Pharmacodynamics<unk>  is a melatonin receptor agonist (MT1 (Ki 0.1 nM) and MT2 (Ki = 0.12 nM)) and serotonin 5-HT2C (Ki = 631 nM) and 5-HT2B receptor (Ki = 660 nM) antagonist. Binding studies indicate that it has no effect on monoamine uptake and no affinity for adrenergic, histamine, cholinergic, dopamine, and benzodiazepine receptors, nor other serotonin receptors.<unk>  resynchronizes circadian rhythms in animal models of delayed sleep phase syndrome. By antagonizing 5-HT2C, it disinhibits/increases noradrenaline and dopamine release specifically in the frontal cortex. Therefore, it is sometimes classified as a norepinephrine–dopamine disinhibitor. It has no influence on the extracellular levels of serotonin.<unk>  has shown an antidepressant-like effect in animal models of depression (learned helplessness test, despair test, chronic mild stress) as well as in models with circadian rhythm desynchronisation and in models related to stress and anxiety. In humans,<unk>  has positive phase-shifting properties; it induces a phase advance of sleep, body temperature decline, and melatonin onset. Antagonism of 5-HT2B is an antidepressant property<unk>  shares with several atypical antipsychotics, such as aripiprazole, which are themselves used as atypical antidepressants. 5-HT2B antagonists are currently being investigated for their usefulness in reducing cardiotoxicity of drugs as well as being effective in reducing headache. Hence this particular receptor antagonism of<unk>  is useful for its antidepressant effectiveness as well as reducing the drug's adverse effects.
Agomelatine
Tropisetron
Granisetron
Alosetron
Avacopan
Cabergoline
Loteprednol
Cilansetron