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

Aided by cutting-edge Magic™ membrane protein production platform, Creative Biolabs is proud to offer the preparation of these targets in required formats using various strategies, such as detergent micelles, proteoliposomes, nanodiscs, lipoparticles, polymers, stable cell line.

Magic™ membrane protein production platform – Creative Biolabs

Meanwhile, our Magic™ membrane protein antibody discovery platform can help to discover antibodies against these targets, even fully humanized antibodies, by various approaches including hybridoma technology, phage display technology, etc. we also present DNA immunization service for anti-membrane protein antibody development. Please feel free to contact us for more information.


  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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