5-HT4受容体、5-HT4レセプター、セロトニン4受容体、セロトニン4レセプター

関: 5-HT4 serotonin receptor

WordNet

the 8th letter of the Roman alphabet (同)h
a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response

PrepTutorEJDIC

hydrogenの化学記号
鉛筆の硬度 / 《俗》heroin
=sense organ / 受信装置

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/03/17 11:59:25」(JST)

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[Wiki en表示]

5-Hydroxytryptamine receptor 4 is a protein that in humans is encoded by the HTR4 gene.^[4]^[5]

Function

This gene is a member of the family of human serotonin receptors, which are G protein-coupled receptors that stimulate cAMP production in response to serotonin (5-hydroxytryptamine). The gene product is a glycosylated transmembrane protein that functions in both the peripheral and central nervous system to modulate the release of various neurotransmitters. Multiple transcript variants encoding proteins with distinct C-terminal sequences have been described, but the full-length nature of some transcript variants has not been determined.^[6]

Location

The receptor is located in the alimentary tract, urinary bladder, heart and adrenal gland as well as the central nervous system (CNS).^[7] In the CNS the receptor appears in the putamen, caudate nucleus, nucleus accumbens, globus pallidus, and substantia nigra, and to a lesser extent in the neocortex, raphe, pontine nuclei, and some areas of the thalamus. It has not been found in the cerebellum.^[8]

Isoforms

Internalization is isoform-specific.^[9]

Ligands

Several drugs that act as 5-HT₄ selective agonists have recently been introduced into use in both scientific research and clinical medicine. Some drugs that act as 5-HT₄ agonists are also active as 5-HT₃ antagonists, such as mosapride, metoclopramide, renzapride, and zacopride, and so these compounds cannot be considered highly selective. Research in this area is ongoing.^[10]

SB-207,145 radiolabeled with carbon-11 is used as a radioligand for 5-HT₄ in positron emission tomography pig^[11] and human^[12] studies.

Agonists

BIMU-8
Cisapride
CJ-033,466 - partial agonist
ML-10302^[13]
Mosapride
Prucalopride
Renzapride
RS-67506
RS-67333 - partial agonist
SL65.0155 - partial agonist
Tegaserod
Zacopride
Metoclopramide
Sulpiride

Antagonists

Piboserod
GR-113,808 (1-methyl-1H-indole-3-carboxylic acid, [1-[2-[(methylsulfonyl)amino]ethyl]-4-piperidinyl]methyl ester)^[14]
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
([Methoxy-¹¹C]1-butylpiperidin-4-yl)methyl 4-amino-3-methoxybenzoate^[15]
Chamomile (ethanol extract)^[16]

References

^ "Drugs that physically interact with 5-hydroxytryptamine receptor 4 view/edit references on wikidata".
^ "Human PubMed Reference:".
^ "Mouse PubMed Reference:".
^ 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". Cytogenetics and Cell Genetics. 78 (2): 133–4. doi:10.1159/000134646. PMID 9371406.
^ Blondel O, Vandecasteele G, Gastineau M, Leclerc S, Dahmoune Y, Langlois M, Fischmeister R (August 1997). "Molecular and functional characterization of a 5-HT4 receptor cloned from human atrium". FEBS Letters. 412 (3): 465–74. doi:10.1016/S0014-5793(97)00820-X. PMID 9276448.
^ "Entrez Gene: HTR4 5-hydroxytryptamine (serotonin) receptor 4".
^ Hegde SS, Eglen RM (October 1996). "Peripheral 5-HT4 receptors". FASEB Journal. 10 (12): 1398–407. PMID 8903510.
^ Varnäs K, Halldin C, Pike VW, Hall H (August 2003). "Distribution of 5-HT4 receptors in the postmortem human brain--an autoradiographic study using [125I]SB 207710". European Neuropsychopharmacology. 13 (4): 228–34. doi:10.1016/S0924-977X(03)00009-9. PMID 12888181.
^ Mnie-Filali O, Amraei MG, Benmbarek S, Archer-Lahlou E, Peñas-Cazorla R, Vilaró MT, Boye SM, Piñeyro G (March 2010). "Serotonin 4 receptor (5-HT4R) internalization is isoform-specific: effects of 5-HT and RS67333 on isoforms A and B". Cellular Signalling. 22 (3): 501–9. doi:10.1016/j.cellsig.2009.11.004. 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.
^ Kornum BR, Lind NM, Gillings N, Marner L, Andersen F, Knudsen GM (January 2009). "Evaluation of the novel 5-HT4 receptor PET ligand [11C]SB207145 in the Göttingen minipig". Journal of Cerebral Blood Flow and Metabolism. 29 (1): 186–96. doi:10.1038/jcbfm.2008.110. PMID 18797470.
^ Marner L, Gillings N, Comley RA, Baaré WF, Rabiner EA, Wilson AA, Houle S, Hasselbalch SG, Svarer C, Gunn RN, Laruelle M, Knudsen GM (June 2009). "Kinetic modeling of 11C-SB207145 binding to 5-HT4 receptors in the human brain in vivo". Journal of Nuclear Medicine. 50 (6): 900–8. doi:10.2967/jnumed.108.058552. PMID 19470850.
^ Godínez-Chaparro B, Barragán-Iglesias P, Castañeda-Corral G, Rocha-González HI, Granados-Soto V (March 2011). "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. 152 (3): 687–97. doi:10.1016/j.pain.2010.12.020. PMID 21239110.
^ Gale JD, Grossman CJ, Whitehead JW, Oxford AW, Bunce KT, Humphrey PP (January 1994). "GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor". British Journal of Pharmacology. 111 (1): 332–8. doi:10.1111/j.1476-5381.1994.tb14064.x. PMC 1910004. PMID 8012715.
^ Xu R, Hong J, Morse CL, Pike VW (October 2010). "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. 53 (19): 7035–47. doi:10.1021/jm100668r. PMC 2951497. PMID 20812727.
^ 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. 13 Suppl 5: 51–5. doi:10.1016/j.phymed.2006.03.012. PMID 16973340.

External links

"5-HT₄". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
Human HTR4 genome location and HTR4 gene details page in the UCSC Genome Browser.

This article incorporates text from the United States National Library of Medicine, which is in the public domain.

UpToDate Contents

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1. セロトニンモジュレータ：薬理学、投与、および副作用 serotonin modulators pharmacology administration and side effects
2. 選択的セロトニン再取り込み阻害剤：薬理学、投与方法、および副作用 selective serotonin reuptake inhibitors pharmacology administration and side effects
3. 制吐剤の特性 characteristics of antiemetic drugs
4. セロトニン症候群 serotonin syndrome
5. 麻酔後ケア病棟における合併症発生の概要 overview of complications occurring in the post anesthesia care unit

English Journal

Discovery of TD-8954, a clinical stage 5-HT4 receptor agonist with gastrointestinal prokinetic properties.

McKinnell RM, Armstrong SR, Beattie DT, Fatheree PR, Long DD, Marquess DG, Shaw JP, Vickery RG.SourceTheravance, Inc., 901 Gateway Blvd, South San Francisco, CA 94080, United States. Electronic address: mmckinnell@theravance.com.
Bioorganic & medicinal chemistry letters.Bioorg Med Chem Lett.2013 Jul 15;23(14):4210-5. doi: 10.1016/j.bmcl.2013.05.018. Epub 2013 May 16.
The discovery of a series of 5-HT4 receptor agonists based on a novel 2-alkylbenzimidazole aromatic core is described. Optimization of the 2-substituent of the benzimidazole ring led to a series of agonists with subnanomolar binding affinity and moderate-to-high intrinsic activity relative to that o
PMID 23756062

Chronic 5-HT4 receptor activation decreases Aβ production and deposition in hAPP/PS1 mice.

Tesseur I, Pimenova AA, Lo AC, Ciesielska M, Lichtenthaler SF, De Maeyer JH, Schuurkes JA, D'Hooge R, De Strooper B.SourceCenter for Human Genetics, Leuven Research Institute for Neuroscience and Disease (LIND), University of Leuven, Leuven, Belgium ina.tesseur@med.kuleuven.be
Neurobiology of aging.Neurobiol Aging.2013 Jul;34(7):1779-89. doi: 10.1016/j.neurobiolaging.2013.01.020. Epub 2013 Mar 6.
Lowering the production and accumulation of Aβ has been explored as treatment for Alzheimer's disease (AD), because Aβ is postulated to play an important role in the pathogenesis of AD. 5-HT4 receptors are an interesting drug target in this regard, as their activation might stimulate α-secretase
PMID 23474291

Ozone exposure alters serotonin and serotonin receptor expression in the developing lung.

Murphy SR, Schelegle ES, Miller LA, Hyde DM, Van Winkle LS.Source* Center for Health and the Environment.
Toxicological sciences : an official journal of the Society of Toxicology.Toxicol Sci.2013 Jul;134(1):168-79. doi: 10.1093/toxsci/kft090. Epub 2013 Apr 9.
Ozone, a pervasive environmental pollutant, adversely affects functional lung growth in children. Animal studies demonstrate that altered lung development is associated with modified signaling within the airway epithelial mesenchymal trophic unit, including mediators that can change nerve growth. We
PMID 23570994

Japanese Journal

A protein tyrosine kinase receptor, c-RET signaling pathway contributes to the enteric neurogenesis induced by a 5-HT₄ receptor agonist at an anastomosis after transection of the gut in rodents

Goto Kei,Kawahara Isao,Kuniyasu Hiroki [他]
The journal of physiological sciences 65(4), 377-383, 2015-07
NAID 40020509938

炎症性腸疾患モデル動物における温度感受性受容体TRPV1とセロトニンシグナリングの変化

松本健次郎
薬学雑誌. 乙号 134(11), 1165-1170, 2014
… Hypersensitivity of afferent fibers occurs during inflammation, and therefore to gain insight into the alteration of receptors and channels, we examined receptors such as 5-HT receptors and transient receptor potential vanilloid type 1 (TRPV1), which are expressed in primary afferent neurons. …
NAID 130004712972

排便と健康

浦尾正彦
順天堂醫事雑誌 60(1), 16-24, 2014
便秘とは，排便の頻度が週2回以下で，便が硬く，排便困難，残便感がある状態といわれている．実際には放置されていたり自己流の対処をされていることが多い．が，便秘患者では労働生産性が障害されたり，肛門疾患や結腸癌などの様々なリスクも増加することが知られており，しっかり取り組むべき疾患である．慢性便秘は，症候性，薬剤性，器質性，機能性便秘などに分類される．症候性便秘は神経疾患，内分泌疾患の症状の一部として …
NAID 130004684311

「5-HT4受容体」

HTR4
Identifiers
Aliases	HTR4, 5-HT4, 5-HT4R, 5-HT4 receptor, 5-hydroxytryptamine receptor 4
External IDs	MGI: 109246 HomoloGene: 20243 GeneCards: HTR4
Targeted by Drug
	vilazodone, pathogen, 5-methoxytryptamine, α-methyl-5-HT, mosapride, renzapride, zacopride, prucalopride, RS 67333, gr-113808, piboserod, SB 204070
Gene ontology
Molecular function	• G-protein coupled receptor activity; • signal transducer activity; • G-protein coupled serotonin receptor activity; • trace-amine receptor activity;
Cellular component	• cytoplasm; • integral component of membrane; • endosome; • plasma membrane; • integral component of plasma membrane; • membrane;
Biological process	• 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; • signal transduction; • chemical synaptic transmission; • G-protein coupled serotonin receptor signaling pathway;
	Sources:Amigo / QuickGO
RNA expression pattern
	; ; ; ;
	More reference expression data
Orthologs
	3360
	15562
	ENSG00000164270
	ENSMUSG00000026322
	Q13639
	P97288
NM_000870; NM_001040169; NM_001040172; NM_001040173; NM_001040174;
	NM_001286410; NM_199453
	NM_008313
NP_000861; NP_001035259; NP_001035262; NP_001035263; NP_001273339;
	NP_955525
	NP_032339.2; NP_032339
	Wikidata
View/Edit Human	View/Edit Mouse

　　[★]

英: 5-HT4 receptor
関: 5-HT4レセプター、5-HT4セロトニンレセプター、セロトニン4レセプター、セロトニン4受容体

「5-HT4レセプター」

　　[★]

英: 5-HT4 receptor
関: 5-HT4受容体、セロトニン4レセプター、セロトニン4受容体

「セロトニン4受容体」

　　[★]

英: 5-HT4 receptor
関: 5-HT4受容体、5-HT4レセプター、セロトニン4レセプター

「セロトニン4レセプター」

　　[★]

英: 5-HT4 receptor
関: 5-HT4受容体、5-HT4レセプター、セロトニン4受容体

「HT」

　　[★]

「H」

　　[★]

[1] "Drugs that physically interact with 5-hydroxytryptamine receptor 4 view/edit references on wikidata".

[2] "Human PubMed Reference:".

[3] "Mouse PubMed Reference:".

[pmid9371406-4] 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". Cytogenetics and Cell Genetics. 78 (2): 133–4. doi:10.1159/000134646. PMID 9371406.

[pmid9276448-5] Blondel O, Vandecasteele G, Gastineau M, Leclerc S, Dahmoune Y, Langlois M, Fischmeister R (August 1997). "Molecular and functional characterization of a 5-HT4 receptor cloned from human atrium". FEBS Letters. 412 (3): 465–74. doi:10.1016/S0014-5793(97)00820-X. PMID 9276448.

[entrez-6] "Entrez Gene: HTR4 5-hydroxytryptamine (serotonin) receptor 4".

[7] Hegde SS, Eglen RM (October 1996). "Peripheral 5-HT4 receptors". FASEB Journal. 10 (12): 1398–407. PMID 8903510.

[8] Varnäs K, Halldin C, Pike VW, Hall H (August 2003). "Distribution of 5-HT4 receptors in the postmortem human brain--an autoradiographic study using [125I]SB 207710". European Neuropsychopharmacology. 13 (4): 228–34. doi:10.1016/S0924-977X(03)00009-9. PMID 12888181.

[9] Mnie-Filali O, Amraei MG, Benmbarek S, Archer-Lahlou E, Peñas-Cazorla R, Vilaró MT, Boye SM, Piñeyro G (March 2010). "Serotonin 4 receptor (5-HT4R) internalization is isoform-specific: effects of 5-HT and RS67333 on isoforms A and B". Cellular Signalling. 22 (3): 501–9. doi:10.1016/j.cellsig.2009.11.004. PMID 19922792.

[pmid19168624-10] 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.

[11] Kornum BR, Lind NM, Gillings N, Marner L, Andersen F, Knudsen GM (January 2009). "Evaluation of the novel 5-HT4 receptor PET ligand [11C]SB207145 in the Göttingen minipig". Journal of Cerebral Blood Flow and Metabolism. 29 (1): 186–96. doi:10.1038/jcbfm.2008.110. PMID 18797470.

[pmid19470850-12] Marner L, Gillings N, Comley RA, Baaré WF, Rabiner EA, Wilson AA, Houle S, Hasselbalch SG, Svarer C, Gunn RN, Laruelle M, Knudsen GM (June 2009). "Kinetic modeling of 11C-SB207145 binding to 5-HT4 receptors in the human brain in vivo". Journal of Nuclear Medicine. 50 (6): 900–8. doi:10.2967/jnumed.108.058552. PMID 19470850.

[pmid21239110-13] Godínez-Chaparro B, Barragán-Iglesias P, Castañeda-Corral G, Rocha-González HI, Granados-Soto V (March 2011). "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. 152 (3): 687–97. doi:10.1016/j.pain.2010.12.020. PMID 21239110.

[14] Gale JD, Grossman CJ, Whitehead JW, Oxford AW, Bunce KT, Humphrey PP (January 1994). "GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor". British Journal of Pharmacology. 111 (1): 332–8. doi:10.1111/j.1476-5381.1994.tb14064.x. PMC 1910004. PMID 8012715.

[15] Xu R, Hong J, Morse CL, Pike VW (October 2010). "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. 53 (19): 7035–47. doi:10.1021/jm100668r. PMC 2951497. PMID 20812727.

[16] 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. 13 Suppl 5: 51–5. doi:10.1016/j.phymed.2006.03.012. PMID 16973340.

リンク元	「5-HT4受容体」「5-HT4レセプター」「セロトニン4受容体」「セロトニン4レセプター」
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5-HT4 receptor