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Encyclopedia > Serotonin 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 in animals and mediate the effects of serotonin as the endogenous ligand and of a broad range of pharmaceutical and recreational drugs. 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.

  • 5-HT2 receptors are Gq/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-HT4 receptor is Gs coupled, mediating cellular effects through increasing cellular levels of cAMP.
  • The 5-HT7 receptors is Gs coupled, mediating cellular effects through increasing cellular levels of cAMP.

Characterised 5-HT receptors

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

Summary of characterised 5-HT receptors, with selected agonist/antagonist agents
receptor actions agonists antagonists
5-HT1A CNS: neuronal inhibition, behavioural effects (sleep, feeding, thermoregulation, anxiety) buspirone spiperone, methiothepin, ergotamine, yohimbine
5-HT1B CNS: presynaptic inhibition, behavioural effects; vascular: pulmonary vasoconstriction ergotamine, sumatriptan methiothepin, yohimbine, metergoline
5-HT1D CNS: locomotion; vascular: cerebral vasoconstriction sumatriptan methiothepin, yohimbine, metergoline, ergotamine
5-HT2A CNS: neuronal excitation, behavioural effects; smooth muscle: contraction, vasoconstriction/dilatation; platelets: aggregation α-methyl-5-HT, LSD (CNS) ketanserin, cyproheptadine, pizotifen, LSD (PNS)
5-HT2B stomach: contraction α-methyl-5-HT, LSD (CNS) yohimbine, LSD (PNS)
5-HT2C CNS, choroid plexus: cerebrospinal fluid (CSF) secretion α-methyl-5-HT, LSD (CNS) mesulergine, LSD (PNS)
5-HT3 CNS, PNS: neuronal excitation, anxiety, emesis 2-methyl-5-HT metoclopramide (high doses), renzapride, ondansetron, alosetron
5-HT4 GIT, CNS: neuronal excitation, gastrointestinal motility 5-methoxytryptamine, metoclopramide, renzapride, tegaserod GR113808
5-ht5 CNS: unknown unknown unknown
5-ht6 CNS: unknown unknown unknown
5-HT7 CNS, GIT, blood vessels: unknown 5-carboxytryptamine, LSD methiothepin


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


External links

  • Serotonin Receptor Subtypes and Ligands (http://www.acnp.org/g4/GN401000039/Ch039.html)
  • 5-HT Receptors and their Ligands (http://www.biotrend.com/pdf/serot.pdf)
  • Basic Neurochemistry - Serotonin Receptors (http://www.ncbi.nlm.nih.gov/books/bv.fcgi?call=bv.View..ShowSection&rid=bnchm.section.963)

  Results from FactBites:
 
5-HT receptor - Wikipedia, the free encyclopedia (400 words)
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 in animals and mediate the effects of serotonin as the endogenous ligand and of a broad range of pharmaceutical and hallucinogenic drugs.
With the exception of the 5-HT 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.
DNA encoding serotonin 1C (5HT1c) receptor, isolated 5HT1c receptor, mammalian cells expressing same and uses thereof - ... (9121 words)
Serotonin receptors are also thought to be linked to the direct modification of ion channel states, and are implicated in mechanisms associated with pain, migraine headaches, and motor control.
The serotonin receptor is shown to belong to the family of rhodopsin-like signal transducers which are distinguished by their seven-transmembrane configuration and their functional linkage to G-proteins.
Receptor RNA was not detected in the cerebellum or in liver, kidney, intestine, heart, and lung.
  More results at FactBites »

 
 

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