生物活性

• 描述Minoxidil (U10858) is an ATP-sensitive potassium (KATP) channel opener, a potent oral antihypertensive agent and a peripheral vasodilator that promotes vasodilation also affects hair growth. Minoxidil is also a potent inhibitor of soybean lipoxygenaseare with an IC50 of 20 μM. Minoxidil (0.01 mmoL/kg body weight; intraperitoneal injection; for 3.5 hours; fisher 344 rats) treatment inhibits carrageenan-induced rat paw oedema with an inhibitory potency (49%)^[3]. Minoxidil induces generalized hypertrichosis when administered systemically, or localized hair regrowth when applied topically to sites of severe alopecia areata. In the presence of minoxidil, cultures showed a marked dose-dependent second peak of DNA synthesis 8-10 days after culture initiation in epidermal cells. In addition, two morphologically distinct cell types appeared^[4]. Minoxidil is a potassium channel opener, causing hyperpolarization of cell membranes and it is also a vasodilator, by widening blood vessels and opening potassium channels, it allows more oxygen, blood and nutrients to the follicle. This can also cause follicles in the telogen phase to shed, usually soon to be replaced by new, thicker hairs in a new anagen phase. The most common adverse reactions of the topical formulation are limited to irritant and allergic contact dermatitis on the scalp^[5].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT00283686	Kidney, Polycystic	Phase 3	Completed	-	United States, Colorado ... more >> University of Colorado Health Sciences Center Denver (Aurora), Colorado, United States, 800045 United States, Georgia Emory University School of Medicine Atlanta, Georgia, United States, 30322 United States, Kansas University of Kansas Medical Center Kansas City, Kansas, United States, 66160 United States, Massachusetts Tufts University-New England Medical Center Boston, Massachusetts, United States, 02111 Beth Israel Deaconess Medical Center Boston, Massachusetts, United States, 02215 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 United States, Ohio Cleveland Clinic Foundation Cleveland, Ohio, United States, 44195 Collapse <<
  NCT00283686	-	-	Completed	-	-
  NCT01227031	-	-	Unknown	July 2011	Taiwan ... more >> Taipei Medical University-Wan Fang Hospital Not yet recruiting Taipei, Taiwan Contact: Ren-Yu Tsai    886-2-29307930 ext 2980    b671022@tmu.edu.tw Collapse <<

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• 参考文献

• [1] Grice JE, Ciotti S, et al. Relative uptake of minoxidil into appendages and stratum corneum and permeation through human skin in vitro. J Pharm Sci. 2010 Feb;99(2):712-8.

  [2] Grice JE, Ciotti S, et al. Relative uptake of minoxidil into appendages and stratum corneum and permeation through human skin in vitro. J Pharm Sci. 2010 Feb;99(2):712-8.

  [3] Hadjipavlou-Litina D, Magoulas GE, Bariamis SE, et al. Synthesis and evaluation of the antioxidative potential of minoxidil-polyamine conjugates. Biochimie. 2013;95(7):1437-1449

  [4] Cohen RL, Alves ME, Weiss VC, West DP, Chambers DA. Direct effects of minoxidil on epidermal cells in culture. J Invest Dermatol. 1984;82(1):90-93

  [5] Rossi A, Cantisani C, Melis L, Iorio A, Scali E, Calvieri S. Minoxidil use in dermatology, side effects and recent patents. Recent Pat Inflamm Allergy Drug Discov. 2012;6(2):130-136

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