NMDA Receptor Complex Antagonists Have Ethanol‐like Discriminative Stimulus Effects

NMDA Receptor Complex Antagonists Have Ethanol‐like Discriminative Stimulus Effects
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NMDA 受体复合物拮抗剂具有类似乙醇的辨别刺激作用

DOI:
10.1111/j.1749-6632.1992.tb25986.x
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发表时间:
1992
影响因子:
5.2
通讯作者:
K. Grant
K. Grant
中科院分区:
综合性期刊3区
文献类型:
--
作者:
G. Colombo;K. Grant

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N-甲基-马斯巴达酸受体作为具有几个调节NMDA去极化作用的位点的大分子复合物存在。复合物的主要成分是NMDA识别位点、士的宁不敏感的甘氨酸位点和受体偶联阳离子通道。苯环己哌啶类化合物,包括二苯并环庚烯亚胺地佐环平(MK-801)结合在通道内,并以非竞争性方式阻断电导。药物如CPPene和CGS 19755结合到NMDA识别位点并以竞争性方式阻断电导。在piho研究2.3和piw研究中,乙醇(10-50 mM)已被报道拮抗与NMDA受体刺激相关的阳离子电导。“我们已经使用了一种药物辨别程序来证明NMDA神经传递的拮抗作用导致了与ethan 01在感知上相似的刺激效应。吹的研究检查是否NMDA拮抗剂,无论是在离子载体或在NMDA识别位点的行为有刺激作用类似于乙醇,如果这些相似性的影响,由乙醇的训练剂量。
The N-methyl-maspartate receptor exists as a macromolecular complex with several sites that modulate the depolarizing actions of NMDA. The primary components of the complex are the NMDA recognition site, a strychnine-insensitive glycine site, and the receptor-coupled cation channel. Phencyclidine-like compounds, including the dibenzocydoheptenimine dizocilpine (MK-801) bind within the channel and block conductance in an uncompetitive manner. Drugs such as CPPene and CGS 19755 bind to the NMDA recognition site and block conductance in a competitive manner.' Ethanol (10-50 mM) has been reported to antagonize cation conductance associated with the stimulation of NMDA receptors in both in piho studies2.3 and in piw studies.' We have used a drug discrimination procedure to demonstrate that antagonism of NMDA neurotransmission results in stimulus effects that are perceptively similar to ethan01.~ The blowing study examined whether NMDA antagonists that act either within the ionophore or at the NMDA recognition site have stimulus effects similar to ethanol, and if these similarities are influenced by the training dose of ethanol.
乙醇抑制体内 NMDA 诱发的电生理活动。
DOI: --
发表时间: 1991
期刊: The Journal of pharmacology and experimental therapeutics
影响因子: --
作者:
Simson,PE;Criswell,HE;Johnson,KB;Hicks,RE;Breese,GR
通讯作者: Breese,GR