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Serotonin antagonist and reuptake inhibitors (SARIs) are a class of drugs used mainly as antidepressants, but also as anxiolytics and hypnotics. They act by antagonizing serotonin receptors such as 5-HT2A and inhibiting the reuptake of serotonin, norepinephrine, and/or dopamine. Additionally, most also antagonize α1-adrenergic receptors. The majority of the currently marketed SARIs belong to the phenylpiperazine class of compounds.
Contents
List of SARIs
Vilazodone is a related drug but does not fit into this class as it does not function as a serotonin antagonist, acting as a 5-HT1A receptor partial agonist instead. Vortioxetine, another closely related drug, could technically be considered to be a member of this group, but both vilazodone and vortioxetine are instead generally labeled as serotonin modulators and stimulators.
Niaprazine is a drug related to this group but does not inhibit the reuptake of serotonin or the other monoamines.
Medifoxamine could technically be said to belong to this group, as it is a serotonin-dopamine reuptake inhibitor and 5-HT2A and 5-HT2C receptor antagonist.
Binding profile
The affinities (Kd (nM)) of a selection of SARIs have been compared below at an assortment of binding sites:
The selected ligands act as antagonists (or inverse agonists depending on the site in question) at all receptors listed except at 5-HT1A where they are partial agonists, and as inhibitors of all transporters listed.