奎尼丁对大鼠心脏毒蕈碱受体的抑制作用。
Inhibitory effects of quinidine on rat heart muscarinic receptors.
作者信息
Waelbroeck M, De Neef P, Robberecht P, Christophe J
出版信息
Life Sci. 1984 Sep 3;35(10):1069-76. doi: 10.1016/0024-3205(84)90071-7.
Quinidine inhibited binding of the labelled agonist [3H]oxotremorine M [( 3H]Oxo-M) and the labelled antagonist [3H]N-methylscopolamine [( 3H]NMS) to rat heart muscarinic receptors. Kinetic studies demonstrated that quinidine decreased the association rates (I50: 4 and 7.5 microM) and dissociation rates (I50: 100 and 68 microM) of [3H]Oxo-M and [3H]NMS, with different potencies. These cooperative effects explained the low Hill coefficients and apparent selectivity of quinidine competition curves.
奎尼丁抑制标记激动剂[3H]氧震颤素M（[3H]Oxo-M）和标记拮抗剂[3H]N-甲基东莨菪碱（[3H]NMS）与大鼠心脏毒蕈碱受体的结合。动力学研究表明，奎尼丁以不同的效力降低了[3H]Oxo-M和[3H]NMS的结合速率（半数抑制浓度：4和7.5微摩尔）和解离速率（半数抑制浓度：100和68微摩尔）。这些协同效应解释了奎尼丁竞争曲线的低希尔系数和明显的选择性。
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