Eszopiclone - CAS 138729-47-2
Catalog number: 138729-47-2
Category: Inhibitor
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GABA Receptor
Eszopiclone is an active stereoisomer of zopiclone with hypnotic and sedative activity and without significant anxiolytic activity. Eszopiclone is a GABA A receptor agonist. It is able to bind to and activate the omega-1 subtype of the alpha subunit of the GABA receptor complex. This leads to the opening of chloride channels, causing hyperpolarization, inhibition of neuronal firing, and enhancement of the inhibitory effect of GABA. Eszopiclone is an approved for the treatment of insomnia. It is a controlled substance (depressant) in the US but not in Canada.
White To Pale Yellow Solid
Lunesta; (S)-Zopiclone; Estorra; Esopiclone;[(7S)-6-(5-chloropyridin-2-yl)-5-oxo-7H-pyrrolo[3,4-b]pyrazin-7-yl] 4-methylpiperazine-1-carboxylate
Acetone, Chloroform, Ethanol, Phosphate Buffer (pH 3.2),
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Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
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No Data Available
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Current Developer:
Eisai Co Ltd; Sepracor; Sunovion Pharmaceuticals
1.Dissection of the factors driving the placebo effect in hypnotic treatment of depressed insomniacs.
McCall WV;D'Agostino R Jr;Rosenquist PB;Kimball J;Boggs N;Lasater B;Blocker J Sleep Med. 2011 Jun;12(6):557-64. doi: 10.1016/j.sleep.2011.03.008. Epub 2011 May 20.
OBJECTIVES: ;Our prior work has shown that there is improvement in self-reported sleep in persons receiving placebo in hypnotic clinical trials. We examined the components of the "placebo response" in a hypnotic clinical trial.;METHODS: ;This was an exploratory analysis of a randomized, double-blind clinical trial of eszopiclone versus placebo in the treatment of persons with depression and insomnia who were also receiving fluoxetine at a clinic of a teaching hospital. Sixty adults with both depression and insomnia symptoms, who were free of significant primary sleep disorders, received open-label fluoxetine for 9weeks. Patients were further randomized 1:1 to receive either masked eszopiclone 3mg or placebo at bedtime after the first week of fluoxetine. We examined the respective contributions of three factors associated with the "placebo effect": (1) regression to the mean, (2) expectancy, and (3) social desirability.;RESULTS: ;There was evidence for regression to the mean for the continuous measurement of the Insomnia Severity Index (ISI) and the Hamilton Depression Rating Scale. There was evidence for expectancy in self-reported Wake After Sleep Onset, continuous measurement of ISI, and dichotomous remission/non-remitter measurement of ISI.
2.The modulation of synaptic GABA(A) receptors in the thalamus by eszopiclone and zolpidem.
Jia F;Goldstein PA;Harrison NL J Pharmacol Exp Ther. 2009 Mar;328(3):1000-6. doi: 10.1124/jpet.108.146084. Epub 2008 Nov 25.
Eszopiclone (Lunesta; Sepracor, Marlborough, MA) and zolpidem [N,N,6-trimethyl-2-(4-methylphenyl)-imidazo(1,2-a)pyridine-3-acetamide] are among the most commonly prescribed hypnotics in use in the United States. The thalamus plays a pivotal role in sleep regulation and rhythmicity. Two distinct subtypes of synaptic GABA(A) receptors (GABA(A)-Rs), alpha(1)beta(2)gamma(2) and alpha(3)beta(3)gamma(2), are expressed in thalamocortical relay neurons and in interneurons of the RTN (reticular thalamic nucleus), respectively. Thalamocortical neurons also express extrasynaptic GABA(A)-Rs composed of alpha(4)beta(2)delta subunits. In this study, we compared the effects of eszopiclone and zolpidem on miniature inhibitory postsynaptic currents (IPSCs), spontaneous IPSCs, and tonic inhibition in the mouse thalamus. Eszopiclone (0.1-1 microM) slowed the decay phase of IPSCs recorded from RTN neurons, whereas zolpidem was less effective and increased the decay time constant only at > or = 0.3 microM. IPSCs of RTN neurons were more sensitive to eszopiclone than zolpidem at all concentrations tested. On the other hand, IPSCs of relay neurons in the ventrobasal nucleus (VB) were more sensitive to zolpidem than eszopiclone.
3.Safety, Tolerability and Efficacy of Drugs for Treating Behavioural Insomnia in Children with Attention-Deficit/Hyperactivity Disorder: A Systematic Review with Methodological Quality Assessment.
Anand S;Tong H;Besag FMC;Chan EW;Cortese S;Wong ICK Paediatr Drugs. 2017 Jun;19(3):235-250. doi: 10.1007/s40272-017-0224-6.
OBJECTIVE: ;A large proportion of paediatric patients with attention-deficit/hyperactivity disorder (ADHD) have associated sleep problems which not only affect the child's wellbeing but also impact family functioning. Management of sleep problems is consequently an important aspect of overall ADHD management in paediatric patients. Although some drugs are being used off-label for the management of paediatric insomnia, there is scant clinical evidence supporting their use. Our aim was to identify and assess the quality of published studies reporting the safety, tolerability and efficacy of drugs used for treating behavioural insomnia in children with ADHD.;METHODS: ;After an initial screen to determine which drugs were most commonly used, we conducted a systematic review of English-language publications from searches of PubMed, EMBASE, PsycINFO and two trial register databases to February 2017, using keywords 'clonidine', 'melatonin', 'zolpidem', 'eszopiclone', 'L-theanine', 'guanfacine', 'ADHD', 'sleep disorder' and 'children'. For quality assessment of included studies, we used the CONSORT checklist for randomised control trials (RCTs) and the Downs and Black checklist for non-RCTs.
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CAS 138729-47-2 Eszopiclone

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