5-HT2 Receptors

Serotonin 5-HT2 receptors are a subfamily of 5-HT receptors which bind the neurotransmitter serotonin (5-hydroxytryptamine). Three subtypes have been identified: 5-HT2A, 5-HT2B and 5-HT2C.

5-HT2 Receptor Target Files

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5-HT2A, 5-HT2B and 5-HT2C are are G-protein-coupled receptors that couple to Gq/11 causing activation of phospholipase C (PLC). PLC in turn hydrolyzes phosphatidylinositol (PIP2) to diacylglycerol (DAG) and inositol triphosphate (IP3). Localization and function of the individual receptor subtypes is summarized in the table below.

Receptor Subtype 5-HT2A 5-HT2B 5-HT2C
Transduction Mechanism ↑ PLC (Gq/11) ↑ PLC (Gq/11) ↑ PLC (Gq/11)
Primary Distribution Forebrain, caudate nucleus, nucleus accumbens, hippocampus, olfactory tubercle, vascular smooth muscle, blood platelets Brain, stomach fundus (rat), gut, heart, kidney, lung Choroid plexus, cortex, limbic system, basal ganglia
Function Neuronal depolarization, head twitch, hyperthermia, modulation of neurotransmitter release smooth muscle contraction, platelet activation Contraction of the stomach fundus, anxiety Hypolocomotion, hypophagia, penile erection, hyperthermia, anxiety, ↓ noradrenalin and dopamine release
Selective Agonists TCB-2 (2592) BW 723C86 (1059) MK 212 (0941)
Ro 60-0175 (1854)
SCH 23390 (0925)
WAY 161503 (1801)
WAY 629 (2173)
CP 809101 (3041)
1-Methylpsilocin (3017)
Non-subtype Selective Agonists PNU 22394 (2201)*
α-methyl-5-hydroxytryptamine (0557)
PNU 22394 (2201)*
α-methyl-5-hydroxytryptamine (0557)
m-CPP (0875)
PNU 22394 (2201)
α-methyl-5-hydroxytryptamine (0557)
m-CPP (0875)
Selective Antagonists R-96544 (1742)
Spiperone (0995)
4F 4PP (0523)
Risperidone (2865)
SB 204741 (1372)
LY 272015 (3077)
N-Desmethylclozapine (1007)
RS 102221 (1050)
SB 242084 (2901)
Non-subtype Selective Antagonists Altanserin (1809)
Cyproheptadine (0996)
MDL 11,939 (0870)
Ritanserin (1955)
Altanserin (1809)
Cyproheptadine (0996)
MDL 11,939 (0870)
Ritanserin (1955)
Altanserin (1809)
Cyproheptadine (0996)
MDL 11,939 (0870)
Ritanserin (1955)

*partial agonist

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