5-HT1E receptor

5-HT1E receptor, (5-hidroksitriptaminski (serotoninski) 1E receptor, 5-HT_1E) je visoko izraženi humani G-protein spregnuti receptor^[1] koji pripada familiji 5-HT1 receptora (G_i-spregnutih serotoninskih receptora).^[2][3] Humani gen se označava sa HTR1E.^[4]

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5-HT1E serotoninski receptor
Identifikatori
Simboli	HTR1E; 5-HT1E
Vanjski ID	OMIM: 182132 HomoloGene: 55491 IUPHAR: 5-ht1e GeneCards: HTR1E Gene
Ontologija gena Molekularna funkcija • aktivnost rodopsinu-sličnog receptora • receptorska aktivnost • aktivnost serotoninskog receptora Celularna komponenta • integralno sa ćelijskom membranom • membrana Biološki proces • prenos signala • G-proteinska signalizacija, spregnuta sa cikličnim nukleotidnim sekundarnim glasnikom • sinaptička transmisija
Pregled RNK izražavanja
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		n/a

Funkcija

Funkcija 5-HT_1E receptora nije poznata usled nedostatka selektivnih farmakoloških oruđa, specifičnih antitela, i podobnih životinjskih modela.^[5] Gen 5-HT_1E receptora nema polimorfizama među ljudima (mali je broj mutacija), što je indikacija visokog nivoa evolucione konzervacije njegove genetičke sekvence, iz čega sledi da 5-HT_1E receptor ima važnu fiziološku ulogu kod ljudi.^[6] Pretpostavlja se da 5-HT_1E 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-HT_1E receptor. Međutim genomi svinje, rezus majmuna, i nekoliko lagomorfa (što obuhvata morsko prase i zeca) sadrže homologne 5-HT_1E gene.^[7] Morsko prase je najverovatniji kandidat za buduća ispitivanja funkcije 5-HT_1E receptor in vivo. Izražavanje 5-HT_1E receptora u mozgu morskog praseta je farmakološki potvrđeno. Obrasci izražavanja 5-HT_1E receptora u mozgu ljudi i morskog praseta su slični.^[5]

Selektivni ligandi

Visoko selektivni ligandi 5-HT_1E još uvek nisu dostupni. [³H]5-HT je jedini dostupni radioligand visokog afinita za 5-HT_1E receptor (5 nM).

Agonisti

• BRL-54443 (5-Hidroksi-3-(1-metilpiperidin-4-il)-1H-indol) - mešoviti 5-HT_1E/1F agonist

Antagonisti

Antagonisti nisu poznati.

Povezano

• 5-HT₁ receptor
• 5-HT receptor

Reference

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. 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. 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-HT_1e”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Arhivirano iz originala na datum 2016-03-04.