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Tag Archives: Agomelatine

Agomelatine is a melatonin receptor agonist (MT1 (Ki=0.1nM) and MT2 (Ki=0.12nM)) and a 5-HT2C (Ki=631nM) receptor antagonist. Binding studies announce that it has no aftereffect on monoamine uptake and no affection for adrenergic, histaminergic, cholinergic, dopaminergic and benzodiazepine receptors, nor added serotonergic receptors.
Agomelatine resynchronises circadian rhythms in beastly models of delayed beddy-bye appearance syndrome. By antagonizing 5-HT2C receptors, it disinhibits/increases noradrenaline and dopamine absolution accurately in the aboveboard cortex. Therefore, it is sometimes classified as a norepinephrine–dopamine disinhibitor. It has no access on the extracellular levels of serotonin. Agomelatine has apparent an antidepressant-like aftereffect in beastly models of abasement (learned helplessness test, anguish test, abiding balmy stress) as able-bodied as in models with circadian accent desynchronisation and in models accompanying to accent and anxiety. In humans, agomelatine has absolute appearance alive properties; it induces a appearance beforehand of sleep, physique temperature abatement and melatonin onset.