5-HT4 수용체
5-HT4 receptor| HTR4 | |||||||
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| 식별자 | |||||||
| 별칭 | HTR4, 5-HT4, 5-HT4R, 5-HT4 수용체, 5-HT4 수용체, 5-히드록시트리프타민 수용체 4 | ||||||
| 외부 ID | OMIM: 602164 MGI: 109246 호몰로진: 20243 GeneCard: HTR4 | ||||||
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| 직교체 | |||||||
| 종 | 인간 | 마우스 | |||||
| 엔트레스 | |||||||
| 앙상블 | |||||||
| 유니프로트 | |||||||
| RefSeq(mRNA) |
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| RefSeq(단백질) |
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| 위치(UCSC) | Chr 5: 148.45 – 148.68Mb | Cr 18: 62.32 – 62.5Mb | |||||
| PubMed 검색 | [3] | [4] | |||||
| 위키다타 | |||||||
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5-히드록시트리프타민 수용체 4는 인간에서 HTR4 유전자에 의해 암호화된 단백질이다.[5][6]
함수
이 유전자는 인간 세로토닌 수용체 계열의 구성원으로 세로토닌(5-히드록시트리프타민)에 반응해 cAMP 생성을 자극하는 G단백질결합 수용체다. 유전자 생산물은 글리코실화 트랜섬브레인 단백질로 말초신경계와 중추신경계 모두에서 다양한 신경전달물질의 방출을 조절하는 기능을 한다. 뚜렷한 C-단자 시퀀스를 가진 단백질을 인코딩하는 다중 대본 변형이 설명되었지만, 일부 대본 변형의 전체 길이 속성은 결정되지 않았다.[7]
위치
수용체는 중추신경계(CNS)뿐만 아니라 소화기관, 방광, 심장, 부신 등에 위치한다.[8] CNS에서 수용체는 putamen, caudate nucleus, nuclear accumbens, globus pallidus, serembia nigra에 나타나며, 신피질, raphe, pontine nuclei 및 thalamus의 일부 영역에는 더 작은 범위까지 나타난다. 그것은 소뇌에서 발견되지 않았다.[9]
이소폼스
내부화는 이소 형태에 특화되어 있다.[10]
리간즈
5-HT4 선택적 작용제 역할을 하는 여러 가지 약물이 최근 과학 연구와 임상 의학 모두에 도입되었다. 5-HT4 작용제로 작용하는 일부 약물은 모사프라이드, 메토클로프라미드, 렌자프라이드, 자코프라이드 등 5-HT3 길항제로서도 활발히 활동하기 때문에 이들 화합물은 선택성이 높다고 볼 수 없다. 이 분야에 대한 연구는 진행 중이다.[11]
탄소-11로 방사선을 쬐는 SB-207,145는 양전자 방출 단층 촬영 돼지[12] 및 인체[13] 연구에서4 5-HT용 방사선으로 사용된다.
고민자
- BIMU-8
- 시사프라이드
- CJ-033,466 - 부분작용제
- ML-10302[14]
- 모사프리드
- 프루칼로프라이드
- 렌자프리드
- RS-67506
- RS-67333 - 부분작용제
- SL65.0155 - 부분작용제
- 테가세로드
- 자코프라이드
- 메토클로프라미드
- 설피라이드
반목자
- 리신
- 피보세로드
- GR-113,808(1-메틸-1H-indole-3-카르복실산, [1-[(메틸설폰)아미노]에틸]-4-피페리디닐]메틸에스테르)[15]
- GR-125,487
- RS-39604(1-[4-아미노-5-클로로-2-(3,5-디메트호섹시페닐)메틸록시]-3-[1-[2-메틸슐포닐아미노]피페리딘-4-yl]프로판-1-1)
- SB-203,186
- SB-204,070
- ([Methoxy-C11]1-부틸피페리딘-4-yl)메틸 4-아미노-3-메톡시벤조이트[16]
- 카모마일(에탄올 추출물)[17]
참고 항목
참조
- ^ Jump up to: a b c GRCh38: 앙상블 릴리스 89: ENSG00000164270 - 앙상블, 2017년 5월
- ^ Jump up to: a b c GRCm38: 앙상블 릴리스 89: ENSMUSG000026322 - 앙상블, 2017년 5월
- ^ "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 (December 1997). "Assignment of 5-hydroxytryptamine receptor (HTR4) to human chromosome 5 bands q31-->q33 by in situ hybridization" (PDF). 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. S2CID 23714426.
- ^ "Entrez Gene: HTR4 5-hydroxytryptamine (serotonin) receptor 4".
- ^ Hegde SS, Eglen RM (October 1996). "Peripheral 5-HT4 receptors". FASEB Journal. 10 (12): 1398–407. doi:10.1096/fasebj.10.12.8903510. PMID 8903510. S2CID 21596751.
- ^ 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. S2CID 27945284.
- ^ 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" (PDF). Molecular Pharmacology. 75 (4): 982–90. doi:10.1124/mol.108.053686. PMID 19168624. S2CID 17957338.
- ^ 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. S2CID 140204185.
- ^ 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 (2006). "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.
추가 읽기
- 리히트 CL, 2009년, 우울증 및 항우울제 치료의 동물 모델에서 5-HT4 수용체의 변화, 코펜하겐 대학의 박사 논문.
- Ullmer C, Schmuck K, Kalkman HO, Lübbert H (August 1995). "Expression of serotonin receptor mRNAs in blood vessels". FEBS Letters. 370 (3): 215–21. doi:10.1016/0014-5793(95)00828-W. PMID 7656980. S2CID 9015835.
- 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. S2CID 23714426.
- Van den Wyngaert I, Gommeren W, Verhasselt P, Jurzak M, Leysen J, Luyten W, Bender E (November 1997). "Cloning and expression of a human serotonin 5-HT4 receptor cDNA". Journal of Neurochemistry. 69 (5): 1810–9. doi:10.1046/j.1471-4159.1997.69051810.x. PMID 9349523. S2CID 25269904.
- Claeysen S, Faye P, Sebben M, Lemaire S, Bockaert J, Dumuis A (October 1997). "Cloning and expression of human 5-HT4S receptors. Effect of receptor density on their coupling to adenylyl cyclase" (PDF). NeuroReport. 8 (15): 3189–96. doi:10.1097/00001756-199710200-00002. PMID 9351641. S2CID 20624532.
- Blondel O, Gastineau M, Dahmoune Y, Langlois M, Fischmeister R (June 1998). "Cloning, expression, and pharmacology of four human 5-hydroxytryptamine 4 receptor isoforms produced by alternative splicing in the carboxyl terminus". Journal of Neurochemistry. 70 (6): 2252–61. doi:10.1046/j.1471-4159.1998.70062252.x. PMID 9603189. S2CID 24203530.
- 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)". Molecular Membrane Biology. 15 (2): 75–8. doi:10.3109/09687689809027521. PMID 9724925.
- Claeysen S, Sebben M, Becamel C, Bockaert J, Dumuis A (May 1999). "Novel brain-specific 5-HT4 receptor splice variants show marked constitutive activity: role of the C-terminal intracellular domain". Molecular Pharmacology. 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 (February 2000). "Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant". Journal of Neurochemistry. 74 (2): 478–89. doi:10.1046/j.1471-4159.2000.740478.x. PMID 10646498. S2CID 33817190.
- 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 (February 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". British Journal of Pharmacology. 129 (4): 771–81. doi:10.1038/sj.bjp.0703101. PMC 1571890. PMID 10683202.
- Bach T, Syversveen T, Kvingedal AM, Krobert KA, Brattelid T, Kaumann AJ, Levy FO (February 2001). "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. 363 (2): 146–60. doi:10.1007/s002100000299. PMID 11218067. S2CID 27504006.
- Medhurst AD, Lezoualc'h F, Fischmeister R, Middlemiss DN, Sanger GJ (June 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 Research. Molecular Brain Research. 90 (2): 125–34. doi:10.1016/S0169-328X(01)00095-X. PMID 11406291.
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외부 링크
- "5-HT4". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
- UCSC 게놈 브라우저의 인간 HTR4 유전자 위치 및 HTR4 유전자 세부 정보 페이지.
이 기사는 공공영역에 있는 미국 국립 의학 도서관의 텍스트를 통합하고 있다.
