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  Oct 11, 2018

Drugs Targeting the 5-HT System

Serotonin or 5-hydroxytryptamine (5-HT) is a neurotransmitter that binds to 5-HT receptors in the central and peripheral nervous systems. Serotonin is an example of an inhibitory neurotransmitter that has general sedative effects on the brain and counteracts the effects of stimulants such as caffeine, for example.

Adequate serotonin levels are needed to maintain a stable and balanced mood. Serotonin is mainly found in the gastrointestinal tract, the platelets and the central nervous system of animals and is thought to contribute to a sense of well being and happiness.

Several drugs are available that modify the 5-HT system and examples include:


Several types of drug are used to modify the 5-HT system in the treatment of depression. Monoamine-oxidase inhibitors (MOAIs) are drugs that prevent the breakdown of serotonin by the enzyme monoamine oxidase.

Selective serotonin reuptake inhibitors (SSRIs) are another form of therapy that prevents the reuptake of serotonin from the synaptic cleft so that it remains available to target nerve cells. Tricyclic antidepressants (TCAs) inhibit the re-uptake of both serotonin and norepinephrine from the synaptic cleft