2020
Chronic mirabegron treatment increases human brown fat, HDL cholesterol, and insulin sensitivity
O'Mara A, Johnson J, Linderman J, Brychta R, McGehee S, Fletcher L, Fink Y, Kapuria D, Cassimatis T, Kelsey N, Cero C, Sater Z, Piccinini F, Baskin A, Leitner B, Cai H, Millo C, Dieckmann W, Walter M, Javitt N, Rotman Y, Walter P, Ader M, Bergman R, Herscovitch P, Chen K, Cypess A. Chronic mirabegron treatment increases human brown fat, HDL cholesterol, and insulin sensitivity. Journal Of Clinical Investigation 2020, 130: 2209-2219. PMID: 31961826, PMCID: PMC7190915, DOI: 10.1172/jci131126.Peer-Reviewed Original ResearchConceptsBAT metabolic activityIntravenous glucose tolerance testGlucose tolerance testΒ3-AR agonistInsulin sensitivityTolerance testMetabolic diseasesObesity-related metabolic diseasesWhite adipose tissue lipolysisBrown adipose tissue thermogenesisOpen-label studyTotal bile acidsHuman brown fatHigher insulin sensitivityAdipose tissue lipolysisAdipose tissue thermogenesisPET/CTΒ3-adrenergic receptor agonistIntramural Research ProgramChronic pharmacological stimulationMetabolic activityMirabegron therapyMirabegron treatmentPrimary endpointSecondary endpoints
2018
Regulation of Human Adipose Tissue Activation, Gallbladder Size, and Bile Acid Metabolism by a β3-Adrenergic Receptor Agonist
Baskin AS, Linderman JD, Brychta RJ, McGehee S, Anflick-Chames E, Cero C, Johnson JW, O'Mara AE, Fletcher LA, Leitner BP, Duckworth CJ, Huang S, Cai H, Garraffo HM, Millo CM, Dieckmann W, Tolstikov V, Chen EY, Gao F, Narain NR, Kiebish MA, Walter PJ, Herscovitch P, Chen KY, Cypess AM. Regulation of Human Adipose Tissue Activation, Gallbladder Size, and Bile Acid Metabolism by a β3-Adrenergic Receptor Agonist. Diabetes 2018, 67: db180462. PMID: 29980535, PMCID: PMC6152342, DOI: 10.2337/db18-0462.Peer-Reviewed Original ResearchMeSH KeywordsAcetanilidesAdipose Tissue, BrownAdolescentAdrenergic beta-AgonistsAdultAgedAged, 80 and overAnimalsBile Acids and SaltsGallbladderHealthy VolunteersHumansMiceMice, Inbred C57BLMiddle AgedReceptors, Adrenergic, betaReceptors, Adrenergic, beta-3RNA, MessengerThermogenesisThiazolesYoung AdultConceptsBile acid metabolismΒ3-adrenergic receptor agonistBrown adipose tissueReceptor agonistGallbladder sizeSelective β3-AR agonistΒ3-AR agonist mirabegronPositron emission tomography/White adipose tissue lipolysisUrinary bladder relaxationΒ3-AR mRNADose-proportional increaseDoses of placeboObesity-related complicationsBAT metabolic activityEmission tomography/Adipose tissue lipolysisHuman β3-ARAcid metabolismΒ3-AR agonistConjugated bile acidsGallbladder relaxationBladder relaxationOveractive bladderHealthy men