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.

Targets
Literature
Receptor Data

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.

Literature for 5-HT2 Receptors

GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Secretin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling
5-HT Receptors

5-HT Receptors Scientific Review

Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.

Depression

Depression Poster

Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.

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.