- 関
- adrenergic beta-3 receptor、beta3 adrenergic receptor
WordNet
- to remain unmolested, undisturbed, or uninterrupted -- used only in infinitive form; "let her be"
- work in a specific place, with a specific subject, or in a specific function; "He is a herpetologist"; "She is our resident philosopher" (同)follow
- have life, be alive; "Our great leader is no more"; "My grandfather lived until the end of war" (同)live
- be identical to; be someone or something; "The president of the company is John Smith"; "This is my house"
- happen, occur, take place; "I lost my wallet; this was during the visit to my parents house"; "There were two hundred people at his funeral"; "There was a lot of noise in the kitchen"
- have the quality of being; (copula, used with an adjective or a predicate noun); "John is rich"; "This is not a good answer"
- occupy a certain position or area; be somewhere; "Where is my umbrella?" "The toolshed is in the back"; "What is behind this behavior?"
- spend or use time; "I may be an hour"
- stake on the outcome of an issue; "I bet $100 on that new horse"; "She played all her money on the dark horse" (同)wager, play
- the act of gambling; "he did it on a bet" (同)wager
- maintain with or as if with a bet; "I bet she will be there!" (同)wager
- second in order of importance; "the candidate, considered a beta male, was perceived to be unable to lead his party to victory"
- the 2nd letter of the Greek alphabet
- preliminary or testing stage of a software or hardware product; "a beta version"; "beta software"
- 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
- drug that has the effects of epinephrine (同)adrenergic_drug
- relating to epinephrine (its release or action) (同)sympathomimetic
PrepTutorEJDIC
- 《連結語として補語を伴なって…『である』,…だ,…です / 《位置・場所を表す語句を伴って》(…に)『ある』,いる(occupy a place or situation) / 〈物事が〉『存在する』,ある(exist);〈生物が〉生存する,生きている(live) / 行われる,起こる,発生する(take place, occur) / 存続する,そのままでいる(remain as before) / 《『be to』 do》 / …する予定である,…することになっている / …すべきだ / 《受動態の不定詞を伴って》…できる / 《命令》…するのだ / 《条件節に》…する意図がある / 《『if…were to』 do》…するとしたなら / 《『be』 do『ing』》《進行形》 / 《進行中の動作》…している,しつつある / 《近い未来》…しようとしている,するつもり / 《動作の反復》(いつも)…している / 《『be』+『他動詞の過去分詞』》《受動態》…される,されている / 《『be』+『自動詞の過去分詞』》《完了形》…した[状態にある]
- 『かけ』・(…との)かけ《+『with』+『名』》 / かけた物(金) / かけの対象 / 〈金・物〉'を'『かける』 / (かけ事・ゲームなどで)〈人〉‘と'『かけをする』《+『名』〈人〉+『on』+『名』》 / (…に)『かける』《+『on』(『against』)+『名』(one's do『ing』)》
- ベータ(ギリシア語アルファベットの第2文字;B,β;英語のB,b に遭当)
- =sense organ / 受信装置
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2015/07/17 14:18:05」(JST)
[Wiki en表示]
Adrenoceptor beta 3 |
Available structures |
PDB |
Ortholog search: PDBe, RCSB |
List of PDB id codes |
2CDW
|
|
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Identifiers |
Symbols |
ADRB3 ; BETA3AR |
External IDs |
OMIM: 109691 MGI: 87939 HomoloGene: 37250 IUPHAR: 30 ChEMBL: 246 GeneCards: ADRB3 Gene |
Gene ontology |
Molecular function |
• beta-adrenergic receptor activity
• protein binding
• beta3-adrenergic receptor activity
• beta-3 adrenergic receptor binding
• protein homodimerization activity
• epinephrine binding
• norepinephrine binding
|
Cellular component |
• nucleus
• plasma membrane
• integral component of plasma membrane
• receptor complex
|
Biological process |
• temperature homeostasis
• diet induced thermogenesis
• vasodilation by norepinephrine-epinephrine involved in regulation of systemic arterial blood pressure
• desensitization of G-protein coupled receptor protein signaling pathway by arrestin
• carbohydrate metabolic process
• generation of precursor metabolites and energy
• energy reserve metabolic process
• receptor-mediated endocytosis
• G-protein coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger
• adenylate cyclase-modulating G-protein coupled receptor signaling pathway
• activation of adenylate cyclase activity
• cell-cell signaling
• aging
• response to cold
• heat generation
• negative regulation of multicellular organism growth
• eating behavior
• positive regulation of MAPK cascade
• response to antibiotic
• brown fat cell differentiation
• adenylate cyclase-activating adrenergic receptor signaling pathway
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Sources: Amigo / QuickGO |
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RNA expression pattern |
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More reference expression data |
Orthologs |
Species |
Human |
Mouse |
Entrez |
155 |
11556 |
Ensembl |
ENSG00000188778 |
ENSMUSG00000031489 |
UniProt |
P13945 |
P25962 |
RefSeq (mRNA) |
NM_000025 |
NM_013462 |
RefSeq (protein) |
NP_000016 |
NP_038490 |
Location (UCSC) |
Chr 8:
37.96 – 37.97 Mb |
Chr 8:
27.23 – 27.23 Mb |
PubMed search |
[1] |
[2] |
|
The beta-3 adrenergic receptor (β3 adrenoreceptor), also known as ADRB3, is a beta-adrenergic receptor, and also denotes the human gene encoding it.[1]
Contents
- 1 Function
- 2 Mechanism of action
- 3 Ligands
- 3.1 Agonists
- 3.2 Antagonists
- 4 Interactions
- 5 See also
- 6 References
- 7 Further reading
- 8 External links
Function
Actions of the β3 receptor include:
- Enhancement of lipolysis in adipose tissue.[2]
- Thermogenesis in skeletal muscle[3]
It is located mainly in adipose tissue and is involved in the regulation of lipolysis and thermogenesis. Some β3 agonists have demonstrated antistress effects in animal studies, suggesting it also has a role in the central nervous system (CNS). Beta3-Receptors are found in the gallbladder, urinary bladder, and in brown adipose tissue. Their role in gallbladder physiology is unknown, but they are thought to play a role in lipolysis and thermogenesis in brown fat. In the urinary bladder it is thought to cause relaxation of the bladder and prevention of urination.[4]
Mechanism of action
Beta adrenergic receptors are involved in the epinephrine- and norepinephrine-induced activation of adenylate cyclase through the action of the G proteins of the type Gs.[1]
Ligands
Agonists
- Amibegron (SR-58611A)[5][6]
- CL-316,243[7]
- L-742,791[8]
- L-796,568[9]
- LY-368,842
- Mirabegron (YM-178),[10] approved for treatment of overactive bladder in Japan, United States, UK, Canada, China and India.
- Ro40-2148
- Solabegron (GW-427,353)[11]
A selective β3 agonist has potential weight loss effects through modulation of lipolysis.[2]
Antagonists
- L-748,328[8]
- L-748,337[8]
- SR 59230A was thought to be a selective β3 antagonist[12] but later found to also be an antagonist of the α1 receptor.[13]
Interactions
Beta-3 adrenergic receptor has been shown to interact with Src.[14]
See also
- Other adrenergic receptors
- Alpha-1 adrenergic receptor
- Alpha-2 adrenergic receptor
- Beta-1 adrenergic receptor
- Beta-2 adrenergic receptor
- Beta Blocker
References
- ^ a b "Entrez Gene: ADRB3 adrenergic, beta-3-, receptor".
- ^ a b Ferrer-Lorente R, Cabot C, Fernández-López JA, Alemany M (September 2005). "Combined effects of oleoyl-estrone and a β3-adrenergic agonist (CL316,243) on lipid stores of diet-induced overweight male Wistar rats". Life Sciences 77 (16): 2051–8. doi:10.1016/j.lfs.2005.04.008. PMID 15935402.
- ^ Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4. Page 163
- ^ Sawa M, Harada H (2006). "Recent Developments in the Design of Orally Bioavailable β3-Adrenergic Receptor Agonists". Current Medicinal Chemistry 13 (1): 25–37. doi:10.2174/092986706775198006. PMID 16457637.
- ^ Consoli D, Leggio GM, Mazzola C, Micale V, Drago F (November 2007). "Behavioral effects of the β3 adrenoceptor agonist SR58611A: is it the putative prototype of a new class of antidepressant/anxiolytic drugs?". European Journal of Pharmacology 573 (1–3): 139–47. doi:10.1016/j.ejphar.2007.06.048. PMID 17669397.
- ^ Overstreet DH, Stemmelin J, Griebel G (June 2008). "Confirmation of antidepressant potential of the selective β3 adrenoceptor agonist amibegron in an animal model of depression". Pharmacology, Biochemistry, and Behavior 89 (4): 623–6. doi:10.1016/j.pbb.2008.02.020. PMID 18358519.
- ^ Fu L, Isobe K, Zeng Q, Suzukawa K, Takekoshi K, Kawakami Y (2008). "The effects of beta(3)-adrenoceptor agonist CL-316,243 on adiponectin, adiponectin receptors and tumor necrosis factor-alpha expressions in adipose tissues of obese diabetic KKAy mice". European Journal of Pharmacology 584 (1): 202–6. doi:10.1016/j.ejphar.2008.01.028. PMID 18304529.
- ^ a b c Candelore MR, Deng L, Tota L, Guan XM, Amend A, Liu Y et al. (Aug 1999). "Potent and selective human beta(3)-adrenergic receptor antagonists.". The Journal of Pharmacology and Experimental Therapeutics 290 (2): 649–55. PMID 10411574.
- ^ Larsen TM, Toubro S, van Baak MA, Gottesdiener KM, Larson P, Saris WH et al. (2002). "Effect of a 28-d treatment with L-796568, a novel β3-adrenergic receptor agonist, on energy expenditure and body composition in obese men". The American Journal of Clinical Nutrition 76 (4): 780–8. PMID 12324291.
- ^ Gras J (2012). "Mirabegron for the treatment of overactive bladder". Drugs of today (Barcelona, Spain : 1998) 48 (1): 25–32. doi:10.1358/dot.2012.48.1.1738056. PMID 22384458.
- ^ Hicks A, McCafferty GP, Riedel E, Aiyar N, Pullen M, Evans C et al. (October 2007). "GW427353 (solabegron), a novel, selective beta3-adrenergic receptor agonist, evokes bladder relaxation and increases micturition reflex threshold in the dog". The Journal of Pharmacology and Experimental Therapeutics 323 (1): 202–9. doi:10.1124/jpet.107.125757. PMID 17626794.
- ^ Nisoli E, Tonello C, Landi M, Carruba MO (1996). "Functional studies of the first selective β3-adrenergic receptor antagonist SR 59230A in rat brown adipocytes". Mol. Pharmacol. 49 (1): 7–14. PMID 8569714.
- ^ Bexis S, Docherty JR (April 2009). "Role of α1- and β3-adrenoceptors in the modulation by SR59230A of the effects of MDMA on body temperature in the mouse". British Journal of Pharmacology 158 (1): 259–66. doi:10.1111/j.1476-5381.2009.00186.x. PMC 2795232. PMID 19422394.
- ^ Cao W, Luttrell LM, Medvedev AV, Pierce KL, Daniel KW, Dixon TM et al. (2000). "Direct binding of activated c-Src to the beta 3-adrenergic receptor is required for MAP kinase activation". J. Biol. Chem. 275 (49): 38131–4. doi:10.1074/jbc.C000592200. PMID 11013230.
Further reading
- Granneman JG, Lahners KN, Rao DD (1993). "Rodent and human beta 3-adrenergic receptor genes contain an intron within the protein-coding block". Mol. Pharmacol. 42 (6): 964–70. PMID 1336117.
- Nahmias C, Blin N, Elalouf JM, Mattei MG, Strosberg AD, Emorine LJ (1991). "Molecular characterization of the mouse beta 3-adrenergic receptor: relationship with the atypical receptor of adipocytes". EMBO J. 10 (12): 3721–7. PMC 453106. PMID 1718744.
- Emorine LJ, Marullo S, Briend-Sutren MM, Patey G, Tate K, Delavier-Klutchko C et al. (1989). "Molecular characterization of the human beta 3-adrenergic receptor". Science 245 (4922): 1118–21. doi:10.1126/science.2570461. PMID 2570461.
- Guan XM, Amend A, Strader CD (1995). "Determination of structural domains for G protein coupling and ligand binding in beta 3-adrenergic receptor". Mol. Pharmacol. 48 (3): 492–8. PMID 7565630.
- Rodriguez M, Carillon C, Coquerel A, Le Fur G, Ferrara P, Caput D et al. (1995). "Evidence for the presence of beta 3-adrenergic receptor mRNA in the human brain". Brain Res. Mol. Brain Res. 29 (2): 369–75. doi:10.1016/0169-328X(94)00274-I. PMID 7609625.
- Clément K, Vaisse C, Manning BS, Basdevant A, Guy-Grand B, Ruiz J et al. (1995). "Genetic variation in the beta 3-adrenergic receptor and an increased capacity to gain weight in patients with morbid obesity". N. Engl. J. Med. 333 (6): 352–4. doi:10.1056/NEJM199508103330605. PMID 7609752.
- Dib A, Adélaïde J, Chaffanet M, Imbert A, Le Paslier D, Jacquemier J et al. (1995). "Characterization of the region of the short arm of chromosome 8 amplified in breast carcinoma". Oncogene 10 (5): 995–1001. PMID 7898940.
- Mahmoudian M (1994). "The complex of human Gs protein with the beta 3 adrenergic receptor: a computer-aided molecular modeling study". Journal of molecular graphics 12 (1): 22–8, 34. doi:10.1016/0263-7855(94)80004-9. PMID 8011597.
- Wilkie TM, Chen Y, Gilbert DJ, Moore KJ, Yu L, Simon MI et al. (1994). "Identification, chromosomal location, and genome organization of mammalian G-protein-coupled receptors". Genomics 18 (2): 175–84. doi:10.1006/geno.1993.1452. PMID 8288218.
- Krief S, Lönnqvist F, Raimbault S, Baude B, Van Spronsen A, Arner P et al. (1993). "Tissue distribution of beta 3-adrenergic receptor mRNA in man". J. Clin. Invest. 91 (1): 344–9. doi:10.1172/JCI116191. PMC 330032. PMID 8380813.
- van Spronsen A, Nahmias C, Krief S, Briend-Sutren MM, Strosberg AD, Emorine LJ (1993). "The promoter and intron/exon structure of the human and mouse beta 3-adrenergic-receptor genes". Eur. J. Biochem. 213 (3): 1117–24. doi:10.1111/j.1432-1033.1993.tb17861.x. PMID 8389293.
- Lelias JM, Kaghad M, Rodriguez M, Chalon P, Bonnin J, Dupre I et al. (1993). "Molecular cloning of a human beta 3-adrenergic receptor cDNA". FEBS Lett. 324 (2): 127–30. doi:10.1016/0014-5793(93)81377-C. PMID 8389717.
- Candelore MR, Deng L, Tota LM, Kelly LJ, Cascieri MA, Strader CD (1996). "Pharmacological characterization of a recently described human beta 3-adrenergic receptor mutant". Endocrinology 137 (6): 2638–41. doi:10.1210/en.137.6.2638. PMID 8641219.
- Fujisawa T, Ikegami H, Yamato E, Takekawa K, Nakagawa Y, Hamada Y et al. (1996). "Association of Trp64Arg mutation of the beta3-adrenergic-receptor with NIDDM and body weight gain". Diabetologia 39 (3): 349–52. doi:10.1007/BF00418352. PMID 8721782.
- Higashi K, Ishikawa T, Ito T, Yonemura A, Shige H, Nakamura H (1997). "Association of a genetic variation in the beta 3-adrenergic receptor gene with coronary heart disease among Japanese". Biochem. Biophys. Res. Commun. 232 (3): 728–30. doi:10.1006/bbrc.1997.6339. PMID 9126344.
- Hoffstedt J, Poirier O, Thörne A, Lönnqvist F, Herrmann SM, Cambien F et al. (1999). "Polymorphism of the human beta3-adrenoceptor gene forms a well-conserved haplotype that is associated with moderate obesity and altered receptor function". Diabetes 48 (1): 203–5. doi:10.2337/diabetes.48.1.203. PMID 9892244.
- Halushka MK, Fan JB, Bentley K, Hsie L, Shen N, Weder A et al. (1999). "Patterns of single-nucleotide polymorphisms in candidate genes for blood-pressure homeostasis". Nat. Genet. 22 (3): 239–47. doi:10.1038/10297. PMID 10391210.
- Kimura K, Sasaki N, Asano A, Mizukami J, Kayahashi S, Kawada T et al. (2000). "Mutated human beta3-adrenergic receptor (Trp64Arg) lowers the response to beta3-adrenergic agonists in transfected 3T3-L1 preadipocytes". Horm. Metab. Res. 32 (3): 91–6. doi:10.1055/s-2007-978597. PMID 10786926.
- Cao W, Luttrell LM, Medvedev AV, Pierce KL, Daniel KW, Dixon TM et al. (2001). "Direct binding of activated c-Src to the beta 3-adrenergic receptor is required for MAP kinase activation". J. Biol. Chem. 275 (49): 38131–4. doi:10.1074/jbc.C000592200. PMID 11013230.
- Russell ST, Hirai K, Tisdale MJ (2002). "Role of β3-adrenergic receptors in the action of a tumour lipid mobilizing factor". Br. J. Cancer 86 (3): 424–8. doi:10.1038/sj.bjc.6600086. PMC 2375201. PMID 11875710.
External links
- "β3-adrenoceptor". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
UpToDate Contents
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English Journal
- Patient and physician preferences for oral pharmacotherapy for overactive bladder: two discrete choice experiments.
- Heisen M1, Baeten SA1, Verheggen BG1, Stoelzel M2, Hakimi Z2, Ridder A2, van Maanen R2, Stolk EA3.
- Current medical research and opinion.Curr Med Res Opin.2016 Feb 12:1-10. [Epub ahead of print]
- Objective We examined patient and treating physician (general practitioners, urologists, and [uro]gynecologists) preferences for oral pharmacotherapy (antimuscarinics and beta-3 adrenoceptor agonists) for overactive bladder to gain a deeper understanding of which attributes drive their treatment dec
- PMID 26789823
- Association analysis of the beta-3 adrenergic receptor Trp64Arg (rs4994) polymorphism with urate and gout.
- Fatima T1, Altaf S1, Phipps-Green A1, Topless R1, Flynn TJ1, Stamp LK2, Dalbeth N3, Merriman TR4.
- Rheumatology international.Rheumatol Int.2016 Feb;36(2):255-61. doi: 10.1007/s00296-015-3370-6. Epub 2015 Sep 26.
- The Arg64 allele of variant rs4994 (Trp64Arg) in the β3-adrenergic receptor gene has been associated with increased serum urate and risk of gout. Our objective was to investigate the relationship of rs4994 with serum urate and gout in New Zealand European, Māori and Pacific subjects. A total of 17
- PMID 26410617
- Discovery of benzamides as potent human β3 adrenergic receptor agonists.
- Zhu C1, Kar NF2, Li B3, Costa M2, Dingley KH3, Di Salvo J3, Ha SN3, Hurley AL2, Li X2, Miller RR3, Salituro GM2, Struthers M3, Weber AE3, Hale JJ2, Edmondson SD3.
- Bioorganic & medicinal chemistry letters.Bioorg Med Chem Lett.2016 Jan 1;26(1):55-9. doi: 10.1016/j.bmcl.2015.11.030. Epub 2015 Nov 11.
- The paper will describe the synthesis and SAR studies that led to the discovery of benzamide (reverse amide) as potent and selective human β3-adrenergic receptor agonist. Based on conformationally restricted pyrrolidine scaffold we discovered earlier, pyrrolidine benzoic acid intermediate 22 was sy
- PMID 26590100
Japanese Journal
- 4) 幼少期の高アンドロゲン環境とインスリン抵抗性からみたPCOSの病因および管理に関する検討(シンポジウム3:生殖「多嚢胞性卵巣症候群(PCOS)の病因・病態と管理」,第65回日本産科婦人科学会・学術講演会)
- Beta-3-adrenergic receptor Trp64Arg polymorphism : does it modulate the relationship between exercise and percentage of body fat in young adult Japanese males?
- Environmental health and preventive medicine 18(4), 323-329, 2013-07-01
- NAID 10031189209
- Increased Norepinephrine by Medium-Chain Triglyceride Attributable to Lipolysis in White and Brown Adipose Tissue of C57BL/6J Mice
- Bioscience, biotechnology, and biochemistry 76(6), 1213-1218, 2012-06-23
- NAID 10030818451
Related Links
- 1. Medicina (Kaunas). 2004;40(5):407-13. Structure and function of beta3-adrenergic receptors. Skeberdis VA(1). Author information: (1)Institute of Cardiology, Kaunas University of Medicine, Lithuania. arske@kmu.lt Beta ...
- Learn about the importance of beta-3 adrenergic receptors in the bladder. Watch the mechanism of action (MOA) video. MYRBETRIQ for overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency, and urinary ...
Related Pictures
★リンクテーブル★
[★]
- 英
- beta3 adrenergic receptor、beta-3 adrenergic receptor, β3-AR, β3AR
- 同
- β3アドレナリンレセプター
- 関
- アドレナリン受容体、肥満
[★]
- 関
- beta-3 adrenergic receptor
[★]
アドレナリン受容体刺激薬、アドレナリン作用薬
- 関
- adrenergic、adrenergic agent、adrenergic agonist、adrenergic drug、adrenergic receptor agonist
[★]
[★]
β、ベータ
[★]
[★]
アドレナリン受容体