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However, rodent studies suggest that these drugs could have other beneficial effects on human metabolism. We performed tissue receptor profiling and showed that the human \u03b23-AR mRNA is also highly expressed in gallbladder and brown adipose tissue (BAT). We next studied the clinical implications of this distribution in 12 healthy men given one-time randomized doses of placebo, the approved dose of 50 mg, and 200 mg of the \u03b23-AR agonist mirabegron. There was a more-than-dose-proportional increase in BAT metabolic activity as measured by [18F]-2-fluoro-D-2-deoxy-d-glucose positron emission tomography\/computed tomography (medians 0.0 vs. 18.2 vs. 305.6 mL \u22c5 mean standardized uptake value [SUVmean] \u22c5 g\/mL). Only the 200-mg dose elevated both nonesterified fatty acids (68%) and resting energy expenditure (5.8%). Previously undescribed increases in gallbladder size (35%) and reductions in conjugated bile acids were also discovered. Therefore, besides urinary bladder relaxation, the human \u03b23-AR contributes to white adipose tissue lipolysis, BAT thermogenesis, gallbladder relaxation, and bile acid metabolism. This physiology should be considered in the development of more selective \u03b23-AR agonists to treat obesity-related complications.<\/jats:p>","DOI":"10.2337\/db18-0462","type":"journal-article","created":{"date-parts":[[2018,7,6]],"date-time":"2018-07-06T13:46:52Z","timestamp":1530884812000},"page":"2113-2125","update-policy":"https:\/\/doi.org\/10.2337\/ada-journal-policies","source":"Crossref","is-referenced-by-count":138,"title":["Regulation of Human Adipose Tissue Activation, Gallbladder Size, and Bile Acid Metabolism by a \u03b23-Adrenergic Receptor Agonist"],"prefix":"10.2337","volume":"67","clinical-trial-number":[{"clinical-trial-number":"nct01950520","registry":"10.18810\/clinical-trials-gov"},{"clinical-trial-number":"nct01950520","registry":"10.18810\/clinical-trials-gov","type":"results"}],"author":[{"given":"Alison S.","family":"Baskin","sequence":"first","affiliation":[{"name":"Diabetes, Endocrinology, and Obesity Branch, Intramural Research Program, National Institute 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