5-HT2 Receptor Data

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)
Altanserin (1809)
SB 204741 (1372)
LY 272015 (3077)
N-Desmethylclozapine (1007)
RS 102221 (1050)
SB 242084 (2901)
Non-subtype Selective Antagonists Cyproheptadine (0996)
MDL 11,939 (0870)
Ritanserin (1955)
Cyproheptadine (0996)
MDL 11,939 (0870)
Ritanserin (1955)
Cyproheptadine (0996)
MDL 11,939 (0870)
Ritanserin (1955)

*partial agonist

References

Hoyer et al (1994) VII. International union of pharmacology classification of receptors for 5-hydroxytryptamine (serotonin). Pharmacol. Rev. 46 157. Barnes and Sharp (1999) A review of central 5-HT receptors and their function. Neuropharmacol. 38 1083. Pauwels (2003) 5-HT receptors and their ligands. Tocris Reviews No. 25.