Fluoxetine and Sleep EEG Effects of a Single Dose, Subchronic Treatment, and Discontinuation in Healthy Subjects

Feige, Bernd

doi:10.1016/s0893-133x(01)00314-1

Cited by 51 publications

(26 citation statements)

References 48 publications

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“…Abnormalities of REM sleep (shortening of REM latency, lengthening of the duration of the first REM period) are frequently observed in patients with major depressive disorder and have been considered specific of depressive disease (Feige et al, 2002;Chalon et al, 2005). In the present study, THIIC decreased REM sleep and increased NREM sleep.…”

Section: Discussionsupporting

confidence: 48%

N-(4-((2-(trifluoromethyl)-3-hydroxy-4-(isobutyryl)phenoxy)methyl)benzyl)-1-methyl-1H-imidazole-4-carboxamide (THIIC), a Novel Metabotropic Glutamate 2 Potentiator with Potential Anxiolytic/Antidepressant Properties: In Vivo Profiling Suggests a Link between Behavioral and Central Nervous System Neurochemical Changes

Fell

Witkin²,

Falcone³

et al. 2010

J Pharmacol Exp Ther

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The normalization of excessive glutamatergic neurotransmission through the activation of metabotropic glutamate 2 (mGlu2) receptors may have therapeutic potential in a variety of psychiatric disorders, including anxiety/depression and schizophrenia. Here, we characterize the pharmacological properties of N- (4-((2-(trifluoromethyl)-3-hydroxy-4-(isobutyryl)phenoxy)methyl)benzyl)-1-methyl-1H-imidazole-4-carboxamide (THIIC), a structurally novel, potent, and selective allosteric potentiator of human and rat mGlu2 receptors (EC 50 ϭ 23 and 13 nM, respectively). THIIC produced anxiolytic-like efficacy in the rat stress-induced hyperthermia assay and the mouse stress-induced elevation of cerebellar cGMP and marble-burying assays. THIIC also produced robust activity in three assays that detect antidepressant-like activity, including the mouse forced-swim test, the rat differential reinforcement of low rate 72-s assay, and the rat dominant-submissive test, with a maximal response similar to that of imipramine. Effects of THIIC in the forced-swim test and marble burying were deleted in mGlu2 receptor null mice. Analysis of sleep electroencephalogram (EEG) showed that THIIC had a sleeppromoting profile with increased non-rapid eye movement (REM) and decreased REM sleep. THIIC also decreased the dark phase increase in extracellular histamine in the medial prefrontal cortex and decreased levels of the histamine metabolite tele-methylhistamine (t-MeHA) in rat cerebrospinal fluid. Collectively, these results indicate that the novel mGlu2-positive allosteric modulator THIIC has robust activity in models used to predict anxiolytic/antidepressant efficacy, substantiating, at least with this molecule, differentiation in the biological impact of mGlu2 potentiation versus mGlu2/3 orthosteric agonism. In addition, we provide evidence that sleep EEG and CSF t-MeHA might function as viable biomarker approaches to facilitate the translational development of THIIC and other mGlu2 potentiators.

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Section: Discussionsupporting

confidence: 48%

N-(4-((2-(trifluoromethyl)-3-hydroxy-4-(isobutyryl)phenoxy)methyl)benzyl)-1-methyl-1H-imidazole-4-carboxamide (THIIC), a Novel Metabotropic Glutamate 2 Potentiator with Potential Anxiolytic/Antidepressant Properties: In Vivo Profiling Suggests a Link between Behavioral and Central Nervous System Neurochemical Changes

Fell

Witkin²,

Falcone³

et al. 2010

J Pharmacol Exp Ther

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show abstract

“…Different medications have different effects on various sleep parameters (17,(96)(97)(98)(99). Some SSRIs and tricyclics can improve delta sleep (32,(100)(101)(102)(103). In fact, SSRIs have been observed to improve DSR in both remitters and nonremitters (104).…”

Section: Discussionmentioning

confidence: 99%

Decreased delta sleep ratio and elevated alpha power predict vulnerability to depression during interferon-alpha treatment

Lotrich

Germain

2014

Acta Neuropsychiatr.

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“…: cf. Feige et al, 2002, for an example of a pharmacological manipulation of delta activity). delta waves, while both duration and the intensity of wakefulness shape delta activity in NREMS (cf.…”

Section: A Theory On the Function (S) Of Sleepmentioning

confidence: 99%

Toward an integrative theory of sleep and dreaming

Muzur

2005

Journal of Theoretical Biology

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Fluoxetine and Sleep EEG Effects of a Single Dose, Subchronic Treatment, and Discontinuation in Healthy Subjects

Cited by 51 publications

References 48 publications

Decreased delta sleep ratio and elevated alpha power predict vulnerability to depression during interferon-alpha treatment

Toward an integrative theory of sleep and dreaming

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