Serotonin antagonist and reuptake inhibitor



Serotonin antagonist and reuptake inhibitors (SARIs) are a class of drugs used as antidepressants. They act by antagonizing serotonin receptors such as 5-HT2A and inhibiting the reuptake of serotonin, norepinephrine, and/or dopamine. Additionally most also act as α1-adrenergic receptor antagonists.

List of SARIs

 * Etoperidone (Axiomin, Etonin)
 * Lubazodone (YM-992, YM-35,995)
 * Nefazodone (Serzone, Nefadar)
 * Trazodone (Desyrel)

Vilazodone is a related drug but does not fit into this category as it does not act as a serotonin antagonist, acting as a 5-HT1A receptor partial agonist instead.

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.