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一氧化氮合酶抑制剂的设计与合成

Design and Synthesis of Nitric Oxide Synthase Inhibitors

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【作者】 徐云根; 华维一;

【Author】 Xu Yungen Hua Weiyi (China Pharmaceutical University,Nanjing 210009)

【机构】 中国药科大学新药研究中心;

【摘要】 <正>一氮化氮(NO)是近年来发现的一种重要的生物第二信使,内源性的NO是由一氧化氮合酶(NOS)氧化L-精氨酸(L-Arg)产生的。由于许多疾病的病理过程与体内原先稳定的NO内环境发生变化有关,从而使得NOS成为引人注目的药物作用靶位。NOS有三种同功酶:eNOS

【Abstract】 Nitric oxide(NO) is an important biological second messenger.The endogenous NO is biosynthesized by the oxidation of L-arginine(L-Arg) by a family of isoenzymes called nitric oxide synthases(NOS).The various pathophysiological conditions associated with alterations in the body’s NO homeostasis make NOS an attractive target for drug development.The three isoenzymes include eNOS(the endothelial isoform),nNOS(the neuronal isoform) and iNOS(the inducible isoform).The NO which is synthesized by different NOS is associated with different physiological functions.NO is synthesized in neurons of the central nervous system,where it acts as a neuromediator with many physiological functions,including the formation of memory,coordination between neuronal activity and blood flow,and modulation of pain. But overproduction of NO by nNOS has been implicated in a variety of diseases,such as strokes,seizures,schizophrenia,migraine headaches,and Alzheimer’s disease. When this occurs,selective inhibition of nNOS would decrease the concentration of NO in the brain and have a beneficial effect on neuron,but it has no or very little effect on the level of NO in other tissues and cells.

  • 【会议录名称】 第四届中国新医药博士论坛论文集
  • 【会议名称】第四届中国新医药博士论坛
  • 【会议时间】1999-11-01
  • 【会议地点】中国北京
  • 【分类号】R914
  • 【主办单位】国家科技部生命科学技术发展中心(China Innovation Center for Life Science)
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