ArticlePsychopharmacology2005
Anxiolytic properties of agomelatine, an antidepressant with melatoninergic and serotonergic properties: role of 5-HT2C receptor blockade.
Article in Psychopharmacology, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 55 papers, 1 of them a synthesis that pooled it.
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Who cites it
55 citing papers in PubMed, 1 synthesis or guideline pooled it, 244 citations in OpenAlex.
- Efficacy of Agomelatine 25-50 mg for the Treatment of Anxious Symptoms and Functional Impairment in Generalized Anxiety Disorder: A Meta-Analysis of Three Placebo-Controlled Studies.Advances in therapy · 2021Pooled it
- Agomelatine Increases BDNF Serum Levels in Depressed Patients in Correlation with the Improvement of Depressive Symptoms.The international journal of neuropsychopharmacology · 2016Trial
- Serotonin receptor 4 in the ventral CA3 regulates agomelatine-induced anxiolytic-like behaviors.Acta pharmacologica Sinica · 2026Article
- Agomelatine decreased cocaine-induced locomotor activity in rats; a dose-time response study.Frontiers in pharmacology · 2026Article
- The Neuroprotective Impact of Agomelatine in Preserving Brain Tissue Molecular Structure Against Alzheimer's Disease Etiology.Neurochemical research · 2025Article
- Underlying pharmacological mechanisms of psilocin-induced broadband desynchronization and disconnection of EEG in rats.Frontiers in neuroscience · 2023Article
- Neuroanatomical, Biochemical, and Functional Modifications in Brain Induced by Treatment with Antidepressants.Molecular neurobiology · 2022Review
- Viloxazine for the Treatment of Attention Deficit Hyperactivity Disorder.Health psychology research · 2022Article
- Agomelatine for the treatment of generalized anxiety disorder: focus on its distinctive mechanism of action.Therapeutic advances in psychopharmacology · 2022Review
- GW117: A novel serotonin (5-HTCNS neuroscience & therapeutics · 2021Article
- International Union of Basic and Clinical Pharmacology. CX. Classification of Receptors for 5-hydroxytryptamine; Pharmacology and Function.Pharmacological reviews · 2021Review
- 17β-Estradiol augments the neuroprotective effect of agomelatine in depressive- and anxiety-like behaviors in ovariectomized rats.Psychopharmacology · 2020Article
- Agomelatine for the Treatment of Generalized Anxiety Disorder: A Meta-Analysis.Clinical psychopharmacology and neuroscience : the official scientific journal of the Korean College of Neuropsychopharmacology · 2020Article
- Increased 5-HT2C receptor editing predisposes to PTSD-like behaviors and alters BDNF and cytokines signaling.Translational psychiatry · 2019Article
- Disturbances of diurnal phase markers, behavior, and clock genes in a rat model of depression; modulatory effects of agomelatine treatment.Psychopharmacology · 2018Article
- The potentially beneficial central nervous system activity profile of ivacaftor and its metabolites.ERJ open research · 2018Article
- New targets for rapid antidepressant action.Progress in neurobiology · 2017Review
- A short history of the 5-HTPsychopharmacology · 2017Review
- Article
- Agomelatine in the treatment of mild-to-moderate depression in patients with cardiovascular disease: results of the national multicenter observational study PULSE.Neuropsychiatric disease and treatment · 2017Article
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4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
rationaleThe novel antidepressant agent, agomelatine, behaves as an agonist at melatonin receptors and as an antagonist at serotonin (5-HT)(2C) receptors.
objectivesTo determine whether, by virtue of its antagonist properties at 5-HT(2C) receptors, agomelatine elicits anxiolytic properties in rats.
methodsEmploying a combined neurochemical and behavioural approach, actions of agomelatine were compared to those of melatonin, the selective 5-HT(2C) receptor antagonist, SB243,213, and the benzodiazepine, clorazepate.
resultsIn unfamiliar pairs of rats exposed to a novel environment, agomelatine enhanced the time devoted to active social interaction, an action mimicked by clorazepate and by SB243,213. In a Vogel conflict procedure, agomelatine likewise displayed dose-dependent anxiolytic activity with a maximal effect comparable to clorazepate, and SB243,213 was similarly active in this procedure. In a plus-maze procedure in which clorazepate significantly enhanced percentage entries into open arms, agomelatine revealed only modest activity and SB243,213 was inactive. Further, like SB243,213, and in contrast to clorazepate, agomelatine did not suppress ultrasonic vocalizations emitted by rats re-exposed to an environment associated with an aversive stimulus. Whereas clorazepate reduced dialysate levels of 5-HT and noradrenaline in hippocampus and frontal cortex of freely moving rats, agomelatine did not affect extracellular levels of 5-HT and elevated those of noradrenaline. SB243,213 acted similarly to agomelatine. Melatonin, which did not modify extracellular levels of 5-HT or noradrenaline, was ineffective in all models of anxiolytic activity. Furthermore, the selective melatonin antagonist, S22153, did not modify anxiolytic properties of agomelatine in either the social interaction or the Vogel Conflict tests.
conclusionsIn contrast to melatonin, and reflecting blockade of 5-HT(2C) receptors, agomelatine is active in several models of anxiolytic properties in rodents. The anxiolytic profile of agomelatine differs from that of benzodiazepines from which it may also be distinguished by its contrasting influence on corticolimbic monoaminergic pathways.
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