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5-HT1E receptor

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Title: 5-HT1E receptor  
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Subject: 5-HT1 receptor, BRL-54443, Serotonin, 5-HT5A receptor, 5-HT2B receptor
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5-HT1E receptor

5-hydroxytryptamine (serotonin) receptor 1E, G protein-coupled
Identifiers
Symbols  ; 5-HT1E
External IDs IUPHAR: ChEMBL: GeneCards:
RNA expression pattern
Orthologs
Species Human Mouse
Entrez n/a
Ensembl n/a
UniProt n/a
RefSeq (mRNA) n/a
RefSeq (protein) n/a
Location (UCSC) n/a
PubMed search n/a

5-hydroxytryptamine (serotonin) 1E receptor (5-HT1E) is a highly expressed human G-protein coupled receptor[1] that belongs to the 5-HT1 receptor family (Gi-coupled serotonin receptor).[2][3] The human gene is denoted as HTR1E.[4]

Function

The function of the 5-HT1E receptor is unknown due to the lack of selective pharmacological tools, specific antibodies, and permissive animal models.[5] The 5-HT1E receptor gene lacks polymorphisms amongst humans (few mutations), indicating a high degree of evolutionary conservation of genetic sequence, which suggests that the 5-HT1E receptor has an important physiological role in humans.[6] It is hypothesized that the 5-HT1E receptor is involved in the regulation of memory in humans due to the high abundance of receptors in the frontal cortex, hippocampus, and olfactory bulb, all of which are regions of the brain integral to memory regulation.[7]

This receptor is unique among the serotonin receptors in that it is not known to be expressed by rats or mouse species, all of which lack the gene encoding the 5-HT1E receptor. However the genomes of the pig, rhesus monkey, and several lagomorphs (including rabbit) as well as the guinea pig each encode a homologous 5-HT1E receptor gene.[7] The guinea pig is the most likely candidate for future study of 5-HT1E receptor function in vivo. The expression of 5-HT1E receptors in the guinea pig brain has been pharmacologically confirmed; 5-HT1E receptor expression patterns of the human and guinea pig brains appear to be similar.[5] In the human cortex, the expression of 5-HT1E undergoes a marked transition during adolescence, in a way that is strongly correlated with the expression of 5-HT1B. [8]


The most closely related receptor to the 5-HT1E is the 5-HT1F receptor. They share 57% amino acid sequence homology and have some pharmacological characteristics in common.[9] Both receptors are Gi-coupled (inhibit adenylate cyclase activity) and both receptors have high affinities for 5-HT and low affinities for 5-carboxyamidotryptaine and mesulergine.[10] However, due to major differences in brain expression patters, these receptors are unlikely to mediate similar functions in humans. For example, 5-HT1E receptors are abundant in the hippocampus but are not detectable in the striatum (caudate and putamen of the human brain), while the opposite is true for the 5-HT1F receptor. Thus, conclusions about the function of the 5-HT1E receptor cannot be ascribed to the function of the 5-HT1F receptor, and vice versa.[5]

Selective ligands

No highly selective 5-HT1E ligands are available yet. [3H]5-HT remains the only radioligand available with high affinity for the 5-HT1E receptor (5nM).

Agonists

  • BRL-54443 (5-Hydroxy-3-(1-methylpiperidin-4-yl)-1H-indole) - mixed 5-HT1E/1F agonist

Antagonists

None as yet.

See also

References

  1. ^ Leonhardt S., Herrick-Davis K. and Titeler M. (1989) Detection of a novel serotonin receptor subtype (5-HT1E) in human brain: interaction with a GTP-binding protein. Journal of neurochemistry 53, 465-471. (1989). "Detection of a novel serotonin receptor subtype (5-HT1E) in human brain: interaction with a GTP-binding protein.". Journal of Neurochemistry 53 (2): 465–71.  
  2. ^ McAllister G., Charlesworth A., Snodin C., Beer M. S., Noble A. J., Middlemiss D. N., Iversen L. L. and Whiting P. (1992) Molecular cloning of a serotonin receptor from human brain (5HT1E): a fifth 5HT1-like subtype. Proceedings of the National Academy of Sciences of the United States of America 89, 5517-5521. (1992). "Molecular cloning of a serotonin receptor from human brain (5HT1E): a fifth 5HT1-like subtype". Proceedings of the National Academy of Sciences of the United States of America 89 (12): 5517–21.  
  3. ^ Levy F. O., Gudermann T., Birnbaumer M., Kaumann A. J. and Birnbaumer L. (1992) Molecular cloning of a human gene (S31) encoding a novel serotonin receptor mediating inhibition of adenylyl cyclase. FEBS Lett 296, 201-206. (1994). "Assignment of the gene encoding the 5-HT1E serotonin receptor (S31) (locus HTR1E) to human chromosome 6q14-q15". Genomics 22 (3): 637–40.  
  4. ^ "Entrez Gene: HTR1E 5-hydroxytryptamine (serotonin) receptor 1E". 
  5. ^ a b c Klein, M. T., and M. Teitler. "Guinea Pig Hippocampal 5-Htie Receptors: A Tool for Selective Drug Development." J Neurochem 109, no. 1 (2009): 268-74. (2009). "Guinea pig hippocampal 5-HT1E receptors: a tool for selective drug development". Journal of Neurochemistry 109 (1): 268–74.  
  6. ^ Shimron-Abarbanell D., Nothen M. M., Erdmann J. and Propping P. (1995) Lack of genetically determined structural variants of the human serotonin-1E (5-HT1E) receptor protein points to its evolutionary conservation. Brain Res Mol Brain Res 29, 387-390. (1995). "Lack of genetically determined structural variants of the human serotonin-1E (5-HT1E) receptor protein points to its evolutionary conservation". Brain research. Molecular brain research 29 (2): 387–90.  
  7. ^ a b Bai F., Yin T., Johnstone E. M., Su C., Varga G., Little S. P. and Nelson D. L. (2004) Molecular cloning and pharmacological characterization of the guinea pig 5-HT1E receptor. European journal of pharmacology 484, 127-139. (2004). "Molecular cloning and pharmacological characterization of the guinea pig 5-HT1E receptor". European Journal of Pharmacology 484 (2–3): 127–39.  
  8. ^ Shoval, G., Bar-Shira O., Zalsman G., John J. Mann and Chechik G. (2014) Transitions in the transcriptome of the serotonergic and dopaminergic systems in the human brain during adolescence. European Neuropsychopharmacology. (2014). "Transitions in the transcriptome of the serotonergic and dopaminergic systems in the human brain during adolescence". European neuropsychopharmacology 24 (7): 1123–32.  
  9. ^ Barnes N. M. and Sharp T. (1999) A review of central 5-HT receptors and their function. Neuropharmacology 38, 1083-1152. (1999). "A review of central 5-HT receptors and their function". Neuropharmacology 38 (8): 1083–152.  
  10. ^ Adham N., Kao H. T., Schecter L. E., Bard J., Olsen M., Urquhart D., Durkin M., Hartig P. R., Weinshank R. L. and Branchek T. A. (1993) Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase. Proceedings of the National Academy of Sciences of the United States of America 90, 408-412. (1993). "Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase". Proceedings of the National Academy of Sciences of the United States of America 90 (2): 408–12.  

External links

  • "1e"5-HT. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. 

Further reading

This article incorporates text from the United States National Library of Medicine, which is in the public domain.


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