5-HT receptor

In the field of neurochemistry, 5-HT receptors are receptors for the neurotransmitter and peripheral signal mediator serotonin, also known as 5-hydroxytryptamine or 5-HT. 5-HT receptors are located on the cell membrane of nerve cells and other cell types including smooth muscle in animals, and mediate the effects of serotonin as the endogenous ligand and of a broad range of pharmaceutical and hallucinogenic drugs. All 5-HT receptors reduce cyclic adenosine monophosphate (cAMP).

Classification

With the exception of the 5-HT₃ receptor, a ligand gated ion channel, all other 5-HT receptors are G protein coupled seven transmembrane (or heptahelical) receptors that activate an intracellular second messenger cascade.

Families

5-HT1 receptors are G_i/G_o coupled, mediating cellular effects through decreasing cellular levels of cyclic adenosine monophosphate (cAMP).

5-HT2 receptors are G_q/G₁₁ coupled, mediating cellular effects through increasing cellular levels of inositol trisphosphate (IP3) and diacylglycerol (DAG). Three subtypes exist, namely 5-HT2A, 5-HT2B, and 5-HT2C (formerly called 5-HT1C).

The 5-HT3 receptor is a ligand-gated Na⁺ and K⁺ cation channel, resulting in a direct plasma membrane depolarization.

The 5-HT4 receptor is G_s coupled, mediating cellular effects through increasing cellular levels of cAMP.

The 5-HT5A receptor is G protein coupled; the primary coupling appears to be through Gi/o, inhibiting adenylate cyclase activity.^[1] The 5-HT5B subtype exists, but has not been detected in humans.

The 5-HT7 receptor is G_s coupled, mediating cellular effects through increasing cellular levels of cAMP.

Specific proteins/genes

Within these general classes of 5-HT receptors, a number of specific types have been characterized:

Note that there is no 5-HT1C receptor since, after the receptor was cloned and further characterized, it was found to have more in common with the 5-HT2 family of receptors and was redesignated as the 5-HT2C receptor.

Therapeutic modulation

Various drugs are used to modulate the 5-HT system including some antidepressants, anxiolytics, antiemetics, antipsychotics and anti-migraine agents.

External links

IUPHAR GPCR Database - 5-HT Receptors
Serotonin Receptor Subtypes and Ligands by R.A. Glennon, 2000
G Protein-Coupled Receptor Activation of 5-HT2A and other GPCRs. A hypothetical model of how these receptors work by L.A. Rubenstein, 1997
Basic Neurochemistry - Serotonin Receptors (published 1999)
http://www.if-pan.krakow.pl/pjp/pdf/2002/4_327.pdf, Wesołowska A, In the search for selective ligands of 5-HT5, 5-HT6 and 5-HT7 serotonin receptors, Polish journal of pharmacology, Vol. 54, No. 4, pp. 327-41, 2002, 12523486.

Citations

[1] D.L. Nelson, 5-HT5 receptors, Curr. Drug Targets CNS Neurol. Disord., Vol. 3, No. 1, pp. 53-58, 2004, No. PMID 14965244.

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