Entrainment of circadian rhythms by S-20098, a melatonin agonist, is dose and plasma concentration dependent

Martinet, Lise; Guardiola‐Lemaître, B.; Mocaer, E.

doi:10.1016/0091-3057(95)02221-x

Cited by 96 publications

(49 citation statements)

References 14 publications

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“…These data indicate that the mechanism of therapeutic action of evening administration of agomelatine and melatonin in the CMS model of depression differs from that of traditional antidepressants, and provides further evidence that the antidepressant-like effect of agomelatine depends, at least partially, on its chronobiotic properties exerted by an interaction with melatonin receptors. This conclusion is consistent with other reports showing that agomelatine can resynchronize circadian rhythms in animals (Armstrong et al, 1993;Redman et al, 1995;Martinet et al, 1996;Van Reeth et al, 1997Weibel et al, 2000) and with known clinical observations that disorganization of internal rhythms is one of the most characteristic feature of various depressive disorders and diurnal mood variations (Souetre et al, 1989;Wehr and Wirz-Justice, 1982;Healy, 1993).…”

Section: Discussionsupporting

confidence: 81%

“…The effect of evening treatment can be related to the agonistic action on melatonin receptors, which in consequence leads to normalization of the general impairment of circadian rhythms previously observed in animals undergoing the CMS procedure (Moreau et al, 1995;Gorka et al, 1996;Cheeta et al, 1997;D'Aquila et al, 1997). Actually, contrary to the dose-dependent morning activity of agomelatine, the ceiling effect observed after evening administration can be related to its chronobiotic activity, which is maximal at 8-10 mg/kg (Redman et al, 1995;Martinet et al, 1996). This possibility is strongly supported by the finding that the melatonin antagonist, S 22153, given acutely to stressed animals successfully treated with agomelatine and melatonin, fully reversed the effectiveness of both agents.…”

Section: Discussionmentioning

confidence: 71%

“…After chronic administration, agomelatine dose-dependently restores the phase shifting response to a dark pulse (Van Reeth et al, 2001) and accelerates by 25% resynchronization of the rhythm to the new light-dark cycle in old hamsters (Weibel et al, 2000). The re-entraining activity of agomelatine, which is related to a direct effect on melatonin receptors in the SCN (Redman and Francis, 1998;Ying et al, 1998), is dosedependent, and shows a clear relation to plasma concentration of agomelatine (Martinet et al, 1996). The chronobiotic properties of agomelatine are of particular interest since the disorganization of internal rhythms is believed to be involved in the pathophysiology of depression (Wehr and Wirz-Justice, 1982).…”

Section: Introductionmentioning

confidence: 99%

“…For example, this compound resets the electrical activity of the SCN (Ying et al, 1996) and resynchronizes experimentally disrupted circadian rhythms (Armstrong et al, 1993;Redman et al, 1995;Martinet et al, 1996;Van Reeth et al, 1997). After chronic administration, agomelatine dose-dependently restores the phase shifting response to a dark pulse (Van Reeth et al, 2001) and accelerates by 25% resynchronization of the rhythm to the new light-dark cycle in old hamsters (Weibel et al, 2000).…”

Section: Introductionmentioning

confidence: 99%

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Effect of Agomelatine in the Chronic Mild Stress Model of Depression in the Rat

Papp

Gruca

Boyer

et al. 2002

Neuropsychopharmacol

243

166

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Chronic mild stress (CMS), a well-validated model of depression, was used to study the effects of the melatonin agonist and selective 5-HT 2C antagonist agomelatine (S 20098) in comparison with melatonin, imipramine, and fluoxetine. All drugs were administered either 2 h before (evening treatment) or 2 h after (morning treatment) the dark phase of the 12-h light/dark cycle. Chronic (5 weeks) evening treatment with agomelatine or melatonin (both at 10 and 50 mg/kg i.p.) dose-dependently reversed the CMS-induced reduction in sucrose consumption. The magnitude and time course of the action of both drugs was comparable to that of imipramine and fluoxetine (both at 10 mg/kg i.p.); however, melatonin was less active than agomelatine at this dose. The effect of evening administration of agomelatine and melatonin was completely inhibited by an acute injection of the MT 1 /MT 2 antagonist, S 22153 (20 mg/kg i.p.), while the antagonist had no effect in animals receiving fluoxetine or imipramine. When the drugs were administered in the morning, agomelatine caused effects similar to those observed after evening treatment (with onset of action faster than imipramine) but melatonin was ineffective. Moreover, melatonin antagonist, S 22153, did not modify the intakes in stressed animals receiving morning administration of agomelatine and in any other control and stressed groups tested in this study. These data demonstrate antidepressant-like activity of agomelatine in the rat CMS model of depression, which was independent of the time of drug administration. The efficacy of agomelatine is comparable to that of imipramine and fluoxetine, but greater than that of melatonin, which had no antidepressant-like activity after morning administration. While the evening efficacy of agomelatine can be related to its melatonin receptors agonistic properties, its morning activity, which was not inhibited by a melatonin antagonist, indicates that these receptors are certainly required, but not sufficient to sustain the agomelatine efficacy. It is therefore suggested that the antidepressant-like activity of agomelatine depends on some combination of its melatonin agonist and 5-HT 2C antagonist properties.

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Section: Discussionsupporting

confidence: 81%

Section: Discussionmentioning

confidence: 71%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Effect of Agomelatine in the Chronic Mild Stress Model of Depression in the Rat

Papp

Gruca

Boyer

et al. 2002

Neuropsychopharmacol

243

166

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“…Les études réalisées in vivo ont montré que l'agomé-latine, comme la mélatonine, synchronise les rythmes circadiens d'activité-repos et de la température dans différents modèles de désynchronisation brutale des rythmes, chez les rongeurs placés en obscurité constante (modèle de cécité) [19][20][21], après une avance de phase du rythme lumière/obscurité, chez des rats présentant un retard de phase [22], ainsi que chez des rats et des hamsters âgés [23]. Les animaux âgés présentent des perturbations naturelles des rythmes circadiens et, chez ces animaux, l'agomélatine restaure la réponse de l'horloge circadienne aux stimuli environnementaux tels que les pulses d'obscurité et de lumière [24,25].…”

Section: Amélioration De La Synchronisation Des Rythmes Circadiensunclassified

Comment déveloper un antidépresseur au mécanisme d’action innovant : l’exemple de l’agomélatine

Mocaër

Delalleau

et al. 2005

Med Sci (Paris)

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Les travaux les plus récents ont confirmé la forte pré-valence de la dépression : sur leur vie entière, 20 % des femmes et 10 % des hommes ont fait, font ou feront un épisode dépressif. De tels chiffres sont à l'évidence marquants ; ils le sont encore plus lorsqu'on s'intéresse à la complication majeure de la dépression, le suicide, qui se chiffre à 12 000 décès par an dans des pays comme la France. D'une manière générale, on estime que 15 % des patients déprimés décè-dent par suicide [1]. À la souffrance personnelle et familiale que représente la dépression s'ajoute le poids social important de cette pathologie : la dépression représente d'ores et déjà l'une des premières causes d'arrêts de travail dans les pays occidentaux. Malgré l'arsenal thérapeutique mis à la disposition du corps médical, en particulier SSRI (selective serotonin reuptake inhibitors) et SNRI (serotonin norepinephrine reuptake inhibitors), 30 % de la population dépressive n'est pas traitée. Les SSRI sont relativement bien tolérés comparativement aux antidépresseurs imipraminiques, mais présentent un certain nombre d'effets indésirables tels que des effets gastro-intestinaux et des perturbations de la fonction sexuelle ou du sommeil [2]. Un syndrome de sevrage à l'arrêt du traitement a également été rapporté avec l'emploi de certains SSRI [3]. Il existe donc un besoin évident de nouveaux traitements, plus efficaces, mieux tolérés et d'action plus rapide.

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Sedative‐Hypnotics

Vida¹,

Yevich

2003

Burger's Medicinal Chemistry and Drug Discovery

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This chapter focuses on sedative‐hypnotic drugs that are sued to alleviate the condition of sleep disturbances. One‐third of our life is spent in sleep; the lack, of which, can cause serious physical, social, and psychological problems. This chapter describes the features of an ideal hypnotic drug and provides a classification of sedative‐hypnotic drugs currently in use. These include the barbiturates, benzodiazepines, halogenated sedative‐hypnotics, heterocyclic sedative‐hypnotics, antihistamines, and other sedative‐hypnotics. Individual members of all of these classes of drugs are discussed in detail. The chapter also describes the physiology of sleep and the sleep cycle, including the nonrapid eye movement and rapid eye movement sleep. A list of neurotransmitters and nonhypnotic drugs that have a direct and indirect action on the sleep cycle are provided. The pharmacology including the evaluation of sedative‐hypnotics are also given. The chapter refers to the discovery of one of the most frequently prescribed hypnotic drugs, Zolpidem. The chapter also examines structure‐activity relationships, recent developments, things to come, and available websites.

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Entrainment of circadian rhythms by S-20098, a melatonin agonist, is dose and plasma concentration dependent

Cited by 96 publications

References 14 publications

Effect of Agomelatine in the Chronic Mild Stress Model of Depression in the Rat

Effect of Agomelatine in the Chronic Mild Stress Model of Depression in the Rat

Comment déveloper un antidépresseur au mécanisme d’action innovant : l’exemple de l’agomélatine

Sedative‐Hypnotics

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