Affinity directed reactions of 3-trimethylaminomethyl catechol with the acetylcholine receptor from Torpedo californica.
Affinity directed reactions of 3-trimethylaminomethyl catechol with the acetylcholine receptor from Torpedo californica.
复制标题
3-三甲氨基甲基儿茶酚与加州鱼雷乙酰胆碱受体的亲和定向反应。
DOI：
10.1016/s0006-291x(82)80134-4
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发表时间：
1982
影响因子：
3.1
通讯作者：
R. A. Hudson
中科院分区：
文献类型：
--
作者：
B. Nickoloff;M. Grimes;R. Kelly;R. A. Hudson
合成了3-三甲胺甲基儿茶酚（TMC），结果表明，TMC能最大限度地灭活加利福尼亚电鳗与乙酰胆碱受体（AcChR）结合的α-虫毒（btx） 50%。受体与未取代的儿茶酚孵育不产生毒素结合受体失活。此外，受体与1 mM六甲铵和30 mM TMC共孵育有效阻断了单独与30 mM TMC孵育产生的Btx结合的亲和定向失活。这种保护程度与六甲铵（4.8 × 10−6M）和TMC （2.8 × 10−5M）与AcChR的相对结合常数一致。亲和定向失活可能是由于TMC自发氧化过程中形成的一种或多种醌中间体与AcChR的Btx结合位点发生共价反应。
3-Trimethylaminomethyl catechol (TMC) was synthesized and shown maximally to inactivate 50% of the α-bungarotoxin (B tx) binding to the acetylcholine receptor (AcChR) fromTorpedo californicaelectroplax. Incubation of the receptor with unsubstituted catechol produced no toxin binding inactivation of the receptor. Further, co-incubation of the receptor with 1 mM hexamethonium and 30 mM TMC effectively blocked the affinity-directed inactivation of Btx binding produced by incubation with 30 mM TMC alone. This degree of protection was consistent with the relative binding constants for hexamethonium (4.8 × 10−6M) and TMC (2.8 × 10−5M) with the AcChR. The affinity directed inactivation is suggested to be due to the covalent reaction of one or more of the quinone intermediates formed during the spontaneous oxidation of TMC with the Btx binding sites of the AcChR.