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Serotonin Receptors (5-hydroxytryptamine receptors) (5-HT receptors)

Target
5-HT receptors
Molecular classification
G protein-coupled receptor (GPCR) superfamily, Ligand-gated ion channel, 5-HT1 receptor family, 5-HT2 receptor family, 5-HT3 receptor family, 5-HT4 receptor family, 5-HT5 receptor family, 5-HT6 receptor family, 5-HT7 receptor family
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Overview

Serotonin receptors, also known as 5-hydroxytryptamine receptors (5-HT receptors), are a family of receptors that bind the neurotransmitter serotonin and mediate its diverse effects. They are classified into seven main families (5-HT1 through 5-HT7) with 14-15 known subtypes. Most are G protein-coupled receptors (GPCRs), while the 5-HT3 receptor is a unique ligand-gated ion channel. Widely expressed in the Central Nervous System (CNS) and peripheral tissues, these receptors play crucial roles in neurological, cardiovascular, and gastrointestinal functions. They are implicated in various conditions including anxiety, depression, schizophrenia, migraine, and obesity, making them important therapeutic targets for a range of psychiatric and other disorders.

Other names
5-HT receptors5-hydroxytryptamine receptors
02

Mechanism of action

Drugs act as agonists or antagonists to modulate the activity of specific serotonin receptor subtypes, thereby influencing downstream signaling pathways. GPCR-coupled receptors (5-HT1, 5-HT2, 5-HT4, 5-HT5, 5-HT6, 5-HT7) alter intracellular cAMP or IP3/DAG levels, leading to inhibitory or excitatory effects. The 5-HT3 receptor, a ligand-gated ion channel, causes membrane depolarization. As stated in the text, Selective Serotonin Reuptake Inhibitors (SSRIs) are common antidepressants that act by targeting the 5-HT1A receptor.

03

Biological functions

Neuro-inhibitionNeuro-excitationPlatelet activationVascular smooth muscle contractionGastrointestinal smooth muscle contractionNO-dependent vasorelaxationCSF volume regulationCognitive processesLearningMemory
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Disease associations

Anxiety-like behaviorsDepressionCognitive impairment in psychiatric disordersSchizophreniaMigraineIrritable bowel syndromeObesity
05

Interacting drugs

8-OH-DPAT

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