The behavioral effects of phencyclidines may be due to their blockade of potassium channels.
The behavioral effects of phencyclidines may be due to their blockade of potassium channels.
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苯环己哌啶的行为影响可能是由于其阻断钾通道。
DOI：
10.1073/pnas.78.12.7792
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发表时间：
1981
影响因子：
11.1
通讯作者：
Blaustein,MP
中科院分区：
文献类型：
--
作者：
Albuquerque,EX;Aguayo,LG;Warnick,JE;Weinstein,H;Glick,SD;Maayani,S;Ickowicz,RK;Blaustein,MP
苯环利定[1-（1-苯基环己基）哌啶]的作用本研究对PCP及其行为活性类似物（间氨基-PCP）和两种行为无活性类似物[间硝基-PCP和1-哌啶环己二腈（PCC）]进行了研究。在空间交替表现测试中，PCP和间氨基-PCP比PCC和间硝基-PCP更有效地改变大鼠的行为。我们研究了药物对蛙骨骼肌神经肌肉接点电兴奋膜离子通道和烟碱乙酰胆碱受体离子通道的影响。四种化合物均能阻断间接诱发的肌痉挛，抑制直接诱发的肌动作电位的幅度和上升速率。它们还引起终板电流峰值振幅的电压和浓度依赖性下降，但不与烟碱AcCho受体反应。这些观察结果表明，这四种化合物对与烟碱AcCho受体相关的离子通道具有相当的阻断作用。相比之下，行为活性剂可以通过对K+电导的影响来区分行为非活性剂。PCP和间氨基-PCP阻断了蛙缝匠肌的延迟矫正，延长了2倍以上的肌肉动作电位，并显著增强了直接诱发的肌肉抽搐。这种具有行为活性的化合物还阻断了去极化诱导的86Rb+从大鼠脑突触体流出（可能是对K+电导的一种测量），并增加了青蛙神经肌肉连接处的量子含量。在这些作用中，间硝基pcp的效果要差得多，而PCC相对无效。由于PCP和间氨基-PCP是比PCC和间硝基-PCP更有效的行为调节剂，我们认为PCP和间氨基-PCP的行为影响可能是由于阻断K+电导和增强中枢神经元的递质释放。
The action of phencyclidine [1-(1-phenylcyclohexyl)piperidine; PCP] and its behaviorally active analog (m-amino-PCP) and of two behaviorally inactive analogs [m-nitro-PCP and 1-piperidinocyclohexanecarbonitrile (PCC)] were examined in this study. In a test of spatial alternation performance in rats, PCP and m-amino-PCP were much more potent behavior modifiers than were PCC and m-nitro-PCP. We studied the effects of the drugs on the ionic channels of the electrically excitable membrane and of the nicotinic acetylcholine (AcCho) receptors at the neuromuscular junction of frog skeletal muscle. All four compounds blocked the indirectly elicited muscle twitch and depressed the amplitude and rate of rise of directly elicited muscle action potentials. They also caused a voltage- and concentration-dependent decrease in the peak amplitude of the endplate current but did not react with the nicotinic AcCho receptor. These observations indicate that the four compounds have comparable blocking effects on the ionic channels associated with the nicotinic AcCho receptor. In contrast, the behaviorally active agents could be distinguished from behaviorally inactive ones by their effects on K+ conductance. PCP and m-amino-PCP blocked delayed rectification in frog sartorius muscles, prolonged the muscle action potential more than 2-fold, and markedly potentiated the directly elicited muscle twitch. The behaviorally active compound also blocked depolarization-induced 86Rb+ efflux from rat brain synaptosomes (presumably a measure of K+ conductance) and increased quantal content at the frog neuromuscular junction. In these actions, m-nitro-PCP was much less effective, and PCC was relatively ineffective. Because PCP and m-amino-PCP are much more potent behavior modifiers than PCC and m-nitro-PCP, we suggest that the behavioral effects of PCP and m-amino-PCP, may be due to a block of K+ conductance and enhancement of transmitter release at central neurons.
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用四氯化碳处理引起大鼠肝脏提取物中亚精胺乙酰化的增加。
DOI：
--
发表时间：
1980
期刊：
Biochemical and Biophysical Research Communications - BBRC
影响因子：
--
作者：
I. Matsui;A. Pegg
通讯作者：
A. Pegg
BHK-21/C13 细胞中甲基葡萄糖醛-双（脒腙）和多胺乙酰转移酶活性的积累：亚精胺的作用
DOI：
--
发表时间：
1987
期刊：
影响因子：
--
作者：
M. Nuttall;H. Wallace
通讯作者：
H. Wallace
α-二氟甲基鸟氨酸（鸟氨酸脱羧酶抑制剂）和 N1,N8-双（乙基）亚精胺（该酶的明显调节剂）对 L1210 细胞生长抑制的比较和表征。
影响因子：
11.2
作者：
Porter,CW;Ganis,B;Vinson,T;Marton,LJ;Kramer,DL;Bergeron,RJ
通讯作者：
Bergeron,RJ
酶调节作为干扰多胺生物合成的一种方法——酶抑制的替代方法。
DOI：
10.1016/0065-2571(88)90009-x
发表时间：
1988
期刊：
Advances in enzyme regulation
影响因子：
--
作者：
Porter,CW;Bergeron,RJ
通讯作者：
Bergeron,RJ
多胺和相关化合物对 L6 细胞中亚精胺/精胺 N1-乙酰转移酶的调节。
DOI：
10.1042/bj2380581
发表时间：
1986
期刊：
The Biochemical journal
影响因子：
--
作者：
Erwin,BG;Pegg,AE
通讯作者：
Pegg,AE