Staurosporine, a protein kinase inhibitor, increases the intoxicating potencies of ethanol and other n-alkanols in Rana pipiens tadpoles.
Staurosporine, a protein kinase inhibitor, increases the intoxicating potencies of ethanol and other n-alkanols in Rana pipiens tadpoles.
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Staurosporine 是一种蛋白激酶抑制剂，可增加乙醇和其他正烷醇对 Rana pipiens 蝌蚪的中毒效力。
DOI：
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发表时间：
1995
期刊：
影响因子：
--
通讯作者：
L. Firestone
中科院分区：
文献类型：
--
作者：
S. Firestone;L. Firestone
中枢神经系统蛋白激酶是神经传递所必需的许多信号转导途径的细胞内效应物。虽然这些重要酶中的至少一种蛋白激酶C的体外活性被治疗浓度的乙醇和其他中枢抑制剂降低，但这种效应与体内中毒的关系尚不清楚。如果酒精中毒涉及中枢蛋白激酶抑制，那么这些酶的其他抑制剂应该会增强酒精的致醉效力。为了验证这一假设，我们比较了乙醇和其他两种正链烷醇的中值有效浓度的损失翻正反射在蛙pipiens蝌蚪预处理与staurosporine和未处理的控制。通过气相色谱法确认烷醇浓度，通过紫外吸收分光光度法确认星形孢菌素浓度。用650只动物获得的结果表明，用纳摩尔范围内的星形孢菌素浓度预处理显著降低了乙醇（对照的56%; p < 0.001）、丁醇（对照的38%; p < 0.001）和辛醇（对照的59%; p < 0.001）的中值有效浓度。这一发现支持了中枢蛋白激酶抑制可能参与乙醇和其他正烷醇的急性中毒作用。
Central nervous system protein kinases are the intracellular effectors for many of the signal transduction pathways essential to neurotransmission. Although the in vitro activity of at least one of these important enzymes, protein kinase C, is diminished by therapeutic concentrations of ethanol and other central depressants, the relationship of this effect to intoxication in vivo is not known. If intoxication by ethanol involves central protein kinase inhibition, then other inhibitors of these enzymes should enhance ethanol's intoxicating potency. To test this hypothesis, we compared the median effective concentrations of ethanol and two other n-alkanols for loss-of-righting reflex in Rana pipiens tadpoles pretreated with staurosporine and in untreated controls. Alkanol concentrations were confirmed by gas chromatography and staurosporine concentrations by ultraviolet absorbance spectrophotometry. Results obtained with 650 animals demonstrate that pretreatment with staurosporine concentrations in the nanomolar range significantly decrease the median effective concentration for ethanol (56% of control; p < 0.001), butanol (38% of control; p < 0.001), and octanol (59% of control; p < 0.001). This finding supports that central protein kinase inhibition may be involved in the acute intoxicating effects of ethanol and other n-alkanols.
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影响因子：
21.1
作者：
R. Deitrich;T. Dunwiddie;R. Harris;V. Erwin
通讯作者：
R. Deitrich;T. Dunwiddie;R. Harris;V. Erwin
急性和慢性乙醇治疗对大鼠脑磷脂周转的影响。
影响因子：
5.8
作者：
Lee,NM;Friedman,HJ;Loh,HH
通讯作者：
Loh,HH
研究蛋白激酶 C 在乙醇急性镇静作用中的作用。
DOI：
10.1111/j.1530-0277.1989.tb00413.x
发表时间：
1989
期刊：
Alcoholism, clinical and experimental research
影响因子：
--
作者：
Deitrich,RA;Bludeau,PA;Baker,RC
通讯作者：
Baker,RC
急性乙醇给药引起大鼠脑多磷酸肌醇代谢的改变。
DOI：
--
发表时间：
1988
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
Chandrasekhar,R;Huang,HM;Sun,GY
通讯作者：
Sun,GY