5-HT4受體

5-HT₄受体或5-羟色胺受体4（英语：5-Hydroxytryptamine receptor 4）是在人类上由HTR4基因编码的蛋白质^[6][7]。

5-HT4受体
识别号
别名	HTR4；, 5-HT4, 5-HT4R, 5-HT4 receptor, 5-hydroxytryptamine receptor 4
外部ID	OMIM：602164 MGI：109246 HomoloGene：20243 GeneCards：HTR4
为以下药物的标靶
维拉佐酮、​血清素、​5-甲氧基色胺、​α-methyl-5-HT、​莫沙必利、​伦扎必利、​扎考必利、​普芦卡必利、​RS 67333、​GR-113808、​哌波色罗、​SB 204070、​levosulpiride、​齐美定、​capeserod、​relenopride、​td-8954、​metoclopramide hydrochloride hydrate[1]
基因位置（人类） 染色体 5号染色体[2] 基因座 5q32 起始 148,451,032 bp[2] 终止 148,677,235 bp[2]
基因位置（小鼠） 染色体 小鼠18号染色体[3] 基因座 18|18 E1 起始 62,457,275 bp[3] 终止 62,629,648 bp[3]
RNA表达模式
查阅更多表达数据
基因本体 分子功能 • G protein-coupled receptor activity • signal transducer activity • G protein-coupled serotonin receptor activity • trace-amine receptor activity • 相同蛋白质结合 • neurotransmitter receptor activity • 血浆蛋白结合 细胞组分 • 细胞质 • integral component of membrane • 核内体 • 细胞膜 • integral component of plasma membrane • 膜 • 树突 生物学过程 • gamma-aminobutyric acid signaling pathway • G protein-coupled receptor signaling pathway • G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger • regulation of appetite • 信号转导 • 化学性突触传递 • G protein-coupled serotonin receptor signaling pathway Sources:Amigo / QuickGO
直系同源
物种	人类	小鼠
Entrez	3360	15562
Ensembl	ENSG00000164270	ENSMUSG00000026322
UniProt	Q13639	P97288
mRNA​序列	​NM_000870 ​NM_001040169 ​NM_001040172 ​NM_001040173 ​NM_001040174 ​NM_001286410 ​NM_199453	NM_008313 ​NM_001364956 ​NM_001364957 ​NM_001364958 ​NM_001364959
蛋白序列	NP_000861 ​NP_001035259 ​NP_001035262 ​NP_001035263 ​NP_001273339 ​NP_955525	NP_032339 ​NP_001351885 ​NP_001351886 ​NP_001351887 ​NP_001351888
基因位置​（UCSC）	Chr 5: 148.45 – 148.68 Mb	Chr 18: 62.46 – 62.63 Mb
PubMed​查找	[4]	[5]
维基数据
查看/编辑人类 查看/编辑小鼠

配体

激动剂

• BIMU-8（英语：BIMU-8）
• Cisapride（英语：Cisapride）
• ML-10302^[8]
• 莫沙必利
• Prucalopride（英语：Prucalopride）
• Renzapride（英语：Renzapride）
• RS-67506
• Tegaserod（英语：Tegaserod）
• Zacopride
• Metoclopramide
• 舒必利
• RS-67333（英语：RS-67333） - partial agonist
• SL65.0155（英语：SL65.0155） - partial agonist
• CJ-033,466（英语：CJ-033,466） - partial agonist

拮抗剂

• 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)^[9]
• 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^[10]
• 洋甘菊(酒精萃取)^[11]

参见

• 5-羟色胺受体
• 5-HT₁受体（英语：5-HT1 receptor）
• 5-HT2受体
• 5-HT₃受体（英语：5-HT3 receptor）
• 5-HT₅受体（英语：5-HT5 receptor）
• 5-HT₆受体（英语：5-HT6 receptor）
• 5-HT₇受体（英语：5-HT7 receptor）

参考资料

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. GRCh38: Ensembl release 89: ENSG00000164270 - Ensembl, May 2017
3. GRCm38: Ensembl release 89: ENSMUSG00000026322 - Ensembl, May 2017
4. Human PubMed Reference:. National Center for Biotechnology Information, U.S. National Library of Medicine.
5. Mouse PubMed Reference:. National Center for Biotechnology Information, U.S. National Library of Medicine.
6. 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.
7. 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.
8. 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.
9. 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.
10. 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.
11. 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.

深入阅读

• 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.

外部链接

• 5-HT₄. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. （原始内容存档于2016-06-05）.

5-HT4受体引用了美国国家医学图书馆提供的数据，这些数据属于公共领域。

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