5-HT₄受體

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
基因位置（人类）
染色体	5号染色体
终止	148,677,235 bp
基因位置（小鼠）
染色体	小鼠18号染色体
终止	62,629,648 bp
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
	3360
	15562
	ENSG00000164270
	ENSMUSG00000026322
	Q13639
	P97288
NM_000870; NM_001040169; NM_001040172; NM_001040173; NM_001040174;
	NM_001286410; NM_199453
	NM_008313; NM_001364956; NM_001364957; NM_001364958; NM_001364959
NP_000861; NP_001035259; NP_001035262; NP_001035263; NP_001273339;
	NP_955525
	NP_032339; NP_001351885; NP_001351886; NP_001351887; NP_001351888
	维基数据
查看/编辑人类	查看/编辑小鼠

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]。

配体[编辑]

激动剂[编辑]

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[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)^[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[编辑]

参考资料[编辑]

^ 對5-hydroxytryptamine receptor 4起作用的藥物；在維基數據上查看/編輯參考.
^ ^2.0 ^2.1 ^2.2 GRCh38: Ensembl release 89: ENSG00000164270 - Ensembl, May 2017
^ ^3.0 ^3.1 ^3.2 GRCm38: Ensembl release 89: ENSMUSG00000026322 - Ensembl, May 2017
^ Human PubMed Reference:. National Center for Biotechnology Information, U.S. National Library of Medicine.
^ Mouse PubMed Reference:. National Center for Biotechnology Information, U.S. National Library of Medicine.
^ 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.
^ 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.
^ 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.
^ 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.
^ 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.
^ 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[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.

外部链接[编辑]

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。

#invoke:navbox

[1] 對5-hydroxytryptamine receptor 4起作用的藥物；在維基數據上查看/編輯參考.

[refGRCh38Ensembl-2] 2.0 ^2.1 ^2.2 GRCh38: Ensembl release 89: ENSG00000164270 - Ensembl, May 2017

[refGRCm38Ensembl-3] 3.0 ^3.1 ^3.2 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.

[pmid9371406-6] 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.

[pmid9276448-7] 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.

[pmid21239110-8] 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.

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