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5-Hydroxytryptamine Receptor Family

5-hydroxytryptamine (5-HT) receptors, also known as serotonin receptors, are a group of G protein-coupled receptor. They are ligand-gated ion channels in the central and peripheral nervous systems and found in almost all animals. They mediate both excitatory and inhibitory neurotransmission. The 5-HT receptors are activated by the neurotransmitter serotonin, which acts as their natural ligand.

The 5-hydroxytryptamine receptors affect various biological and neurological processes such as appetite, anxiety, mood, cognition, learning, memory, nausea, sleep, thermoregulation, and aggression. Moreover, 5-HT receptors are the target of a variety of pharmaceutical and recreational drugs. And 5-HT receptor modulating drugs have now established their therapeutic role in various disease conditions like emesis, anxiety, and migraine, in various other neurological conditions, as well as peripheral disorders.

Signal transduction of 5-HT receptor subtypes. Fig.1 Signal transduction of 5-HT receptor subtypes. (Ohno, 2015)

Moreover, 5-hydroxytryptamine is related to carcinoid syndrome which secretes a variety of hormones. The syndrome is readily diagnosed by measuring excretion of 5-HIAA (5-hydroxyindole acetic acid), the main metabolite of 5-HT in the urine. 5-HT receptor modulators may also have some potential in the treatment of cardiovascular system diseases, diabetes, and ocular conditions such as glaucoma. More studies in the future will guide therapeutic potential of 5-HT modulating drugs in other conditions.

Here shows part of the 5-HT receptors in human, e.g. 5-HTI (5-HT1A, 5-HT1B, 5-HTID, 5-HTIE, and 5-HT1F), 5-HT2 (5-HT2A, 5-HT2B, and 5-HT2C), 5-HT3, 5-HT4, 5-HT5 (5-HT5A, 5-HT5B), 5-HT6 and 5-HT7.

Human 5-HT Receptor Members
HTR1A HTR1B HTR1D HTR1E HTR1F HTR2A
HTR2B HTR2C HTR4 HTR5A HTR6 HTR7

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Reference

  1. Ohno Y, et al. (2015). New insight into the therapeutic role of the serotonergic system in Parkinson's disease. Prog Neurobiol. 134: 104-21.

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