Target intelligence / Profile preview

5-Hydroxytryptamine Receptor 2 (5-HT2)

Target
5-HT2
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

The 5-hydroxytryptamine receptor 2 (5-HT2) is a subfamily of serotonin receptors that bind the endogenous neurotransmitter serotonin (5-HT). These receptors are GPCRs that mediate excitatory neurotransmission. The family consists of three subtypes: 5-HT2A, 5-HT2B, and 5-HT2C. They primarily couple to Gq/G11 proteins, activating PLC and leading to DAG/IP3 production and downstream effects. Key functions include mood modulation, perception regulation, and learning/memory. Abnormal activity is linked to psychiatric disorders and cardiovascular function. Both agonists and antagonists interact with these receptors, with complex pharmacology including biased agonism. Alternative splicing and RNA editing generate further diversity.

Other names
Serotonin Receptor 25-HT2 receptor
02

Mechanism of action

Agonist or antagonist binding to 5-HT2 receptors, modulating downstream signaling pathways primarily through Gq/G11 activation, leading to PLC activation, DAG/IP3 production, and PKC/Ca2+ release.

03

Biological functions

Signal transductionModulation of synaptic transmissionVasoconstrictionPlatelet aggregationMood regulationPerception regulationLearning and memory processes
04

Disease associations

DepressionSchizophreniaDrug addictionCardiovascular diseaseNeuroinflammation
05

Safety considerations

Hallucinogenic effects (agonists)Potential cardiovascular effects (vasoconstriction)Psychiatric side effects (antipsychotics/antidepressants)
06

Interacting drugs

Serotonin

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