Beta-3 adrenergički receptor

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Beta-3 adrenergički receptor
Identifikatori
Simboli ADRB3; BETA3AR
Vanjski ID OMIM109691 MGI87939 HomoloGene37250 IUPHAR: β3-adrenoceptor GeneCards: ADRB3 Gene
Pregled RNK izražavanja
PBB GE ADRB3 206812 at tn.png
PBB GE ADRB3 217303 s at tn.png
podaci
Ortolozi
Vrsta Čovek Miš
Entrez 155 11556
Ensembl ENSG00000188778 ENSMUSG00000031489
UniProt P13945 Q3UP63
RefSeq (mRNA) NM_000025 NM_013462
RefSeq (protein) NP_000016 NP_038490
Lokacija (UCSC) Chr 8:
37.94 - 37.94 Mb
Chr 8:
28.69 - 28.7 Mb
PubMed pretraga [1] [2]

Beta-3 adrenergički receptor3 adrenoreceptor), takođe poznat kao ADRB3, je beta-adrenergički receptor. ADRB3 je takođe oznaka za ljudski gen koji ga kodira.[1]

Funkcija[uredi - уреди | uredi izvor]

Dejstva β3 receptora obuhvataju:

Ova receptor je lociran uglavnom u adipoznom tkivu i učestvuje u regulaciji lipolize i termogeneze. Za neki β3 agoniste je utvrđeno da imaju antistresno dejstvo u studijama na životinjama. To sugestira da ovaj receptor takođe ima ulogu u CNS. Beta3-receptori su nađeni u žučnoj kesi, mokraćnoj bešiki, i u moždanom adipoznom tkivu. Njihova uloga u fiziologiji žučne kese je nepoznata, mada se smatra da učestvuju u lipolizi i termogenezi u smeđoj masnoći. Smatra se da u mokraćnoj bešiki izazivaju relaksaciju bešike i sprečavaju mokrenje.[4]

Mehanizam akcije[uredi - уреди | uredi izvor]

Beta adrenergički receptori učestvuju u epinefrinom i norepinefrinom indukovanoj aktivaciji adenilat ciklaze putem aktivacije G proteina Gs tipa.[5]

Agonisti[uredi - уреди | uredi izvor]

  • L-796,568[9]
  • CL-316,243[10]
  • LY-368,842
  • Ro40-2148

Selektivni β3 agonisti mogu potencijalno da pospeše umanjenje telesne težine putem modulacije lipolize.[2]

Antagonisti[uredi - уреди | uredi izvor]

Interakcije[uredi - уреди | uredi izvor]

Za beta-3 adrenergički receptor je pokazano da interaguje sa Src.[13]

Reference[uredi - уреди | uredi izvor]

  1. "Entrez Gene: ADRB1 adrenergic, beta-1-, receptor". http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=153. 
  2. 2,0 2,1 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. PMID 15935402. doi:10.1016/j.lfs.2005.04.008. 
  3. Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4.  Page 163
  4. Masaaki Sawa, Hiroshi Harada (2006). "Recent Developments in the Design of Orally Bioavailable β3-Adrenergic Receptor Agonists". Current Medicinal Chemistry 13 (1): 25–37. PMID 16457637. doi:10.2174/092986706775198006. 
  5. "Entrez Gene: ADRB3 adrenergic, beta-3-, receptor". http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=155. 
  6. 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. PMID 17669397. doi:10.1016/j.ejphar.2007.06.048. 
  7. 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. PMID 18358519. doi:10.1016/j.pbb.2008.02.020. 
  8. Hicks A, McCafferty GP, Riedel E, Aiyar N, Pullen M, Evans C, Luce TD, Coatney RW, Rivera GC, Westfall TD, Hieble JP (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. PMID 17626794. doi:10.1124/jpet.107.125757. 
  9. Larsen TM, Toubro S, van Baak MA, Gottesdiener KM, Larson P, Saris WH, Astrup A (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. 
  10. 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. PMID 18304529. doi:10.1016/j.ejphar.2008.01.028. 
  11. 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. 
  12. Bexis S, Docherty JR (April 2009). "Role of alpha(1)- 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. PMC 2795232. PMID 19422394. doi:10.1111/j.1476-5381.2009.00186.x. 
  13. Cao, W; Luttrell L M, Medvedev A V, Pierce K L, Daniel K W, Dixon T M, Lefkowitz R J, Collins S (December 2000). "Direct binding of activated c-Src to the beta 3-adrenergic receptor is required for MAP kinase activation". J. Biol. Chem. (UNITED STATES) 275 (49): 38131–4. ISSN 0021-9258. PMID 11013230. doi:10.1074/jbc.C000592200. 

Literatura[uredi - уреди | uredi izvor]

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  • Cao W, Luttrell LM, Medvedev AV 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. PMID 11013230. doi:10.1074/jbc.C000592200. 
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