Target intelligence / Profile preview

Serotonin 5-hydroxytryptamine receptor 2A (5-HT2A receptor), Serotonin 5-hydroxytryptamine receptor 2C (5-HT2C receptor), Dopamine receptor D2 (5-HT2A, 5-HT2C, D2)

Target
5-HT2A, 5-HT2C, D2
Molecular classification
G protein-coupled receptor, Receptor, Cell surface receptor
01

Overview

Serotonin 5-HT2A and 5-HT2C receptors, and the Dopamine D2 receptor, are G protein-coupled receptors expressed in the central nervous system and peripheral tissues, each binding their respective neurotransmitters (serotonin or dopamine) to mediate key behavioral, cognitive, and physiological processes. The 5-HT2A receptor signals primarily via the phospholipase C pathway and is implicated in cognition, mood, perception, and the therapeutic and psychedelic effects of many drugs. The 5-HT2C receptor is closely related and is involved in mood, appetite, and neuroendocrine regulation. The Dopamine D2 receptor is a principal mediator of dopaminergic signaling, essential for motor control, reward, and psychosis, and is the primary target of most antipsychotic medications. Each receptor is the subject of intense pharmacological interest, with drugs acting as antagonists, agonists, or partial agonists to modulate their effects in psychiatric and neurological disease[1][4][5][6][8].

Other names
Serotonin receptor 2A5-HT2ARHTR2ASerotonin receptor 2CHTR2CDopamine D2 receptorD2RDRD2
02

Mechanism of action

Antagonists/inverse agonists block receptor-mediated signaling (antipsychotic and antidepressant properties). Agonists stimulate receptor signaling, leading to altered neurotransmission and sometimes hallucinogenic effects. Partial agonists modulate activity without full activation (D2 and 5-HT2A/C).

03

Biological functions

Signal transductionNeurotransmissionCognitive processing (learning, memory, cognition)Mood regulationMotor control (for Dopamine D2)Platelet aggregation and vasoconstriction (5-HT2A)
04

Disease associations

Neuropsychiatric disorders (schizophrenia, depression, bipolar disorder, psychosis)Neurodegenerative diseasesAddictionMovement disorders (Parkinson’s disease, dystonia)AnxietyHallucinations
05

Safety considerations

Hallucinations and psychosis with 5-HT2A agonistsExtrapyramidal symptoms and movement disorders with D2 antagonistsCardiovascular effects (e.g., QT prolongation, platelet aggregation)Metabolic syndromeWeight gainSerotonin syndromeDopaminergic toxicity in overdose
06

Interacting drugs

LSD

9 more in the full profile.

07

Biomarkers

Receptor occupancy (e.g., via PET ligands such as 25B-NBOMe for 5-HT2A)Change in expression or signaling pathway activity in patient samplesNone universally clinically validated, but research ongoing

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