5-HT Receptor

Serotonin (5-hydroxytryptamine, 5-HT) produces its effects through a variety of membrane-bound receptors. 5-HT and its receptors are found both in the central and peripheral nervous system (CNS/PNS), as well as in a number of nonneuronal tissues in the gut, cardiovascular system and blood. 5-HT has been implicated in the aetiology of numerous disease states, including depression, anxiety, social phobia, schizophrenia, obsessive-compulsive and panic disorders; in addition to migraine, hypertension, pulmonary hypertension, eating disorders, vomiting and irritable bowel syndrome.

AS 19
(±)-MDL 105725
Sumatriptan Succinate


An Overview of 5-HT Receptor

5-hydroxytryptamine (5-HT), also known as serotonin, is a heterocyclic amine that participates in the regulation of various physiological functions and pathological states in the brain, and is a substance that plays an absolute role in the process of emotional regulation in the brain. The role of 5-HT in the brain is closely related to the distribution of 5-HT neurons in the central and peripheral nerves and a large number of different types of 5-HT Receptor (5-HTR). At present, there are seven types of 5-HTR, some of which can be divided into several subtypes. Except that 5-HT3R belongs to ligand gated cationic channel, the other receptor subtypes belong to G protein-coupled receptor superfamily. 5-HTR mediates a variety of physiological functions, including regulation of emotion, in which 5-H1AR, 5-HT2AR, 5-HT2CR, 5-H3R and 5-HT7R are closely related to depression.

Agonist of 5-HT Receptor

There are few studies on 5-HTR agonists. Several known high-energy and highly selective receptor agonists include: 2-methyl-5-hydroxytryptamine, m-chlorobenzene biguanidine (m-CPBG), 2,3,5-trichlorobenzene biguanidine, 3, 4, 5- trichlorobenzene biguanidine, YM31636 / SR57227 / S21007, 5-chloro-7-methyl-2- (4-methyl-1-piperazinyl) benzazole, et al.

5-HT Receptor and Diseases

The etiology of depression is complex and the pathogenesis of depression is not clear. It is found that there is a great relationship between 5-HT and serotonin receptor 5-HTR depression. The number of 5-HTR in the brain of depression patients is lower than that of normal persons, and the receptor sensitivity is significantly decreased. At present, the researches on the correlation between 5-HTR and depression are mainly focused on the feedback regulation of 5-HTR and the inhibition of neurotransmitter metabolism. Moreover, 5-HT3R / 5HT6R / 5-HT7R and other receptor antagonists were used to study the relationship between the receptor antagonist and depression. More further studies are needed to analyze how monoamine neurotransmitters and their receptors affect neurogenesis and neural plasticity by regulating neurotrophic factors, and how changes in the genetic environment affect the pathogenesis of the disease.


Zhang Yongchao, Huang Shijing. A. (2014). Research progress on the relationship between serotonin receptor and depression. Medical Recapitulate. 20(05);772-775