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ATP敏感性钾通道:神经精神药理学中的潜在药物靶点。

ATP sensitive potassium channels: potential drug targets in neuropsychopharmacology.

作者信息

Gehlert D R, Robertson D W

机构信息

Lilly Research Laboratories, Indianapolis, IN.

出版信息

Prog Neuropsychopharmacol Biol Psychiatry. 1994 Nov;18(7):1093-102. doi: 10.1016/0278-5846(94)90113-9.

Abstract
  1. K channels are a diverse and ubiquitous class of proteins that regulate a number of biological functions. 2. Ligands for the study of a variety of K channels are available. These include "openers" and antagonists for the ATP sensitive K channel and peptide toxins such as apamin and charybdotoxin that block other subtypes. 3. Antagonists of the ATP sensitive K channel are useful in the treatment of type II diabetes while "openers" of this channel are being tested in asthma and cardiovascular disease. 4. Intracerebroventricular administration of K channel "openers" block experimentally induced seizures in rodents through a hyperpolarization of neurons. K channel openers may also be useful in the treatment of neurodegenerative diseases, pain and cerebral ischemia. 5. A key to the development of psychopharmacological agents to modify brain K channel function is CNS selectivity. The promise of the ATP sensitive K channel openers suggests a bright future for this mechanism.
摘要
  1. K通道是一类多样且普遍存在的蛋白质,可调节多种生物学功能。2. 有多种用于研究各类K通道的配体。这些包括ATP敏感性K通道的“开放剂”和拮抗剂,以及诸如蜂毒明肽和大蝎毒素等可阻断其他亚型的肽类毒素。3. ATP敏感性K通道的拮抗剂可用于治疗II型糖尿病,而该通道的“开放剂”正在哮喘和心血管疾病中进行测试。4. 经脑室注射K通道“开放剂”可通过使神经元超极化来阻断啮齿动物实验性诱发的癫痫发作。K通道开放剂也可能用于治疗神经退行性疾病、疼痛和脑缺血。5. 开发用于改变脑K通道功能的精神药理学药物的关键在于中枢神经系统选择性。ATP敏感性K通道开放剂的前景为这一机制展现了光明的未来。

相似文献

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New windows on the mechanism of action of K(ATP) channel openers.钾离子通道开放剂作用机制的新视角。
Trends Pharmacol Sci. 2000 Nov;21(11):439-45. doi: 10.1016/s0165-6147(00)01563-7.

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