Serotonin antagonist and reuptake inhibitors (SARIs) are a class of drugs used mainly as antidepressants, but also as anxiolytics and hypnotics. They act by receptor antagonist, antagonizing serotonin receptors such as 5-HT2A receptor, 5-HT_2A and reuptake inhibitor, inhibiting the reuptake of serotonin, norepinephrine, and/or dopamine. Additionally, most also receptor antagonist, antagonize alpha-1 adrenergic receptor, 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-HT_1A 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 modulator and stimulator, 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 receptor, 5-HT_2A and 5-HT2C receptor, 5-HT_2C receptor receptor antagonist, antagonist, but not grouped as such.

Never marketed

* Lubazodone (YM-992, YM-35995) – a SARI that was never marketed.

Pharmacology

Binding profiles

The binding profiles of SARIs and some metabolites in terms of their affinity (pharmacology), affinities (, ) for various receptor (biochemistry), receptors and membrane transport protein, transporters are as follows: These drugs act as receptor antagonist, antagonists or inverse agonists of the 5-HT_2A, α₁-adrenergic, and H₁ receptors, as partial agonists of the 5-HT_1A receptor, and as transporter blocker, inhibitors of the transporters. mCPP is an antagonist of the 5-HT_2B receptor, an agonist of the 5-HT_1A, 5-HT_2C, and 5-HT₃ receptors, and acts as a partial agonist of the human 5-HT_2A and 5-HT_2C receptors.

References

{{Monoamine reuptake inhibitors Antidepressants Anxiolytics Serotonin receptor antagonists Serotonin reuptake inhibitors