兴奋性氨基酸拮抗剂的治疗潜力：通道阻滞剂和2,3-苯二氮䓬类药物。

Therapeutic potential of excitatory amino acid antagonists: channel blockers and 2,3-benzodiazepines.

作者信息

Rogawski M A

机构信息

Neuronal Excitability Section, National Institute of Neurological Disorders and Stroke, Bethesda, MD 20892.

出版信息

Trends Pharmacol Sci. 1993 Sep;14(9):325-31. doi: 10.1016/0165-6147(93)90005-5.

DOI:10.1016/0165-6147(93)90005-5

PMID:7504360

Abstract

NMDA and non-NMDA (AMPA/kainate) antagonists have potential in the treatment of a diverse group of neurological disorders associated with excessive activation of excitatory amino acid receptors. Here Michael Rogawski reviews recent progress in the development of therapeutically useful NMDA receptor channel blockers and a new class of selective AMPA/kainate receptor antagonists, the 2,3-benzodiazepines. Research on these novel noncompetitive excitatory amino acid antagonists has opened promising new avenues for the development of drugs to treat epilepsy, ischaemia, neurodegeneration and Parkinson's disease.

摘要

N-甲基-D-天冬氨酸（NMDA）和非NMDA（α-氨基-3-羟基-5-甲基-4-异恶唑丙酸/海人藻酸，AMPA/kainate）拮抗剂在治疗与兴奋性氨基酸受体过度激活相关的多种神经疾病方面具有潜力。在此，迈克尔·罗加夫斯基综述了具有治疗作用的NMDA受体通道阻滞剂以及一类新型选择性AMPA/kainate受体拮抗剂——2,3-苯二氮䓬类药物的最新研发进展。对这些新型非竞争性兴奋性氨基酸拮抗剂的研究为开发治疗癫痫、缺血、神经退行性变和帕金森病的药物开辟了前景广阔的新途径。