Activation of human brown adipose tissue by a β3-adrenergic receptor agonist.
Activation of human brown adipose tissue by a β3-adrenergic receptor agonist.
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DOI：
10.1016/j.cmet.2014.12.009
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发表时间：
2015-01-06
期刊：
影响因子：
29
通讯作者：
Kolodny GM
中科院分区：
文献类型：
--
作者：
Cypess AM;Weiner LS;Roberts-Toler C;Franquet Elía E;Kessler SH;Kahn PA;English J;Chatman K;Trauger SA;Doria A;Kolodny GM
通过激活内源性棕色脂肪组织(BAT)增加能量消耗是治疗肥胖和糖尿病的一种潜在方法。这类β3肾上腺素能受体(AR)激动剂可以刺激啮齿动物蝙蝠，但这种活性从未在人类身上得到证实。在这里，我们确定了与安慰剂相比，200毫克口服米拉贝格隆(美贝特，阿斯特拉斯制药公司)刺激BAT的能力。米拉贝格隆是一种目前被批准用于治疗膀胱过度活跃的β3-AR激动剂。在所有12名健康男性受试者中，通过正电子发射断层扫描结合计算机断层扫描的18F-脱氧葡萄糖测定，米拉贝格隆导致BAT代谢活性增加(p=0.001)，并使静息代谢率增加203±40千卡/天(+13%；p=0.001)。BAT代谢活动也是RMR变化的重要预测因子(p=0.006)。因此，β-3-AR激动剂可以刺激人BAT的产热，有望成为治疗代谢性疾病的一种有前途的药物。
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.
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影响因子：
7.7
作者：
Saito M;Okamatsu-Ogura Y;Matsushita M;Watanabe K;Yoneshiro T;Nio-Kobayashi J;Iwanaga T;Miyagawa M;Kameya T;Nakada K;Kawai Y;Tsujisaki M
通讯作者：
Tsujisaki M
影响因子：
5.8
作者：
Sacks, Harold S.;Fain, John N.;Symonds, Michael E.
通讯作者：
Symonds, Michael E.
影响因子：
5.8
作者：
Chen, Kong Y.;Brychta, Robert J.;Celi, Francesco S.
通讯作者：
Celi, Francesco S.
影响因子：
1.8
作者：
Chapple, Christopher R.;Dvorak, Vladimir;Radziszewski, Pjotr;Van Kerrebroeck, Philip;Wyndaele, Jean Jacques;Bosman, Brigitte;Boerrigter, Peter;Drogendijk, Ted;Ridder, Arwin;Van der Putten-Slob, Ingrid;Yamaguchi, Osamu
通讯作者：
Yamaguchi, Osamu
影响因子：
168.9
作者：
Hall, Kevin D.;Sacks, Gary;Chandramohan, Dhruva;Chow, Carson C.;Wang, Y. Claire;Gortmaker, Steven L.;Swinburn, Boyd A.
通讯作者：
Swinburn, Boyd A.