2015年1月19日訊 /生物谷BIOON/ --本文亮點：
β3-AR激活劑 mirabegron能快速激活人源棕色脂肪組織的葡萄糖攝取
β3-AR激活劑 mirabegron能快速激活人源白色脂肪組織脂類水解
Mirabegron能激活多個身體部位的棕色/米色脂肪組織
Mirabegron誘導產生的棕色脂肪組織活性是全身產熱的一項預測指標
通過激活內源性棕色脂肪組織（BAT，Brown Adipose Tissue）來增加機體能量消耗是治療肥胖和糖尿病的一種策略。β3-腎上腺素受體（β3-AR，β3-adrenergic receptor）激活劑類分子能夠激活鼠的棕色脂肪組織，但是人身上從未發現過類似現象。其中mirabegron作為β3-腎上腺素受體的激活劑，目前已被批准用於治療膀胱過度活動症。
研究者們給志願者口服200 mg mirabegron分子（商品名Myrbetriq，購自Astellas Pharma. Inc.），並與服用安慰劑的志願者們作對照，考察其活性。使用同位素18氟標記脫氧葡萄糖，並結合正電子發射斷層成像技術（PET，positron emission tomography）和計算機斷層掃描（CT，computed tomography）觀察，結果顯示在所有的12位健康男性志願者身上Mirabegron都能夠引起棕色脂肪組織更高的代謝活性（p=0.001）。而且相對於口服藥物之前，Mirabegron將志願者身體的靜息代謝速率（RMR，resting metabolic rate）提升到了203±40 千焦/天（增幅為13%， p=0.001）。同時研究者們認為棕色脂肪組織的代謝活性也是預測靜息代謝速率變化的一項重要參考依據（p=0.006）。
綜上，具有刺激人類棕色脂肪組織產熱的β3-腎上腺素受體激活劑理論上也許能作為一種治療代謝類疾病的藥物，讓我們拭目以待！（生物谷Bioon.com）
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生物谷推薦的英文摘要：
Cell Metabolism DOI: http://dx.doi.org/10.1016/j.cmet.2014.12.009
Activation of Human Brown Adipose Tissue by a β3-Adrenergic Receptor Agonist
Aaron M. Cypess, Lauren S. Weiner, Carla Roberts-Toler, Elisa Franquet Elía, Skyler H. Kessler, Peter A. Kahn, Jeffrey English, Kelly Chatman, Sunia A. Trauger, Alessandro Doria, Gerald M. Kolodny
Highlights
" oThe β3-AR agonist mirabegron acutely activates human BAT glucose uptake
" oThe β3-AR agonist mirabegron acutely activates human WAT lipolysis
" oMirabegron stimulates brown/beige fat in multiple depots.
" oMirabegron-induced BAT activity is a predictor of whole-body thermogenesis
Summary
Increasing energy expenditure through activation of endogenous brown adipose tissue (BAT) is a potential approach to treat obesity and diabetes. The class of β3-adrenergic receptor (AR) agonists stimulates rodent BAT, but this activity has never been demonstrated in humans. Here we determined the ability of 200 mg oral mirabegron (Myrbetriq, Astellas Pharma, Inc.), a β3-AR agonist currently approved to treat overactive bladder, to stimulate BAT as compared to placebo. Mirabegron led to higher BAT metabolic activity as measured via 18F-fluorodeoxyglucose (18F-FDG) using positron emission tomography (PET) combined with computed tomography (CT) in all twelve healthy male subjects (p = 0.001), and it increased resting metabolic rate (RMR) by 203 ± 40 kcal/day (+13%; p = 0.001). BAT metabolic activity was also a significant predictor of the changes in RMR (p = 0.006). Therefore, a β3-AR agonist can stimulate human BAT thermogenesis and may be a promising treatment for metabolic disease.