MT1受容体、MT1レセプター
- 関
- MT1 melatonin receptor
WordNet
- 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
- the 13th letter of the Roman alphabet (同)m
PrepTutorEJDIC
- =sense organ / 受信装置
- Mach number / mark[s] / Monsieur
- Montana
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2015/05/21 20:28:37」(JST)
[Wiki en表示]
Melatonin receptor 1A |
Identifiers |
Symbols |
MTNR1A ; MEL-1A-R; MT1 |
External IDs |
OMIM: 600665 MGI: 102967 HomoloGene: 21207 IUPHAR: 287 ChEMBL: 1945 GeneCards: MTNR1A Gene |
Gene ontology |
Molecular function |
• protein binding
• melatonin receptor activity
• hormone binding
• organic cyclic compound binding
|
Cellular component |
• plasma membrane
• integral component of plasma membrane
• receptor complex
|
Biological process |
• G-protein coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger
• mating behavior
• circadian rhythm
• positive regulation of cGMP biosynthetic process
|
Sources: Amigo / QuickGO |
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RNA expression pattern |
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More reference expression data |
Orthologs |
Species |
Human |
Mouse |
|
Entrez |
4543 |
17773 |
|
Ensembl |
ENSG00000168412 |
ENSMUSG00000054764 |
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UniProt |
P48039 |
Q61184 |
|
RefSeq (mRNA) |
NM_005958 |
NM_008639 |
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RefSeq (protein) |
NP_005949 |
NP_032665 |
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Location (UCSC) |
Chr 4:
186.53 – 186.56 Mb |
Chr 8:
45.07 – 45.09 Mb |
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PubMed search |
[1] |
[2] |
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Melatonin receptor type 1A is a protein that in humans is encoded by the MTNR1A gene.[1][2]
Contents
- 1 Function
- 2 Ligands
- 3 See also
- 4 References
- 5 Further reading
Function
This gene encodes the MT1 protein, one of two high-affinity forms of a receptor for melatonin, the primary hormone secreted by the pineal gland. This receptor is a G protein-coupled, 7-transmembrane receptor that is responsible for melatonin effects on mammalian circadian rhythm and reproductive alterations affected by day length. The receptor is an integral membrane protein that is readily detectable and localized to two specific regions of the brain. The hypothalamic suprachiasmatic nucleus appears to be involved in circadian rhythm while the hypophysial pars tuberalis may be responsible for the reproductive effects of melatonin.[2]
Ligands
- Melatonin – full agonist
- Afobazole – agonist
See also
- Melatonin receptor
- Discovery and development of melatonin receptor agonists
References
- ^ Slaugenhaupt SA, Roca AL, Liebert CB, Altherr MR, Gusella JF, Reppert SM (May 1995). "Mapping of the gene for the Mel1a-melatonin receptor to human chromosome 4 (MTNR1A) and mouse chromosome 8 (Mtnr1a)". Genomics 27 (2): 355–7. doi:10.1006/geno.1995.1056. PMID 7558006.
- ^ a b "Entrez Gene: MTNR1A melatonin receptor 1A".
Further reading
- Brzezinski A (Jan 1997). "Melatonin in humans". The New England Journal of Medicine 336 (3): 186–95. doi:10.1056/NEJM199701163360306. PMID 8988899.
- Khan AU, Olson DL (Aug 1975). "Physical therapy and exercise-induced bronchospasm". Physical Therapy 55 (8): 878–81. PMID 1144527.
- Reppert SM, Weaver DR, Ebisawa T (Nov 1994). "Cloning and characterization of a mammalian melatonin receptor that mediates reproductive and circadian responses". Neuron 13 (5): 1177–85. doi:10.1016/0896-6273(94)90055-8. PMID 7946354.
- Witt-Enderby PA, Dubocovich ML (Jul 1996). "Characterization and regulation of the human ML1A melatonin receptor stably expressed in Chinese hamster ovary cells". Molecular Pharmacology 50 (1): 166–74. PMID 8700109.
- Witt-Enderby PA, Masana MI, Dubocovich ML (Jul 1998). "Physiological exposure to melatonin supersensitizes the cyclic adenosine 3',5'-monophosphate-dependent signal transduction cascade in Chinese hamster ovary cells expressing the human mt1 melatonin receptor". Endocrinology 139 (7): 3064–71. doi:10.1210/en.139.7.3064. PMID 9645677.
- Ebisawa T, Kajimura N, Uchiyama M, Katoh M, Sekimoto M, Watanabe T et al. (Sep 1999). "Alleic variants of human melatonin 1a receptor: function and prevalence in subjects with circadian rhythm sleep disorders". Biochemical and Biophysical Research Communications 262 (3): 832–7. doi:10.1006/bbrc.1999.1308. PMID 10471411.
- Brydon L, Roka F, Petit L, de Coppet P, Tissot M, Barrett P et al. (Dec 1999). "Dual signaling of human Mel1a melatonin receptors via G(i2), G(i3), and G(q/11) proteins". Molecular Endocrinology 13 (12): 2025–38. doi:10.1210/me.13.12.2025. PMID 10598579.
- Niles LP, Wang J, Shen L, Lobb DK, Younglai EV (Oct 1999). "Melatonin receptor mRNA expression in human granulosa cells". Molecular and Cellular Endocrinology 156 (1-2): 107–10. doi:10.1016/S0303-7207(99)00135-5. PMID 10612428.
- Song CK, Bartness TJ (Aug 2001). "CNS sympathetic outflow neurons to white fat that express MEL receptors may mediate seasonal adiposity". American Journal of Physiology. Regulatory, Integrative and Comparative Physiology 281 (2): R666–72. PMID 11448873.
- Roy D, Angelini NL, Fujieda H, Brown GM, Belsham DD (Nov 2001). "Cyclical regulation of GnRH gene expression in GT1-7 GnRH-secreting neurons by melatonin". Endocrinology 142 (11): 4711–20. doi:10.1210/en.142.11.4711. PMID 11606436.
- Savaskan E, Olivieri G, Meier F, Brydon L, Jockers R, Ravid R et al. (Jan 2002). "Increased melatonin 1a-receptor immunoreactivity in the hippocampus of Alzheimer's disease patients". Journal of Pineal Research 32 (1): 59–62. doi:10.1034/j.1600-079x.2002.00841.x. PMID 11841602.
- Savaskan E, Wirz-Justice A, Olivieri G, Pache M, Kräuchi K, Brydon L et al. (Apr 2002). "Distribution of melatonin MT1 receptor immunoreactivity in human retina". The Journal of Histochemistry and Cytochemistry 50 (4): 519–26. doi:10.1177/002215540205000408. PMID 11897804.
- Ayoub MA, Couturier C, Lucas-Meunier E, Angers S, Fossier P, Bouvier M et al. (Jun 2002). "Monitoring of ligand-independent dimerization and ligand-induced conformational changes of melatonin receptors in living cells by bioluminescence resonance energy transfer". The Journal of Biological Chemistry 277 (24): 21522–8. doi:10.1074/jbc.M200729200. PMID 11940583.
- Yuan L, Collins AR, Dai J, Dubocovich ML, Hill SM (Jun 2002). "MT(1) melatonin receptor overexpression enhances the growth suppressive effect of melatonin in human breast cancer cells". Molecular and Cellular Endocrinology 192 (1-2): 147–56. doi:10.1016/S0303-7207(02)00029-1. PMID 12088876.
- Slominski A, Pisarchik A, Zbytek B, Tobin DJ, Kauser S, Wortsman J (Jul 2003). "Functional activity of serotoninergic and melatoninergic systems expressed in the skin". Journal of Cellular Physiology 196 (1): 144–53. doi:10.1002/jcp.10287. PMID 12767050.
- Morcuende JA, Minhas R, Dolan L, Stevens J, Beck J, Wang K et al. (Sep 2003). "Allelic variants of human melatonin 1A receptor in patients with familial adolescent idiopathic scoliosis". Spine 28 (17): 2025–8; discussion 2029. doi:10.1097/01.BRS.0000083235.74593.49. PMID 12973153.
- Aust S, Thalhammer T, Humpeler S, Jäger W, Klimpfinger M, Tucek G et al. (Jan 2004). "The melatonin receptor subtype MT1 is expressed in human gallbladder epithelia". Journal of Pineal Research 36 (1): 43–8. doi:10.1046/j.1600-079X.2003.00095.x. PMID 14675129.
Melatonergics
|
|
Receptor
ligands |
Agonists
|
- Agomelatine
- GR-196,429
- LY-156,735
- Melatonin
- NAS (Normelatonin)
- Ramelteon
- Tasimelteon
|
|
Antagonists
|
- Afobazole
- Luzindole
- Prazosin (at MT3)
|
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Enzyme
inhibitors |
Anabolism
|
AANAT inhibitors
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ASMT inhibitors
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Catabolism
|
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Others |
Precursors
|
- L-Tryptophan → 5-HTP → Serotonin → NAS (Normelatonin)
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Cofactors
|
- Ferrous Iron (Fe2+)
- Magnesium (Mg2+)
- S-Adenosyl-L-methionine
- Tetrahydrobiopterin
- Vitamin B3 (Niacin
- nicotinamide → NADPH)
- Vitamin B6 (Pyridoxine
- Pyridoxamine
- Pyridoxal → Pyridoxal phosphate)
- Vitamin B9 (Folic acid → Tetrahydrofolic acid)
- Vitamin C (Ascorbic acid)
- Zinc (Zn2+)
|
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See also: Adrenergics • Dopaminergics • Serotonergics
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UpToDate Contents
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English Journal
- Gender-related invasion differences associated with mRNA expression levels of melatonin membrane receptors in colorectal cancer.
- León J, Casado J, Carazo A, Sanjuán L, Maté A, Muñoz de Rueda P, de la Cueva P, Quiles R, Ruíz S, Ruíz-Extremera A, Salmerón J.SourceSan Cecilio University Hospital, Granada, Spain; Centro de Investigación Biomédica en Red de Enfermedades Hepáticas y Digestivas (CIBERehd), Barcelona, Spain.
- Molecular carcinogenesis.Mol Carcinog.2012 Aug;51(8):608-18. doi: 10.1002/mc.20832. Epub 2011 Aug 1.
- Melatonin inhibits growth and invasive capacity of colon cancer cells in vitro through its membrane (MT1 and MT2) and/or nuclear receptors (RORα). Previous studies showed that this indoleamine is present in both the normal and colon cancer at similar levels. Therefore, we analyzed MT1, MT2, and ROR
- PMID 21809392
- The antidepressant agomelatine inhibits stress-mediated changes in amino acid efflux in the rat hippocampus and amygdala.
- Reagan LP, Reznikov LR, Evans AN, Gabriel C, Mocaër E, Fadel JR.SourceDepartment of Pharmacology, Physiology and Neuroscience, University of South Carolina School of Medicine, 6439 Garners Ferry Rd, Columbia, SC 29208, USA.
- Brain research.Brain Res.2012 Jul 23;1466:91-8. Epub 2012 May 27.
- Agomelatine is a potent melatonergic (MT1 and MT2) receptor agonist and 5HT(2C) antagonist that is an effective antidepressant in animal models of depression and in patients suffering from depression. Our recent studies revealed that acute restraint stress increases extracellular levels of glutamate
- PMID 22647752
Japanese Journal
- ラメルテオンの基礎研究 (特集 ラメルテオンの基礎と臨床)
- メラトニン受容体作動薬ラメルテオン(ロゼレム^【○!R】錠8mg)の薬理作用と臨床試験成績
- 平井 圭介,加藤 浩紀,西川 久夫,行弘 信仁,西山 啓次,宮本 政臣
- 日本薬理学雑誌 136(1), 51-60, 2010-07-01
- … ,筋弛緩作用,前向性健忘,反跳性不眠,依存性などの種々の有害作用を惹起する.これに対してラメルテオン(Ramelteon,TAK-375,商品名Rozerem®)は,主に視床下部視交叉上核に存在するメラトニン受容体(MT1/MT2受容体)にアゴニストとして作用してcAMP産生系を抑制し,サルおよびネコで強力な睡眠誘発作用を示した.その睡眠パターンは自然睡眠に極めて近いものであった.また,既存薬で見られる学習記憶障害 …
- NAID 10026544589
Related Links
- Receptor, Melatonin, Mt1; Melatonin MT1 Receptor. On-line free medical diagnosis assistant. Ranked list of possible diseases from either several symptoms or a full patient history. A similarity measure between symptoms and ...
- 1. Endocrine. 2005 Jul;27(2):101-10. Functional MT1 and MT2 melatonin receptors in mammals. Dubocovich ML, Markowska M. Melatonin, dubbed the hormone of darkness, is known to regulate a wide variety of physiological ...
★リンクテーブル★
[★]
- 関
- MT1 receptor
[★]
- 英
- MT1 receptor
- 関
- MT1メラトニン受容体、MT1受容体
[★]
- 英
- MT1 receptor
- 関
- MT1レセプター
[★]
[★]
メチオニン methionine