2016年6月24日星期五

Minoxidil Sulfate

Minoxidil an important step in understanding the mechanism of action on the hair follicle is the drug to determine the active form. We used to test the follicles of whiskers organ culture, either minoxidil or minoxidil sulfate its sulfated metabolite that stimulates hair growth. Follicles of newborn mice were cultured with or without medication and the effects assessed by measuring the incorporation of radiolabeled cysteine ​​in hair shafts treated follicles. Analyses of the sulfotransferase activity of minoxidil showed that metabolize vibrissae follicles Minoxidil Minoxidil. Dose-response studies have shown that the minoxidil sulfate is 14 times more powerful to stimulate incorporation into the cysteine ​​Minoxidil in the follicles in culture. Three drugs that block intrafollicular minoxidil sulfate production were tested for their effect on hair growth drug induced. Diethylcarbamazine proved to be an uncompetitive inhibitor of sulfotransferase and prevent stimulation of minoxidil, minoxidil sulfate, but not the growth of hair. intracellular PAPS formation with inhibition also blocked the chlorate effect of minoxidil, but no minoxidil sulfate. Acetaminophen sulfate powerful scavenger blocked Minoxidil incorporation cysteine. It also blocks follicle minoxidil sulfate protested directly to remove sulfate drug. Experiments with U-51607, a similar powerful minoxidil which also forms a sulfated metabolite, showed that its activity is inhibited by both chlorate and diethylcarbamazine. These studies show that sulfation is a critical step for the effects of minoxidil hair growth, and that this contact with the sulfated metabolite, hair follicles immediately.

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