5-HT1E receptor

Из Википедије, слободне енциклопедије
5-HT1E serotoninski receptor
Identifikatori
Simboli HTR1E; 5-HT1E
Vanjski ID OMIM182132 HomoloGene55491 IUPHAR: 5-ht1e GeneCards: HTR1E Gene
Pregled RNK izražavanja
PBB GE HTR1E 207404 s at tn.png
podaci
Ortolozi
Vrsta Čovek Miš
Entrez 3354 n/a
Ensembl ENSG00000168830 n/a
UniProt P28566 n/a
RefSeq (mRNA) NM_000865 n/a
RefSeq (protein) NP_000856 n/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[уреди]

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[уреди]

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[уреди]

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

Antagonisti[уреди]

Antagonisti nisu poznati.

Vidi još[уреди]

Literatura[уреди]

  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. PMID 2664084. doi:10.1111/j.1471-4159.1989.tb07357.x. 
  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. PMC 49323Слободан приступ. PMID 1608964. doi:10.1073/pnas.89.12.5517. 
  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. PMID 8001977. doi:10.1006/geno.1994.1439. 
  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. PMC 2827198Слободан приступ. PMID 19200348. doi:10.1111/j.1471-4159.2009.05958.x. 
  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. PMID 7609628. doi:10.1016/0169-328X(95)00003-B. 
  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. PMID 14744596. doi:10.1016/j.ejphar.2003.11.019. 

Dodatna literatura[уреди]

  • Zgombick JM; Schechter LE; Macchi M; et al. (1992). „Human gene S31 encodes the pharmacologically defined serotonin 5-hydroxytryptamine1E receptor.”. Mol. Pharmacol. 42 (2): 180—5. PMID 1513320. 
  • McAllister G; Charlesworth A; Snodin C; et al. (1992). „Molecular cloning of a serotonin receptor from human brain (5HT1E): a fifth 5HT1-like subtype.”. Proc. Natl. Acad. Sci. U.S.A. 89 (12): 5517—21. PMC 49323Слободан приступ. PMID 1608964. doi:10.1073/pnas.89.12.5517. 
  • Levy FO; Gudermann T; Birnbaumer M; et al. (1992). „Molecular cloning of a human gene (S31) encoding a novel serotonin receptor mediating inhibition of adenylyl cyclase.”. FEBS Lett. 296 (2): 201—6. PMID 1733778. doi:10.1016/0014-5793(92)80379-U. 
  • Levy FO; Holtgreve-Grez H; Taskén K; et al. (1995). „Assignment of the gene encoding the 5-HT1E serotonin receptor (S31) (locus HTR1E) to human chromosome 6q14-q15.”. Genomics. 22 (3): 637—40. PMID 8001977. doi:10.1006/geno.1994.1439. 
  • Pierce PA, Xie GX, Meuser T, Peroutka SJ (1997). „5-Hydroxytryptamine receptor subtype messenger RNAs in human dorsal root ganglia: a polymerase chain reaction study.”. Neuroscience. 81 (3): 813—9. PMID 9316030. doi:10.1016/S0306-4522(97)00235-2. 

Spoljašnje veze[уреди]

  • „5-HT1e. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.