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N-甲基-D-天冬氨酸拮抗剂:准备好用于脑缺血的临床试验了吗?

N-methyl-D-aspartate antagonists: ready for clinical trial in brain ischemia?

作者信息

Albers G W, Goldberg M P, Choi D W

机构信息

Department of Neurology, Stanford University Medical Center, CA 94305.

出版信息

Ann Neurol. 1989 Apr;25(4):398-403. doi: 10.1002/ana.410250412.

DOI:10.1002/ana.410250412
PMID:2565699
Abstract

Antagonists of the N-methyl-D-aspartate (NMDA) subclass of glutamate receptors may offer a new approach for the treatment of ischemic brain injury. This strategy is supported by a well-developed scientific foundation and encouraging results in a variety of in vivo and in vitro experimental models. Several specific antagonists, including MK-801, dextrorphan, dextromethorphan, and ketamine, have already been used at low doses in humans for other indications and are potential candidates for Phase I clinical trials.

摘要

N-甲基-D-天冬氨酸(NMDA)亚型谷氨酸受体拮抗剂可能为缺血性脑损伤的治疗提供一种新方法。这一策略有坚实的科学基础支持,并且在多种体内和体外实验模型中都取得了令人鼓舞的结果。几种特定的拮抗剂,包括MK-801、右啡烷、右美沙芬和氯胺酮,已经在人体中以低剂量用于其他适应症,并且是一期临床试验的潜在候选药物。

相似文献

1
N-methyl-D-aspartate antagonists: ready for clinical trial in brain ischemia?N-甲基-D-天冬氨酸拮抗剂:准备好用于脑缺血的临床试验了吗?
Ann Neurol. 1989 Apr;25(4):398-403. doi: 10.1002/ana.410250412.
2
Frequency-dependent involvement of NMDA receptors in the hippocampus: a novel synaptic mechanism.海马体中NMDA受体的频率依赖性参与:一种新型突触机制。
Nature. 1986;322(6076):265-8. doi: 10.1038/322265a0.
3
Dextrorphan and levorphanol selectively block N-methyl-D-aspartate receptor-mediated neurotoxicity on cortical neurons.右啡烷和左啡诺可选择性阻断N-甲基-D-天冬氨酸受体介导的对皮质神经元的神经毒性作用。
J Pharmacol Exp Ther. 1987 Aug;242(2):713-20.
4
Selective vulnerability of the brain: new insights into the pathophysiology of stroke.
Ann Intern Med. 1989 Jun 15;110(12):992-1000. doi: 10.7326/0003-4819-110-12-992.
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Do NMDA antagonists protect against cerebral ischemia: are clinical trials warranted?N-甲基-D-天冬氨酸(NMDA)拮抗剂能预防脑缺血吗:是否有必要进行临床试验?
Cerebrovasc Brain Metab Rev. 1990 Spring;2(1):1-26.
6
Potential therapeutic uses of N-methyl-D-aspartate antagonists in cerebral ischemia.N-甲基-D-天冬氨酸拮抗剂在脑缺血中的潜在治疗用途。
Clin Neuropharmacol. 1990 Jun;13(3):177-97. doi: 10.1097/00002826-199006000-00001.
7
Ifenprodil and SL 82.0715 as cerebral anti-ischemic agents. I. Evidence for efficacy in models of focal cerebral ischemia.艾芬地尔和SL 82.0715作为脑缺血治疗药物。I. 局灶性脑缺血模型中的疗效证据。
J Pharmacol Exp Ther. 1988 Dec;247(3):1211-21.
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NMDA and non-NMDA receptors are co-localized at individual excitatory synapses in cultured rat hippocampus.N-甲基-D-天冬氨酸(NMDA)受体和非NMDA受体共定位于培养的大鼠海马体中的单个兴奋性突触处。
Nature. 1989 Sep 21;341(6239):230-3. doi: 10.1038/341230a0.
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Neurotransmission. Are there two functional classes of glutamate receptors?神经传递。谷氨酸受体是否存在两种功能类别?
Nature. 1986;322(6076):210-1. doi: 10.1038/322210a0.
10
Inhibition of rat brain glutamate receptors by philanthotoxin.毒蜘蛛毒素对大鼠脑谷氨酸受体的抑制作用。
J Pharmacol Exp Ther. 1989 Oct;251(1):156-63.

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