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Antidepressant
Serotonin antagonist and reuptake inhibitor
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Serotonin antagonist and reuptake inhibitor

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Chemical structure of the serotonin antagonist and reuptake inhibitor trazodone.

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

List of SARIs

Marketed

Miscellaneous

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 (Ki, nM) for various receptors and transporters are as follows:

Compound SERT NET DAT 5-HT1A 5-HT2A 5-HT2B 5-HT2C 5-HT3 5-HT6 5-HT7 α1 α2 D2 H1 mACh
Etoperidone 890 20,000 52,000 85 36 ND ND ND ND ND 38 570 2,300 3,100 >35,000
Hydroxynefazodone 165–1,203 376–1,053 ND 56–589 7.2–34 ND ND ND ND ND 8.0–145 63–2,490 ND ND 11,357
mCPP 202–432 1,940–4,360 ND 44–400 32–398 3.2–63 3.4–251 427 1,748 163 97–2,900 106–570 >10,000 326 >10,000
Nefazodone 200–459 360–618 360 80 26 ND 72 ND ND ND 5.5–48 84–640 910 ≥370 >10,000
Trazodone 160–367 ≥8,500 ≥7,400 96–118 20–45 74–189 224–402 >10,000 >10,000 1,782 12–153 106–728 ≥3,500 220–1,100 >10,000
Triazoledione ≥34,527 >100,000 ND 636–1,371 159–211 ND ND ND ND ND 173 1,915 ND ND >100,000
Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site. For assay species and references, see the individual drug articles. Most but not all values are for human proteins.

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.

See also


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