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5-HT4受體

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(重定向自5-HT4受体
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HTR4
識別號
别名 HTR4;5-HT4、​5-HT4 receptor、​5-HT4R、​5-hydroxytryptamine receptor 4
外部ID MGI109246 HomoloGene20243 GeneCardsHTR4
為以下藥物的標靶
vilazodone、​血清素、​5-甲氧基色胺、​α-methyl-5-HT、​莫沙必利、​renzapride、​zacopride、​prucalopride、​RS 67333、​gr-113808、​piboserod、​SB 204070[1]
RNA表达模式
PBB GE HTR4 207578 s at fs.png

PBB GE HTR4 207577 at fs.png

PBB GE HTR4 216939 s at fs.png
更多參考(基因)表达數據
直系同源
物種 人類 小鼠
Entrez
Ensembl
UniProt
mRNA​序列

NR_104445、NM_000870、NM_001040169、NM_001040172、NM_001040173、NM_001040174、NM_001286410、NM_199453

NM_008313、XM_006525676、XM_006525678、XM_006525680、XM_006525681、XM_006525682、XM_006525683、XM_011246848、XM_017317839

蛋白序列

NP_000861、NP_001035259、NP_001035262、NP_001035263、NP_001273339、NP_955525

NP_032339、XP_006525739、XP_006525741、XP_006525743、XP_006525744、XP_006525745、XP_006525746、XP_011245150、XP_017173328

基因位置​(UCSC) Chr 5: 148.45 – 148.68 Mb n/a
PubMed​查找 [2] [3]
維基數據
檢視/編輯 人類 檢視/編輯 小鼠

5-HT4受體5-羥色胺受體4英语:5-Hydroxytryptamine receptor 4)是在人類上由HTR4基因編碼的蛋白質[4][5]

配體[编辑]

激動劑[编辑]

拮抗劑[编辑]

  • Piboserod英语Piboserod
  • GR-113,808英语GR-113,808 (1-methyl-1H-indole-3-carboxylic acid, [1-[2-[(methylsulfonyl)amino]ethyl]-4-piperidinyl]methyl ester)[7]
  • GR-125,487
  • RS-39604 (1-[4-Amino-5-chloro-2-(3,5-dimethoxyphenyl)methyloxy]-3-[1-[2-methylsulphonylamino]piperidin-4-yl]propan-1-one)
  • SB-203,186
  • SB-204,070英语SB-204,070
  • ([Methoxy-11C]1-butylpiperidin-4-yl)methyl 4-amino-3-methoxybenzoate[8]
  • 洋甘菊(酒精萃取)[9]

參見[编辑]

參考資料[编辑]

  1. ^ 對5-hydroxytryptamine receptor 4起作用的藥物;在維基數據上查看/編輯參考. 
  2. ^ Human PubMed Reference:. 
  3. ^ Mouse PubMed Reference:. 
  4. ^ Claeysen S, Faye P, Sebben M, Lemaire S, Bockaert J, Dumuis A, Taviaux S. Assignment of 5-hydroxytryptamine receptor (HTR4) to human chromosome 5 bands q31-->q33 by in situ hybridization. Cytogenetics and Cell Genetics. December 1997, 78 (2): 133–4. PMID 9371406. doi:10.1159/000134646. 
  5. ^ Blondel O, Vandecasteele G, Gastineau M, Leclerc S, Dahmoune Y, Langlois M, Fischmeister R. Molecular and functional characterization of a 5-HT4 receptor cloned from human atrium. FEBS Letters. August 1997, 412 (3): 465–74. PMID 9276448. doi:10.1016/S0014-5793(97)00820-X. 
  6. ^ Godínez-Chaparro B, Barragán-Iglesias P, Castañeda-Corral G, Rocha-González HI, Granados-Soto V. Role of peripheral 5-HT(4), 5-HT(6), and 5-HT(7) receptors in development and maintenance of secondary mechanical allodynia and hyperalgesia. Pain. March 2011, 152 (3): 687–97. PMID 21239110. doi:10.1016/j.pain.2010.12.020. 
  7. ^ Gale JD, Grossman CJ, Whitehead JW, Oxford AW, Bunce KT, Humphrey PP. GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor. British Journal of Pharmacology. January 1994, 111 (1): 332–8. PMC 1910004. PMID 8012715. doi:10.1111/j.1476-5381.1994.tb14064.x. 
  8. ^ Xu R, Hong J, Morse CL, Pike VW. Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography. Journal of Medicinal Chemistry. October 2010, 53 (19): 7035–47. PMC 2951497. PMID 20812727. doi:10.1021/jm100668r. 
  9. ^ Simmen U, Kelber O, Okpanyi SN, Jaeggi R, Bueter B, Weiser D. Binding of STW 5 (Iberogast) and its components to intestinal 5-HT, muscarinic M3, and opioid receptors. Phytomedicine: 51–5. PMID 16973340. doi:10.1016/j.phymed.2006.03.012. 

深入閱讀[编辑]

  • Licht CL, 2009, Changes in the 5-HT4 receptor in animal models of depression英语animal models of depression and antidepressant treatment, PhD thesis, University of Copenhagen.
  • Ullmer C, Schmuck K, Kalkman HO, Lübbert H. Expression of serotonin receptor mRNAs in blood vessels. FEBS Letters. August 1995, 370 (3): 215–21. PMID 7656980. doi:10.1016/0014-5793(95)00828-W. 
  • Blondel O, Vandecasteele G, Gastineau M, Leclerc S, Dahmoune Y, Langlois M, Fischmeister R. Molecular and functional characterization of a 5-HT4 receptor cloned from human atrium. FEBS Letters. August 1997, 412 (3): 465–74. PMID 9276448. doi:10.1016/S0014-5793(97)00820-X. 
  • Van den Wyngaert I, Gommeren W, Verhasselt P, Jurzak M, Leysen J, Luyten W, Bender E. Cloning and expression of a human serotonin 5-HT4 receptor cDNA. Journal of Neurochemistry. November 1997, 69 (5): 1810–9. PMID 9349523. doi:10.1046/j.1471-4159.1997.69051810.x. 
  • Claeysen S, Faye P, Sebben M, Lemaire S, Bockaert J, Dumuis A. Cloning and expression of human 5-HT4S receptors. Effect of receptor density on their coupling to adenylyl cyclase. NeuroReport. October 1997, 8 (15): 3189–96. PMID 9351641. doi:10.1097/00001756-199710200-00002. 
  • Blondel O, Gastineau M, Dahmoune Y, Langlois M, Fischmeister R. Cloning, expression, and pharmacology of four human 5-hydroxytryptamine 4 receptor isoforms produced by alternative splicing in the carboxyl terminus. Journal of Neurochemistry. June 1998, 70 (6): 2252–61. PMID 9603189. doi:10.1046/j.1471-4159.1998.70062252.x. 
  • Cichon S, Kesper K, Propping P, Nöthen MM. Assignment of the human serotonin 4 receptor gene (HTR4) to the long arm of chromosome 5 (5q31-q33). Molecular Membrane Biology. 1998, 15 (2): 75–8. PMID 9724925. doi:10.3109/09687689809027521. 
  • Claeysen S, Sebben M, Becamel C, Bockaert J, Dumuis A. Novel brain-specific 5-HT4 receptor splice variants show marked constitutive activity: role of the C-terminal intracellular domain. Molecular Pharmacology. May 1999, 55 (5): 910–20. PMID 10220570. 
  • Bender E, Pindon A, van Oers I, Zhang YB, Gommeren W, Verhasselt P, Jurzak M, Leysen J, Luyten W. Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant. Journal of Neurochemistry. February 2000, 74 (2): 478–89. PMID 10646498. doi:10.1046/j.1471-4159.2000.740478.x. 
  • Mialet J, Berque-Bestel I, Eftekhari P, Gastineau M, Giner M, Dahmoune Y, Donzeau-Gouge P, Hoebeke J, Langlois M, Sicsic S, Fischmeister R, Lezoualc'h F. 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. British Journal of Pharmacology. February 2000, 129 (4): 771–81. PMC 1571890. PMID 10683202. doi:10.1038/sj.bjp.0703101. 
  • Bach T, Syversveen T, Kvingedal AM, Krobert KA, Brattelid T, Kaumann AJ, Levy FO. 5HT4(a) and 5-HT4(b) receptors have nearly identical pharmacology and are both expressed in human atrium and ventricle. Naunyn-Schmiedeberg's Archives of Pharmacology. February 2001, 363 (2): 146–60. PMID 11218067. doi:10.1007/s002100000299. 
  • Medhurst AD, Lezoualc'h F, Fischmeister R, Middlemiss DN, Sanger GJ. 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 Research. Molecular Brain Research. June 2001, 90 (2): 125–34. PMID 11406291. doi:10.1016/S0169-328X(01)00095-X. 
  • Hiroi T, Hayashi-Kobayashi N, Nagumo S, Ino M, Okawa Y, Aoba A, Matsui H. Identification and characterization of the human serotonin-4 receptor gene promoter. Biochemical and Biophysical Research Communications. November 2001, 289 (2): 337–44. PMID 11716477. doi:10.1006/bbrc.2001.5979. 
  • Vilaró MT, Doménech T, Palacios JM, Mengod G. 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. January 2002, 42 (1): 60–73. PMID 11750916. doi:10.1016/S0028-3908(01)00154-X. 
  • López-Rodríguez ML, Murcia M, Benhamú B, Olivella M, Campillo M, Pardo L. Computational model of the complex between GR113808 and the 5-HT4 receptor guided by site-directed mutagenesis and the crystal structure of rhodopsin. Journal of Computer-Aided Molecular Design. November 2001, 15 (11): 1025–33. PMID 11989623. doi:10.1023/A:1014895611874. 
  • Ohtsuki T, Ishiguro H, Detera-Wadleigh SD, Toyota T, Shimizu H, Yamada K, Yoshitsugu K, Hattori E, Yoshikawa T, Arinami T. Association between serotonin 4 receptor gene polymorphisms and bipolar disorder in Japanese case-control samples and the NIMH Genetics Initiative Bipolar Pedigrees. Molecular Psychiatry. 2003, 7 (9): 954–61. PMID 12399948. doi:10.1038/sj.mp.4001133. 
  • Norum JH, Hart K, Levy FO. Ras-dependent ERK activation by the human G(s)-coupled serotonin receptors 5-HT4(b) and 5-HT7(a). The Journal of Biological Chemistry. January 2003, 278 (5): 3098–104. PMID 12446729. doi:10.1074/jbc.M206237200. 
  • Cartier D, Lihrmann I, Parmentier F, Bastard C, Bertherat J, Caron P, Kuhn JM, Lacroix A, Tabarin A, Young J, Vaudry H, Lefebvre H. Overexpression of serotonin4 receptors in cisapride-responsive adrenocorticotropin-independent bilateral macronodular adrenal hyperplasia causing Cushing's syndrome. The Journal of Clinical Endocrinology and Metabolism. January 2003, 88 (1): 248–54. PMID 12519861. doi:10.1210/jc.2002-021107. 
  • Manzke T, Guenther U, Ponimaskin EG, Haller M, Dutschmann M, Schwarzacher S, Richter DW. 5-HT4(a) receptors avert opioid-induced breathing depression without loss of analgesia. Science. July 2003, 301 (5630): 226–9. PMID 12855812. doi:10.1126/science.1084674. 

外部連結[编辑]


5-HT4受體引用了美国国家医学图书馆提供的資料,这些資料属于公共领域


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