5-HT1E receptor
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5-HT1E serotoninski receptor | |||||||||||
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Identifikatori | |||||||||||
Simboli | HTR1E; 5-HT1E | ||||||||||
Vanjski ID | OMIM: 182132 HomoloGene: 55491 IUPHAR: 5-ht1e GeneCards: HTR1E Gene | ||||||||||
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Pregled RNK izražavanja | |||||||||||
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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
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
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
- BRL-54443 (5-Hidroksi-3-(1-metilpiperidin-4-il)-1H-indol) - mešoviti 5-HT1E/1F agonist
Antagonisti
Antagonisti nisu poznati.
Povezano
- 5-HT1 receptor
- 5-HT receptor
Reference
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ „Entrez Gene: HTR1E 5-hydroxytryptamine (serotonin) receptor 1E”.
- ↑ 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.
- ↑ 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.
- ↑ 7,0 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
- 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. DOI:10.1073/pnas.89.12.5517. PMC 49323. PMID 1608964.
- 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. DOI:10.1016/0014-5793(92)80379-U. PMID 1733778.
- 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. DOI:10.1006/geno.1994.1439. PMID 8001977.
- 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. DOI:10.1016/S0306-4522(97)00235-2. PMID 9316030.
Spoljašnje veze
- „5-HT1e”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Arhivirano iz originala na datum 2016-03-04.
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