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新型靶向一氧化氮的药物。

Novel agents targeting nitric oxide.

机构信息

1st Cardiology Unit, Hippokration Hospital, Athens University Medical School, Athens, Greece.

出版信息

Curr Vasc Pharmacol. 2012 Jan;10(1):61-76. doi: 10.2174/157016112798829805.

DOI:10.2174/157016112798829805
PMID:22112348
Abstract

Nitric oxide (NO) is a soluble gas continuously synthesized from the amino acid L-arginine in endothelial cells by the constitutive calcium-calmodulin-dependent enzyme nitric oxide synthase (NOS). Endothelial dysfunction has been identified as a major mechanism involved in all the stages of atherogenesis. Evaluation of endothelial function seems to have a predictive role in humans, and therapeutic interventions improving nitric oxide bioavailability in the vasculature, may improve the long-term outcome in healthy individuals, high-risk subjects or patients with advanced atherosclerosis. Several therapeutic strategies (including statins, angiotensin converting enzyme inhibitors/angiotensin receptors blockers, insulin sensitizers, antioxidant compounds) are now available, targeting both the synthesis and oxidative inactivation of NO in human vasculature, reversing in that way endothelial dysfunction which is enhanced by the release of nitric oxide from the endothelium.

摘要

一氧化氮(NO)是一种可溶性气体,在血管内皮细胞中,由氨基酸 L-精氨酸在钙-钙调蛋白依赖性酶一氧化氮合酶(NOS)的作用下连续合成。内皮功能障碍已被确定为参与动脉粥样硬化所有阶段的主要机制之一。内皮功能的评估似乎在人类中具有预测作用,并且改善血管中一氧化氮生物利用度的治疗干预措施可能会改善健康个体、高危人群或晚期动脉粥样硬化患者的长期预后。目前有几种治疗策略(包括他汀类药物、血管紧张素转换酶抑制剂/血管紧张素受体阻滞剂、胰岛素增敏剂、抗氧化化合物),针对人类血管中一氧化氮的合成和氧化失活,从而逆转内皮功能障碍,内皮功能障碍是由一氧化氮从内皮细胞释放增强的。

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