5-HT4 receptor
(Preusmjereno sa stranice 5-HT4)
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| 5-hidroksitriptaminski (serotoninski) receptor 4 | |||||||||||
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| Identifikatori | |||||||||||
| Simboli | HTR4; 5-HT4; 5-HT4R | ||||||||||
| Vanjski ID | OMIM: 602164 MGI: 109246 HomoloGene: 20243 IUPHAR: 5-HT4 GeneCards: HTR4 Gene | ||||||||||
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| Pregled RNK izražavanja | |||||||||||
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| podaci | |||||||||||
| Ortolozi | |||||||||||
| Vrsta | Čovek | Miš | |||||||||
| Entrez | 3360 | 15562 | |||||||||
| Ensembl | ENSG00000164270 | ENSMUSG00000026322 | |||||||||
| UniProt | Q13639 | Q3URB5 | |||||||||
| RefSeq (mRNA) | NM_000870 | NM_008313 | |||||||||
| RefSeq (protein) | NP_000861 | NP_032339 | |||||||||
| Lokacija (UCSC) | Chr 5: 147.81 - 148.01 Mb | Chr 18: 62.45 - 62.59 Mb | |||||||||
| PubMed pretraga | [1] | [2] | |||||||||
5-HT4 receptor (5-hidroksitriptaminski receptor 4) je protein koji je kod ljudi kodiran HTR4 genom.[1][2]
Ovaj gen je član familije serotoninskih receptora, koji su G protein spregnuti receptori koji stimulišu cAMP produkciju u responsu na vezivanje serotonina (5-hidroksitriptamina). To je glikolizirani transmembranski protein koji funkcioniše u perifernom i centralnom nervnom sistemu gde modulara otpuštanje raznih neurotransmitera. Postoji više transkriptnih varijanti koje kodiraju proteine sa distinktnim C-terminalnim sekvencama.[3]
Lokacija[uredi | uredi kod]
Receptor je lociran u alimentarnom traktu, mokraćnoj bešiki, srcu i nadbubrežnoj žlezdi, kao i u centralnom nervnom sistemu (CNS).[4] On nije nađen u cerebelumu.[5]
Izoforme[uredi | uredi kod]
Internalizacija je specifična za pojedine izoforme.[6]
Ligandi[uredi | uredi kod]
Postoji nekoliko lekova kaji deluju na 5-HT4 kao selektivni agonisti. Oni se koriste u naučnim istraživanjima i kliničkoj medicini. Neki od lekova koji deluju kao 5-HT4 agonisti su isto tako aktivni kao 5-HT3 antagonisti, npr, mosaprid, metoclopramid, renzaprid i zacoprid.[7] SB-207,145 radio obeležen sa ugljenikom-11 se koristi kao radioligand za 5-HT4 ispitivanja pozitronskom emisionom tomografijom na životinjama[8] i u humanim ispitivanjima.[9].
2
Vidi još[uredi | uredi kod]
Reference[uredi | uredi kod]
- ↑ Claeysen S, Faye P, Sebben M, Lemaire S, Bockaert J, Dumuis A, Taviaux S (December 1997). „Assignment of 5-hydroxytryptamine receptor (HTR4) to human chromosome 5 bands q31→q33 by in situ hybridization.”. Cytogenet Cell Genet 78 (2): 133–4. DOI:10.1159/000134646. PMID 9371406.
- ↑ , Blondel O, Vandecasteele G, Gastineau M, Leclerc S, Dahmoune Y, Langlois M, Fischmeister R (September 1997). „Molecular and functional characterization of a 5-HT4 receptor cloned from human atrium.”. FEBS Lett 412 (3): 465–74. DOI:10.1016/S0014-5793(97)00820-X. PMID 9276448.
- ↑ „Entrez Gene: HTR4 5-hydroxytryptamine (serotonin) receptor 4”.
- ↑ S. S. Hegde, R. M. Eglen (1996-01-10). „Peripheral 5-HT4 receptors”. The FASEB journal 10 (12): 1398–1407. PMID 8903510.
- ↑ Katarina Varnäs, Christer Halldin, Victor W. Pike, Håkan Hall (2003). „Distribution of 5-HT4 receptors in the postmortem human brain–an autoradiographic study using [125]SB 207710”. European Neuropsychopharmacology 13: 228–234. DOI:10.1016/S0924-977X(03)00009-9.
- ↑ PMID 19922792
- ↑ Pellissier LP, Sallander J, Campillo M, Gaven F, Queffeulou E, Pillot M, Dumuis A, Claeysen S, Bockaert J, Pardo L (April 2009). „Conformational toggle switches implicated in basal constitutive and agonist-induced activated states of 5-hydroxytryptamine-4 receptors”. Molecular Pharmacology 75 (4): 982–90. DOI:10.1124/mol.108.053686. PMID 19168624.
- ↑ B. R. Kornum, N. M. Lind, N. Gillings, Lisbeth Marner, F. Andersen, Gitte Moos Knudsen (September 2008). „Evaluation of the novel 5-HT(4) receptor PET ligand [(11)C]SB207145 in the Gottingen minipig”. Journal of Cerebral Blood Flow and Metabolism 29 (1): 186. DOI:10.1038/jcbfm.2008.110. PMID 18797470.
- ↑ Lisbeth Marner, Nic Gillings, Roger Gunn, Robert Comley, William Baaré, Steen Hasselbalch and Gitte Knudsen (2008-01-05). „Quantification of 11C-SB207145-PET for 5-HT4 receptors in the human brain: Preliminary results”. Journal of Nuclear Medicine 48 (Supplement 2) (Supplement 2): 159P. Arhivirano iz originala na datum 2016-03-03. Pristupljeno 2014-05-02.
- ↑ Gale JD, Grossman CJ, Whitehead, JW Oxford AW, Bunce KT, Humphrey PP (1994). „GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor.”. British journal of pharmacology 111 (1): 332–8. PMC 1910004. PMID 8012715.
- ↑ Xu R, Hong J, Morse CL, Pike VW (2010-10-14). „Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography”. J Med Chem 53 (19): 7035-47. PMID 20812727.
Literatura[uredi | uredi kod]
- Cecilie Löe Licht, Changes in the 5-HT4 receptor in animal models of depression and antidepressant treatment, PhD thesis, Faculty of Health Sciences, University of Copenhagen. Submitted 2008 October.
- Ullmer C, Schmuck K, Kalkman HO, Lübbert H (1995). „Expression of serotonin receptor mRNAs in blood vessels.”. FEBS Lett. 370 (3): 215–21. DOI:10.1016/0014-5793(95)00828-W. PMID 7656980.
- Blondel O, Vandecasteele G, Gastineau M, et al. (1997). „Molecular and functional characterization of a 5-HT4 receptor cloned from human atrium.”. FEBS Lett. 412 (3): 465–74. DOI:10.1016/S0014-5793(97)00820-X. PMID 9276448.
- Van den Wyngaert I, Gommeren W, Verhasselt P, et al. (1997). „Cloning and expression of a human serotonin 5-HT4 receptor cDNA.”. J. Neurochem. 69 (5): 1810–9. DOI:10.1046/j.1471-4159.1997.69051810.x. PMID 9349523.
- Claeysen S, Faye P, Sebben M, et al. (1997). „Cloning and expression of human 5-HT4S receptors. Effect of receptor density on their coupling to adenylyl cyclase.”. Neuroreport 8 (15): 3189–96. DOI:10.1097/00001756-199710200-00002. PMID 9351641.
- Blondel O, Gastineau M, Dahmoune Y, et al. (1998). „Cloning, expression, and pharmacology of four human 5-hydroxytryptamine 4 receptor isoforms produced by alternative splicing in the carboxyl terminus.”. J. Neurochem. 70 (6): 2252–61. DOI:10.1046/j.1471-4159.1998.70062252.x. PMID 9603189.
- Cichon S, Kesper K, Propping P, Nöthen MM (1998). „Assignment of the human serotonin 4 receptor gene (HTR4) to the long arm of chromosome 5 (5q31-q33).”. Mol. Membr. Biol. 15 (2): 75–8. DOI:10.3109/09687689809027521. PMID 9724925.
- Claeysen S, Sebben M, Becamel C, et al. (1999). „Novel brain-specific 5-HT4 receptor splice variants show marked constitutive activity: role of the C-terminal intracellular domain.”. Mol. Pharmacol. 55 (5): 910–20. PMID 10220570.
- Bender E, Pindon A, van Oers I, et al. (2000). „Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant.”. J. Neurochem. 74 (2): 478–89. DOI:10.1046/j.1471-4159.2000.740478.x. PMID 10646498.
- Mialet J, Berque-Bestel I, Eftekhari P, et al. (2000). „Isolation of the serotoninergic 5-HT4(e) receptor from human heart and comparative analysis of its pharmacological profile in C6-glial and CHO cell lines.”. Br. J. Pharmacol. 129 (4): 771–81. DOI:10.1038/sj.bjp.0703101. PMC 1571890. PMID 10683202.
- Bach T, Syversveen T, Kvingedal AM, et al. (2001). „5HT4(a) and 5-HT4(b) receptors have nearly identical pharmacology and are both expressed in human atrium and ventricle.”. Naunyn Schmiedebergs Arch. Pharmacol. 363 (2): 146–60. DOI:10.1007/s002100000299. PMID 11218067.
- Medhurst AD, Lezoualc'h F, Fischmeister R, et al. (2001). „Quantitative mRNA analysis of five C-terminal splice variants of the human 5-HT4 receptor in the central nervous system by TaqMan real time RT-PCR.”. Brain Res. Mol. Brain Res. 90 (2): 125–34. DOI:10.1016/S0169-328X(01)00095-X. PMID 11406291.
- Hiroi T, Hayashi-Kobayashi N, Nagumo S, et al. (2002). „Identification and characterization of the human serotonin-4 receptor gene promoter.”. Biochem. Biophys. Res. Commun. 289 (2): 337–44. DOI:10.1006/bbrc.2001.5979. PMID 11716477.
- Vilaró MT, Doménech T, Palacios JM, Mengod G (2002). „Cloning and characterization of a novel human 5-HT4 receptor variant that lacks the alternatively spliced carboxy terminal exon. RT-PCR distribution in human brain and periphery of multiple 5-HT4 receptor variants.”. Neuropharmacology 42 (1): 60–73. DOI:10.1016/S0028-3908(01)00154-X. PMID 11750916.
- López-Rodríguez ML, Murcia M, Benhamú B, et al. (2002). „Computational model of the complex between GR113808 and the 5-HT4 receptor guided by site-directed mutagenesis and the crystal structure of rhodopsin.”. J. Comput. Aided Mol. Des. 15 (11): 1025–33. DOI:10.1023/A:1014895611874. PMID 11989623.
- Ohtsuki T, Ishiguro H, Detera-Wadleigh SD, et al. (2003). „Association between serotonin 4 receptor gene polymorphisms and bipolar disorder in Japanese case-control samples and the NIMH Genetics Initiative Bipolar Pedigrees.”. Mol. Psychiatry 7 (9): 954–61. DOI:10.1038/sj.mp.4001133. PMID 12399948.
- Norum JH, Hart K, Levy FO (2003). „Ras-dependent ERK activation by the human G(s)-coupled serotonin receptors 5-HT4(b) and 5-HT7(a).”. J. Biol. Chem. 278 (5): 3098–104. DOI:10.1074/jbc.M206237200. PMID 12446729.
- Strausberg RL, Feingold EA, Grouse LH, et al. (2003). „Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.”. Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. DOI:10.1073/pnas.242603899. PMC 139241. PMID 12477932.
- Cartier D, Lihrmann I, Parmentier F, et al. (2003). „Overexpression of serotonin4 receptors in cisapride-responsive adrenocorticotropin-independent bilateral macronodular adrenal hyperplasia causing Cushing's syndrome.”. J. Clin. Endocrinol. Metab. 88 (1): 248–54. DOI:10.1210/jc.2002-021107. PMID 12519861.
- Manzke T, Guenther U, Ponimaskin EG, et al. (2003). „5-HT4(a) receptors avert opioid-induced breathing depression without loss of analgesia.”. Science 301 (5630): 226–9. DOI:10.1126/science.1084674. PMID 12855812.