Endogenous Inhibitor of Ligand Binding to the Muscarinic Acetylcholine Receptor
Endogenous Inhibitor of Ligand Binding to the Muscarinic Acetylcholine Receptor
复制标题
配体与毒蕈碱乙酰胆碱受体结合的内源性抑制剂
作者：
Ramon Diaz‐Arrastia;T. Ashizawa;S. Appel
翻译后摘要：L-[3 H]quinuclinidinyl benzilate结合到脑毒蕈碱乙酰胆碱受体的内源性抑制剂被确定。[3 H]二苯羟喹啉酸酯与大鼠脑突触体的结合使用过滤试验进行测量。该抑制剂是从几种小牛组织中制备的，在胸腺中的比活性最高。结合活性的丧失是缓慢的，需要用抑制剂预孵育突触体30-40分钟，并通过洗涤膜去除抑制剂来逆转。结合数据的Scatchard分析表明，抑制是非竞争性的亲和力和结合位点的数量减少的结果。这种效应需要低浓度的Zn 2+。毒蕈碱乙酰胆碱受体在突触膜和膜的大多数外周膜蛋白的自由仍然敏感的抑制。抑制分子的初步表征表明，它具有低分子量、中等热稳定性和酸性。抑制剂被非特异性亲核试剂灭活，但不被伯胺或硫醇基团特异性试剂灭活。
Abstract: An endogenous inhibitor of L‐[3H]quinuclinidinyl benzilate binding to the brain muscarinic acetylcholine receptor was identified. [3H]Quinuclinidinyl benzilate binding to rat brain synaptosomes was measured using a filtration assay. The inhibitor was prepared from several calf tissues and was found in highest specific activity in thymus. The loss of binding activity was slow, requiring a 30–40 min preincubation of the synaptosomes with the inhibitor, and reversed by removing the inhibitor by washing the membranes. Scatchard analysis of the binding data showed that the inhibition was noncompetitive resulting from both a decrease in affinity and a decrease in the number of binding sites. Zn2+ was required in low concentrations for this effect. Muscarinic acetylcholine receptor in synaptic membranes and in membranes free of most peripheral membrane proteins was still sensitive to inhibition. Preliminary characterization of the inhibitory molecule showed that it is of low molecular weight, moderately heat‐stable, and acidic. The inhibitor was inactivated by reagents that are nonspecific for nucleophiles, but not by reagents specific for primary amine or thiol groups.
纹状体毒蕈碱受体：多巴胺能激动剂的调节。
影响因子：
6.1
作者：
Ehlert,FJ;Roeske,WR;Yamamura,HI
通讯作者：
Yamamura,HI
培养心脏细胞中毒蕈碱胆碱能受体的激动剂和鸟嘌呤核苷酸调节。
DOI：
--
发表时间：
1980
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
Galper,JB;Smith,TW
通讯作者：
Smith,TW