作者: Gibson Km , Wang Wh , Quiggle Dd , Kantoci D , Pham T
DOI:
关键词: Biological activity 、 Vitamin E 、 Mechanism of action 、 Metabolite 、 Potassium channel 、 Loop of Henle 、 Pharmacology 、 Extracellular fluid 、 Internal medicine 、 gamma-Tocopherol 、 Chemistry 、 Endocrinology
摘要: The structural elucidation and mechanism of action a potential component, LLU-α, what is possibly multifactorial complex known as “natriuretic hormone” was recently reported [Wechter, W.J. et al. (1996a) Proc. Natl. Acad. Sci. U.S.A. 93: 6002–6007]. “Natriuretic hormone,” long-sought factor, believed to regulate extracellular fluid volume consequently be pathomimetic for hypertension, cirrhosis, congestive heart failure other expanded states. studies herein further characterize LLU-α. precursor the endogenous LLU-α demonstrated γ-tocopherol by radiolabeling studies. pharmacokinetics infused rac -LLU-α proved biphasic (half-lives: 12 min 6 h). Specificity inhibition 70 pS potassium channel thick ascending limb loop Henle examined with natural S -enantiomer being most potent inhibitor whereas analogous α-tocopherol metabolite, -5-Me-LLU-α, showed no inhibition. Rac does not inhibit two isozymes Na+/K+-ATPase. natriuretic acting via Na+/K+-ATPase, assumed hormone.” metabolite vitamin, if it were found play role in regulation volume, would second example vitamin hormone. Of considerable interest fact that this manuscript reports first biological activity γ-tocopherol, member E complex.