Target intelligence / Profile preview

Serotonin 2 Receptor (5-HT2 Receptor)

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

Overview

The serotonin 2 receptor (5-HT2 receptor) is a G protein-coupled receptor that plays key roles in neurotransmission and various physiological processes. It is comprised of three main subtypes: 5-HT2A, 5-HT2B, and 5-HT2C receptors. These receptors are involved in cognition, mood regulation, cardiac function, appetite control, and vasoconstriction. Drugs targeting this receptor family include psychedelics, antidepressants, and antipsychotics. Abnormalities in 5-HT2 receptor function are associated with psychiatric conditions such as depression, schizophrenia, and addiction, as well as cardiovascular side effects.

Other names
5-Hydroxytryptamine 2 Receptor
02

Mechanism of action

Agonists (e.g., LSD, psilocybin) stimulate the receptor. Antagonists (e.g., atypical antipsychotics) block the receptor. Activation leads to stimulation of phospholipase C (PLC), resulting in increased production of IP₃/DAG, intracellular calcium release, and activation of protein kinase C. Chronic administration of SSRIs and atypical antipsychotics leads to adaptive downregulation.

03

Biological functions

NeurotransmissionSignal transductionCognitionMood regulationVasoconstrictionInflammationWound healingAppetite controlCardiac function
04

Disease associations

DepressionSchizophreniaAddictionCardiovascular diseaseSuicidality
05

Safety considerations

Cardiovascular side effects (drug-induced valvulopathy)Hallucinogenic effects (agonists)Psychiatric side effects
06

Interacting drugs

LSD

3 more in the full profile.

07

Biomarkers

Post-synaptic receptor density (altered in depression)

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