Serotonin antagonist and reuptake inhibitor
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Through Drug, Metabolite and Ligand (biochemistry)
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.
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Pharmacology
Binding profiles
The binding profiles of SARIs and some metabolites in terms of their affinities (Ki, nM) for various receptors and transporters are as follows:
These drugs act as antagonists or inverse agonists of the 5-HT2A, α1-adrenergic, and H1 receptors, as partial agonists of the 5-HT1A receptor, and as inhibitors of the transporters. mCPP is an antagonist of the 5-HT2B receptor, an agonist of the 5-HT1A, 5-HT2C, and 5-HT3 receptors, and acts as a partial agonist of the human 5-HT2A and 5-HT2C receptors.
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