5-HT1E receptor

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5-HT1E serotoninski receptor
Identifikatori
SimboliHTR1E; 5-HT1E
Vanjski IDOMIM182132 HomoloGene55491 IUPHAR: 5-ht1e GeneCards: HTR1E Gene
Pregled RNK izražavanja
podaci
Ortolozi
VrstaČovekMiš
Entrez3354n/a
EnsemblENSG00000168830n/a
UniProtP28566n/a
RefSeq (mRNA)NM_000865n/a
RefSeq (protein)NP_000856n/a
Lokacija (UCSC)Chr 6:
87.7 - 87.78 Mb
n/a
PubMed pretraga[1]n/a

5-HT1E receptor, (5-hidroksitriptaminski (serotoninski) 1E receptor, 5-HT1E) je visoko izraženi humani G-protein spregnuti receptor[1] koji pripada familiji 5-HT1 receptora (Gi-spregnutih serotoninskih receptora).[2][3] Humani gen se označava sa HTR1E.[4]

Funkcija[uredi | uredi kod]

Funkcija 5-HT1E receptora nije poznata usled nedostatka selektivnih farmakoloških oruđa, specifičnih antitela, i podobnih životinjskih modela.[5] Gen 5-HT1E receptora nema polimorfizama među ljudima (mali je broj mutacija), što je indikacija visokog nivoa evolucione konzervacije njegove genetičke sekvence, iz čega sledi da 5-HT1E receptor ima važnu fiziološku ulogu kod ljudi.[6] Pretpostavlja se da 5-HT1E receptor učestvuje u regulaciji memorije kod ljudi, zbog zbog visoke zastupljenosti ovog receptora u frontalnom korteksu, hipokampusu, i bulbus olfactorius, što su integralni moždani regioni za regulaciju memorije.[7]

Ovaj receptor je jedinstven među serotoninskim receptorima po tome što nije izražen kod glodarskih vrsta. Tim vrstama nedostaje gen koji kodira 5-HT1E receptor. Međutim genomi svinje, rezus majmuna, i nekoliko lagomorfa (što obuhvata morsko prase i zeca) sadrže homologne 5-HT1E gene.[7] Morsko prase je najverovatniji kandidat za buduća ispitivanja funkcije 5-HT1E receptor in vivo. Izražavanje 5-HT1E receptora u mozgu morskog praseta je farmakološki potvrđeno. Obrasci izražavanja 5-HT1E receptora u mozgu ljudi i morskog praseta su slični.[5]

Selektivni ligandi[uredi | uredi kod]

Visoko selektivni ligandi 5-HT1E još uvek nisu dostupni. [3H]5-HT je jedini dostupni radioligand visokog afinita za 5-HT1E receptor (5 nM).

Agonisti[uredi | uredi kod]

  • BRL-54443 (5-Hidroksi-3-(1-metilpiperidin-4-il)-1H-indol) - mešoviti 5-HT1E/1F agonist

Antagonisti[uredi | uredi kod]

Antagonisti nisu poznati.

Vidi još[uredi | uredi kod]

Reference[uredi | uredi kod]

  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. DOI:10.1111/j.1471-4159.1989.tb07357.x. PMID 2664084. 
  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. DOI:10.1073/pnas.89.12.5517. PMC 49323. PMID 1608964. 
  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. DOI:10.1006/geno.1994.1439. PMID 8001977. 
  4. „Entrez Gene: HTR1E 5-hydroxytryptamine (serotonin) receptor 1E”. 
  5. 5,0 5,1 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-HT(1E) receptors: a tool for selective drug development.”. Journal of neurochemistry 109 (1): 268–74. DOI:10.1111/j.1471-4159.2009.05958.x. PMC 2827198. PMID 19200348. 
  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. DOI:10.1016/0169-328X(95)00003-B. PMID 7609628. 
  7. 7,0 7,1 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. DOI:10.1016/j.ejphar.2003.11.019. PMID 14744596. 

Literatura[uredi | uredi kod]

Spoljašnje veze[uredi | uredi kod]

  • „5-HT1e. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Arhivirano iz originala na datum 2016-03-04.