Staurosporine inhibits the extent of acetylcholine receptor recovery from carbachol-induced desensitization in snake twitch fibres.
Staurosporine inhibits the extent of acetylcholine receptor recovery from carbachol-induced desensitization in snake twitch fibres.
复制标题
星形孢菌素抑制蛇抽搐纤维中卡巴胆碱诱导的脱敏作用中乙酰胆碱受体恢复的程度。
DOI：
10.1111/j.1476-5381.1991.tb12521.x
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发表时间：
1991
影响因子：
7.3
通讯作者：
Parsons,RL
中科院分区：
文献类型：
--
作者：
Hardwick,JC;Coniglio,LM;Parsons,RL
1.研究了蛋白激酶抑制剂staurosporine对卡巴胆碱诱导脱敏后恢复程度和时间过程的影响，研究对象是保持在等渗丙酸钾溶液中并电压钳位至+30 mV的蛇抽搐肌纤维。2.用星形孢菌素（0.5 μ M）预处理降低了自发性微终板电流（m.e.p.c.）持续应用540 μ M卡巴胆碱脱敏后的振幅。在不改变m.e.p.c.时程的情况下，恢复受到约50%的抑制。复苏3.星形孢菌素也产生了浓度依赖性（10 nM至0.5 μ M）的第二卡巴胆碱诱导的电流的幅度下降，洗涤期后，与初始卡巴胆碱应用产生的电流的幅度相比。预处理与0.5 μ M K252 a，另一种广谱蛋白激酶抑制剂，也降低了恢复的程度，第二卡巴胆碱应用脱敏后的反应。4.星形孢菌素预处理（0.5 μ M）对受体通道门控动力学或初始终板对激动剂的敏感性均无影响。这是通过比较卡巴胆碱（540 μ M）诱导的电流的幅度和控制和星形孢菌素处理的纤维中的m.e.p.cs的幅度和衰减率来确定的。5.星形孢菌素对540 μ M卡巴胆碱初始应用期间产生的脱敏发作的时间过程或暴露于540 μ M卡巴胆碱2-3分钟结束时产生的脱敏深度没有影响。（250字处删节）
1. The effect of the protein kinase inhibitor, staurosporine, on the extent and time course of recovery following carbachol-induced desensitization was studied in snake twitch-muscle fibres maintained in an isotonic potassium propionate solution and voltage-clamped to +30 mV. 2. Pretreatment with staurosporine (0.5 microM) decreased the extent of recovery of spontaneous miniature endplate current (m.e.p.c.) amplitudes following desensitization by a sustained application of 540 microM carbachol. Recovery was inhibited by approximately 50% without altering the time course of m.e.p.c. recovery. 3. Staurosporine also produced a concentration-dependent (10 nM to 0.5 microM) decrease in the amplitude of a second carbachol-induced current, following a wash period, as compared to the amplitude of the current produced by the initial carbachol application. Pretreatment with 0.5 microM K252a, another wide spectrum protein kinase inhibitor, also decreased the extent of recovery of the response to a second carbachol application following desensitization. 4. Staurosporine pretreatment (0.5 microM) had no effect on either the kinetics of receptor-channel gating or the initial endplate sensitivity to agonist. This was determined by comparing the amplitude of the carbachol (540 microM)-induced currents and the amplitude and decay rate of m.e.p.cs in control and staurosporine-treated fibres. 5. Staurosporine had no effect on the time course of desensitization onset produced during the initial application of 540 microM carbachol or the depth of desensitization produced by the end of a 2-3 min exposure to 540 microM carbachol.(ABSTRACT TRUNCATED AT 250 WORDS)