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Here we report that telmisartan, a structurally unique angiotensin II receptor antagonist used for the treatment of hypertension, can function as a partial agonist of PPAR\u03b3; influence the expression of PPAR\u03b3 target genes involved in carbohydrate and lipid metabolism; and reduce glucose, insulin, and triglyceride levels in rats fed a high-fat, high-carbohydrate diet. None of the other commercially available angiotensin II receptor antagonists appeared to activate PPAR\u03b3 when tested at concentrations typically achieved in plasma with conventional oral dosing. In contrast to ordinary antihypertensive and antidiabetic agents, molecules that can simultaneously block the angiotensin II receptor and activate PPAR\u03b3 have the potential to treat both hemodynamic and biochemical features of the metabolic syndrome and could provide unique opportunities for the prevention and treatment of diabetes and cardiovascular disease in high-risk populations.<\/jats:p>","DOI":"10.1161\/01.hyp.0000123072.34629.57","type":"journal-article","created":{"date-parts":[[2004,3,8]],"date-time":"2004-03-08T20:53:50Z","timestamp":1078779230000},"page":"993-1002","update-policy":"https:\/\/doi.org\/10.1161\/crossmarkpolicy","source":"Crossref","is-referenced-by-count":908,"title":["Identification of Telmisartan as a Unique Angiotensin II Receptor Antagonist With Selective PPAR\u03b3\u2013Modulating Activity"],"prefix":"10.1161","volume":"43","author":[{"given":"Stephen C.","family":"Benson","sequence":"first","affiliation":[{"name":"From the Department of Biological Sciences (S.C.B., C.I.H.), California State University, Hayward; Bethesda Pharmaceuticals, Inc (H.A.P.), Bakersfield, Calif; Departments of Family Medicine (H.A.P.), Kern Medical Center and the University of California, Irvine; Department of Medicinal Chemistry (A.C., P.D., M.A.A.), University of Mississippi; the Institute of Physiology (M.P.), Czech Academy of Sciences, Center for Integrated Genomics, Prague, Czech Republic; and Department of Laboratory Medicine (N..."}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Harrihar A.","family":"Pershadsingh","sequence":"additional","affiliation":[{"name":"From the Department of Biological Sciences (S.C.B., C.I.H.), California State University, Hayward; Bethesda Pharmaceuticals, Inc (H.A.P.), Bakersfield, Calif; Departments of Family Medicine (H.A.P.), Kern Medical Center and the University of California, Irvine; Department of Medicinal Chemistry (A.C., P.D., M.A.A.), University of Mississippi; the Institute of Physiology (M.P.), Czech Academy of Sciences, Center for Integrated Genomics, Prague, Czech Republic; 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