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sxl8495

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Since the first isolation of melatonin in 1959. interest in this hormone has grown steadily. Of particular interest are the reports that melatonin has the ability to inhibit LH secretion. A major difficulty in assessing the physiological properties of melatonin is its very rapid metabolism. This rate of metabolism combined with the polyphasic nature of the process complicates estimation of a biological half-life for melatonin. Kopin et al, estimate that exogenously administered melatonin disappears from whole mice with a half-life of about 2 min through the first 10 min following injection but that after 40 min the half-life has grown to about 35 min. In this same report, data are presented indicating a plasma half-life in rats through the first 30 min of about 15 min. Maickel et al. have estimated the plasma half-life in rats to be about 12 min through the first 2 h following administration.
We undertook the synthesis of a variety of melatonin analogues with the intention of producing compounds with similar physiological properties but greater resistance to metabolism. A more general goal was to establish which features of the melatonin molecule are essential for activity and which sites will tolerate structural modification. In view of the evidence that the major route in the metabolism of melatonin is hydroxylation at the 6 position,' we were particularly interested in synthesizing analogues bearing substituents in that position.

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1楼 2009-03-09 08:56:32

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mayong11

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sxl8495(金币+15,VIP+0):我知有这么多了 3-11 14:48

自从在1959年第一次分离褪黑激素。人们对这个激素的关注稳步增长。特别令人感兴趣的报告说，褪黑激素有能力抑制LH的分泌。评估褪黑激素生理特性的一个主要困难是其非常迅速的新陈代谢。这一代谢速率结合多相性质复杂的过程可以用来估计褪黑素的生物半衰期。Kopin等人，估计外部褪黑素从整个小鼠消失的半衰期在注射后的最初10分钟里，大约为2分钟，但注射后40分钟后半衰期就增长到约35分钟。在这同一份报告中，数据的显示褪黑素在大鼠的血浆中半衰期在注射后30分钟后为15分钟，Maickel等人估计褪黑素在大鼠血浆半衰期在注射2小时后大约为12分钟。

[ Last edited by mayong11 on 2009-3-12 at 08:47 ]