Serotonin antagonist and reuptake inhibitors (SARIs) are a class of drugs used mainly as antidepressants, but also as

anxiolytic An anxiolytic (; also antipanic or antianxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxiet ...

s and hypnotics. They act by antagonizing serotonin receptors such as 5-HT_2A and inhibiting the

reuptake Reuptake is the reabsorption of a neurotransmitter by a neurotransmitter transporter located along the plasma membrane of an axon terminal (i.e., the Synapse, pre-synaptic neuron at a synapse) or glial cell after it has performed its function of ...

of serotonin,

norepinephrine Norepinephrine (NE), also called noradrenaline (NA) or noradrenalin, is an organic chemical in the catecholamine family that functions in the brain and body as both a hormone and neurotransmitter. The name "noradrenaline" (from Latin '' ad' ...

, and/or dopamine. Additionally, most also antagonize α₁-adrenergic receptors. The majority of the currently marketed SARIs belong to the

phenylpiperazine 1-Phenylpiperazine is a simple chemical compound featuring a phenyl group bound to a piperazine ring. The suffix ‘-piprazole’ is sometimes used in the names of drugs to indicate they belong to this class. List phenylpiperazine derivativesAlp ...

class of compounds.

List of SARIs

Marketed

* Etoperidone (Axiomin, Etonin) * Lorpiprazole (Normarex) * Mepiprazole (Psigodal) *

Nefazodone Nefazodone, sold formerly under the brand names Serzone, Dutonin, and Nefadar among others, is an atypical antidepressant which was first marketed by Bristol-Myers Squibb (BMS) in 1994 but has since largely been discontinued. BMS withdrew it from ...

(Serzone, Nefadar) *

Trazodone Trazodone, sold under many brand names, is an antidepressant medication. It is used to treat major depressive disorder, anxiety disorders, and difficulties with sleep. The medication is taken orally. Common side-effects include dry mouth, f ...

(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 In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonis ...

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-HT_2A and 5-HT_2C receptor 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 affinities (, ) for various receptors and transporters are as follows: These drugs act as antagonists or inverse agonists of the 5-HT_2A, α₁-adrenergic, and H₁ receptors, as

s of the 5-HT_1A receptor, and as 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

of the human 5-HT_2A and 5-HT_2C receptors.

References

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