Activation and inhibition of the sarcoplasmic reticulum Ca2+ channel by the polycationic dyes Hoechst 33342 and Hoechst 33258.
Activation and inhibition of the sarcoplasmic reticulum Ca2+ channel by the polycationic dyes Hoechst 33342 and Hoechst 33258.
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聚阳离子染料 Hoechst 33342 和 Hoechst 33258 对肌浆网 Ca2 通道的激活和抑制。
DOI：
10.1007/bf00231436
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发表时间：
1993
期刊：
影响因子：
--
通讯作者：
Gable,K
中科院分区：
文献类型：
--
作者：
Beeler,TJ;Gable,K
多阳离子染料Hoechst 33342 （Bisbenzimide,2 ' -（4-乙氧基苯基）-5-（4-甲基-1-哌嗪基）2,5 ' -bi-1H苯并咪唑）和Hoechst 33258 （Bisbenzimide,2 ' -（4-羟基苯基）5-（4-甲基-1-哌嗪基）-2,5 ' -bi-1H苯并咪唑）改变肌浆网Ca2+通道的活性。尽管它们相互竞争，Hoechst 33342降低，而Hoechst 33258增加，通道介导的Ca2+从连接肌浆网囊泡流出的速率。与其他阳离子肌浆网Ca2+通道拮抗剂不同，Hoechst 33342阻断ryanoine激活的Ca2+通道。Hoechst 33342和Hoechst 33258均可抑制纳入平面脂质双分子层的通道。由于两种染料之间的唯一结构差异是激动剂Hoechst 33258具有羟基，而拮抗剂Hoechst 33342具有乙基，因此更疏水，体积更大的乙基可能会阻止Ca2+通过通道的运动，而羟基只会降低Ca2+的运动速率。此处包含的观点或断言是作者的私人观点，不应被解释为官方观点或反映国防部或卫生科学军警服务大学的观点。
The polycationic dyes, Hoechst 33342 (Bisbenzimide,2′-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl) 2,5′-bi 1H benzimidazole) and Hoechst 33258 (Bisbenzimide,2′-(4-hydroxyphenyl) 5-(4-methyl-1-piperazinyl)-2,5′-bi-1H-benzimidazole) alter the activity of the sarcoplasmic reticulum Ca2+channel. Although they act competitively, Hoechst 33342 decreases, while Hoechst 33258 increases, the rate of channel-mediated Ca2+efflux from junctional sarcoplasmic reticulum vesicles. Unlike other cationic sarcoplasmic reticulum Ca2+channel antagonists, Hoechst 33342 blocks the ryanodine-activated Ca2+channel. Both Hoechst 33342 and Hoechst 33258 inhibit the channel incorporated into the planar lipid bilayer. Since the only structural difference between the two dyes is that the agonist Hoechst 33258 has a hydroxy group where the antagonist Hoechst 33342 has an ethoxy group, it is possible that the more hydrophobic, bulky ethoxy group blocks Ca2+movement through the channel, whereas the hydroxy group only reduces the rate of Ca2+movement.The opinions or assertions contained herein are private ones of the author ad are not to beconstrued as official or reflecting the views of the Department of Defense or the Uniformed Services University of the Health Sciences.