PHOTOCHROMIC ACTIVATORS OF ACETYLCHOLINE RECEPTOR
PHOTOCHROMIC ACTIVATORS OF ACETYLCHOLINE RECEPTOR
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DOI：
10.1073/pnas.68.8.1820
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发表时间：
1971-01-01
影响因子：
11.1
通讯作者：
ERLANGER, BF
中科院分区：
文献类型：
--
作者：
BARTELS, E;WASSERMANN, NH;ERLANGER, BF
目前报道的最有效的光致变色激活剂二溴联苯二溴(described.Trans-3，3′-bis[α-(trimethylammonium)methyl]azobenzene-Q，BIS-Q)是电泳膜的两种光致变色激活剂，其活性浓度小于10-7M。它的异构体是通过330 nm的光照射而获得的，实际上是没有活性的。在Bis-Q存在的情况下，膜的电位发生光调节，这可能是因为在单细胞电浆系统中，活性转移体转化为非活性转移体。第二种活化剂3-(α-bromomethyl)-3′-[α-(trimethylammonium)methyl]azobenzene溴化物在二硫苏糖醇还原后可以共价结合到电浆膜上。膜的活化是由共价连接试剂诱导的。它是通过330 nm的光照射获得的，它的活性很低，就像cis-Bis-Q。Bis-Q的两种异构体都是乙酰胆碱酯酶的抑制剂，在10-5M的浓度下有50%的抑制作用。讨论了利用反式-Bis-Q和反式-QBR鉴定和分离受体蛋白的可能性。
Two photochromic activators of the electrogenic membrane of the electroplax ofElectrophorus electricusare described.Trans-3,3′-bis[α-(trimethylammonium)methyl]azobenzene dibromide (Bis-Q), one of the most potent ever reported, is active at concentrations of less than 10-7M. Itscisisomer, which is obtained from thetransby exposure to light of 330 nm, is practically devoid of activity. Photoregulation of the potential of the membrane takes place in the presence of Bis-Q, presumably because of the conversion of the activetransisomer to the inactivecisisomer in the single-cell electroplax system. The second activator, 3-(α-bromomethyl)-3′-[α-(trimethylammonium)methyl]azobenzene bromide (QBr) can be covalently attached to the electroplax membrane after reduction of the membrane with dithiothreitol. Activation of the membrane is induced by the covalently linked reagent. Itscisisomer, obtained from thetransby exposure to light of 330 nm, is, likecis-Bis-Q, of very low activity. Both isomers of Bis-Q are equally active as inhibitors of acetylcholinesterase, 50% inhibition occurring at a concentration of 10-5M. The possibility of usingtrans-Bis-Q andtrans-QBr to characterize and isolate the receptor protein is discussed.