What is a Serotonin Antagonist and Reuptake Inhibitor?

Published on by Andrew Marshall

Introduction

Serotonin antagonist and reuptake inhibitors (SARIs) are a class of drugs used mainly as antidepressants, but also as anxiolytics and hypnotics. They act by antagonising serotonin receptors such as 5-HT2A and inhibiting the reuptake of serotonin, norepinephrine, and/or dopamine. Additionally, most also antagonise α1-adrenergic receptors. The majority of the currently marketed SARIs belong to the phenylpiperazine class of compounds.

List of SARIs

  • Marketed:
    • Etoperidone (Axiomin, Etonin)
    • Lorpiprazole (Normarex)
    • Mepiprazole (Psigodal)
    • Nefazodone (Serzone, Nefadar)
    • Trazodone (Desyrel)
  • Miscellaneous:
    • Vilazodone (Viibryd) – a related drug but does not fit into this class as it does not function as a serotonin antagonist, acting solely as a 5-HT1A receptor partial agonist instead.
    • Vortioxetine (Trintellix) – 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 (Nopron) – a drug related to this group but does not inhibit the reuptake of serotonin or the other monoamines.
    • Medifoxamine (Clédial, Gerdaxyl) – could perhaps technically be said to belong to this group, as it is a serotonin–dopamine reuptake inhibitor and 5-HT2A and 5-HT2C receptor antagonist, but not grouped as such.
  • Never marketed:
    • Lubazodone (YM-992, YM-35995) – a SARI that was never marketed.

This page is based on the copyrighted Wikipedia article < https://en.wikipedia.org/wiki/Serotonin_antagonist_and_reuptake_inhibitor >; it is used under the Creative Commons Attribution-ShareAlike 3.0 Unported License (CC-BY-SA). You may redistribute it, verbatim or modified, providing that you comply with the terms of the CC-BY-SA.