摘要
Ampakines是研究最成熟的一类AMPA受体正向调节剂,目前已开展的适应证研究涵盖呼吸抑制和精神神经疾病等多个领域。以CX516和CX546为工具化合物进行研究发现,ampakines可分为“高效能ampakines”和“低效能ampakines”,该两类化合物在化学结构、对受体动力学影响、促受体配体结合、促组织突触传递、神经营养因子调控、副作用方面表现出不同性质。从现状来看,低效能ampakines由于其安全性高、耐受性好等优点,其临床应用前景显著优于高效能ampakines。本文对ampakines两类化合物的上述性质作一综述。
Ampakines are a class of pharmacological agents acting as positive modulators of AMPA receptors.Currently,clinical indications studied for ampakines involve many diseases including the respiratory depression and psy?choneurosis,etc.The studies using CX516 and CX546 as tool compounds have shown that ampakines could be classified into“high impact ampakines”and“low impact ampakines”.The two subclasses of ampakines differ in the chemical struc?tures,influences on receptor dynamics,receptor-ligand bindings,synaptic transmissions,neurotrophin regulations and side effects.According to the available literature,the low impact ampakines have better clinical application prospects than high impact ampakines because of their high safety and good tolerance.The above different characteristics of the two subclasses of ampakines are reviewed in this paper.
作者
肖典
刘连奇
周辛波
XIAO Dian;LIU Lian-qi;ZHOU Xin-bo(National Engineering Research Center for the Strategic Drug,Institute of Pharmacology&Toxicology,Academy of Military Medical Sciences,Academy of Military Sciences,Beijing 100850,China)
出处
《国际药学研究杂志》
CAS
北大核心
2019年第5期325-331,共7页
Journal of International Pharmaceutical Research
基金
国家自然基金青年科学基金项目(81803427)
