Serotonin antagonist and reuptake inhibitor


Serotonin antagonist and reuptake inhibitors 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

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-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-HT2A and 5-HT2B receptors and an agonist of the 5-HT1A, 5-HT2C, and 5-HT3 receptors.