베타-3 아드레날린 수용체 (β3 아드레날린 수용체)는 ADRB3으로도 알려져 있는데, 베타 아드레날린 수용체의 일종으로 이를 인코딩하는 인간 유전자를 지칭하기도 한다.[5]
β 3 수용체의 작용에는 다음이 포함된다.
주로 지방 조직에 위치하며 지방 분해 및 열 발생 조절에 관여한다. 일부 β 3 작용제는 항 스트레스 효과가 동물 실험에서 밝혀졌는데, 이는 중추 신경계 (CNS)에서도 역할을 한다는 점을 암시한다. β 3 수용체는 담낭, 방광 및 갈색 지방 조직에서 발견된다. 담낭 생리학에서 그들의 역할은 알려지지 않았지만 갈색 지방에서 지방 분해 및 열 발생에 역할을하는 것으로 생각된다. 방광에서는 방광의 이완과 배뇨 방지를 유발하는 것으로 알려져 있다.[8]
베타 아드레날린 수용체는 Gs 유형의 G 단백질의 작용을 통하여 에피네프린 또는 노르에피네프린에 의하여 유도되는 아데닐레이트 사이클라제의 활성화에 관련되어 있다.[5]
- Amibegron (SR-58611A)[9][10]
- BRL-37344[11]
- CL-316,243[12]
- L-742,791[13]
- L-796,568[14]
- LY-368,842
- Mirabegron (YM-178),[15] 일본, 미국, 영국, 캐나다, 중국 및 인도에서 과민성 방광 치료로 승인됨.
- Nebivolol[16] 선택적 베타 (1) 차단제 및 베타 (3) 작용제.
- Ro40-2148
- 솔라베그론 (GW-427,353)[17]
- Vibegron (MK-4618)[18]
- L-748,328[13]
- L-748,337[13]
- SR 59230A는 원래 선택적 β 3 길항제로 생각되었는데,[19] 그 후, α1 수용체의 길항제인 것으로 밝혀졌다.[20]
베타-3 아드레날린 수용체는 Src와 상호 작용하는 것으로 밝혀졌다.[21]
- ↑ 가 나 다 GRCh38: Ensembl release 89: ENSG00000188778 - 앙상블, May 2017
- ↑ 가 나 다 GRCm38: Ensembl release 89: ENSMUSG00000031489 - 앙상블, May 2017
- ↑ “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》.
- ↑ 가 나 “Entrez Gene: ADRB3 adrenergic, beta-3-, receptor”.
- ↑ “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. September 2005. doi:10.1016/j.lfs.2005.04.008. PMID 15935402.
- ↑ Rang, H. P. (2003). 《Pharmacology》. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4.
- ↑ “Recent Developments in the Design of Orally Bioavailable β3-Adrenergic Receptor Agonists”. 《Current Medicinal Chemistry》 13 (1): 25–37. 2006. doi:10.2174/092986706775198006. PMID 16457637.
- ↑ “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. November 2007. doi:10.1016/j.ejphar.2007.06.048. PMID 17669397.
- ↑ “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. June 2008. doi:10.1016/j.pbb.2008.02.020. PMID 18358519.
- ↑ “BRL37344 stimulates GLUT4 translocation and glucose uptake in skeletal muscle via β2-adrenoceptors without causing classical receptor desensitization”. 《American Journal of Physiology. Regulatory, Integrative and Comparative Physiology》 316 (5): R666–R677. May 2019. doi:10.1152/ajpregu.00285.2018. PMID 30892909.
- ↑ “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. 2008. doi:10.1016/j.ejphar.2008.01.028. PMID 18304529.
- ↑ 가 나 다 “Potent and selective human beta(3)-adrenergic receptor antagonists.”. 《The Journal of Pharmacology and Experimental Therapeutics》 290 (2): 649–55. Aug 1999. PMID 10411574.
- ↑ “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. 2002. doi:10.1093/ajcn/76.4.780. PMID 12324291.
- ↑ “Mirabegron for the treatment of overactive bladder”. 《Drugs of Today》 48 (1): 25–32. 2012. doi:10.1358/dot.2012.48.1.1738056. PMID 22384458.
- ↑ “Nebivolol, a vasodilating selective beta(1)-blocker, is a beta(3)-adrenoceptor agonist in the nonfailing transplanted human heart”. 《J Am Coll Cardiol》 53 (17): 1532–8. doi:10.1016/j.jacc.2008.11.057. PMID 19389564.
- ↑ “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. October 2007. doi:10.1124/jpet.107.125757. PMID 17626794.
- ↑ “Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.”. 《Journal of Medicinal Chemistry》 59 (2): 609–23. January 2016. doi:10.1021/acs.jmedchem.5b01372. PMID 26709102.
- ↑ “Functional studies of the first selective β3-adrenergic receptor antagonist SR 59230A in rat brown adipocytes”. 《Mol. Pharmacol.》 49 (1): 7–14. 1996. PMID 8569714.
- ↑ “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. April 2009. doi:10.1111/j.1476-5381.2009.00186.x. PMC 2795232. PMID 19422394.
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- “β3-adrenoceptor”. 《IUPHAR Database of Receptors and Ion Channels》. International Union of Basic and Clinical Pharmacology. 2014년 12월 30일에 원본 문서에서 보존된 문서. 2021년 3월 25일에 확인함.
- 인간 ADRB3 게놈 위치와 ADRB3 유전자의 상세한 설명은 UCSC 게놈 브라우저에 있습니다.