin or 5-hydroxytryptamine (5-HT) is synthesized in both the brain and peripheral system, which exert their actions at a wide family of receptors classified as 5-HT 1 to 5-HT 7 . Pharmacological, behavioral, and clinical studies involve particularly to the 5-HT 1A receptors (5-HT 1A -R) -auto-receptors (presynaptic) and heteroreceptors (postsynaptic) -in the control of motivated behavior, and consequently in the physiopathology of affective disorders and in the action mechanism of antidepressant drugs. In this way, some research support that 5-HT 1A -R participates in the delayed effect of different types of antidepressants, including selective serotonin reuptake inhibitors (SSRIs), and tricyclic drugs, principally. The therapeutic effect of serotonergic drugs as the SSRIs, starting with the binding to auto-receptors, which produces increases of 5-HT in the synaptic cleft as consequence of blockade of serotonin reuptake. While these molecular events occur initially, in the long-term are produced plastic changes at neuronal level, as well as down-regulation of the 5-HT 1A -R, which is associated with the therapeutic effects of antidepressant drugs. The purpose of this chapter is to analyze and discuss the current information about of 5-HT 1A -R-mediated signaling cascades, the intracellular signaling of 5-HT 1A -R, in addition to their expression and pharmacology that are important to treatment of affective disorders symptoms.

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“…From a disease mechanism point of view, the slow onset of efficacy observed across the spectrum of monoamine re-uptake inhibitors is incongruent with the primary mechanism of action of the drug. Many preclinical animal studies have demonstrated that blockade of re-uptake of neurotransmitters occurs within hours following drug administration [21][22][23]. However, most people with depression exhibit a delay in the therapeutic response that can be ≥ 4 -6 weeks.…”

Section: Treatment Strategies For Depression 21 the Tricyclics And Mmentioning

confidence: 99%

“…Recent attempts to visualise this mechanism have demonstrated that by using positron emission tomographic (PET) techniques, there can be a 30 -40% decrease in the surface dendritic expression of 5-HT 1A receptors following fluoxetine treatment [22]. Thus, use of specific PET probes may provide a viable and rapid means of assessing the potential of antidepressant therapy in any given individual, and may serve as a surrogate marker for efficacy [23]. In attempting to decrease the time for onset of efficacy several compounds have been tried as adjunct therapies along with SSRIs, such as pindolol or trazodone [27,28], clomipramine [29] or risperidone [30], but thus far, have seen limited clinical success.…”

Section: Treatment Strategies For Depression 21 the Tricyclics And Mmentioning

confidence: 99%

The corticotropin-releasing factor receptor: a novel target for the treatment of depression and anxiety-related disorders

Grigoriadis

2005

Expert Opinion on Therapeutic Targets

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The treatment of mood disorders has been the subject of intense study for more than half a century and has resulted in the discovery and availability of a number of compounds that have seen tremendous success in the management of major depression and anxiety-related disorders. In spite of this success, these drugs have not provided a complete therapeutic solution for all patients and this has revitalised the need for a greater understanding of the underlying molecular mechanisms and targets involved in these disorders. Elucidation of these novel targets will enable the development of a better class of compounds which could benefit a greater majority of the patient population and be devoid of the current side effect liabilities. Towards that end, this review examines, in detail, the prospect of one such target, the corticotropin-releasing factor system, as having an enhanced therapeutic profile with the potential of a broader range of efficacy with reduced side effect liabilities.

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Toward brain imaging of serotonin 5-HT1A autoreceptor internalization

Cited by 52 publications

References 25 publications

A comparison of in vivo and in vitro neuroimaging of 5-HT1A receptor binding sites in the cat brain

A comparison of in vivo and in vitro neuroimaging of 5-HT1A receptor binding sites in the cat brain

Association of 5-HT1A Receptors with Affective Disorders

The corticotropin-releasing factor receptor: a novel target for the treatment of depression and anxiety-related disorders

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