In vitro effects of gallamine on dissociation kinetics of (3H)N-methylscopolamine and (3H)pirenzepine from rat brain muscarinic receptors.
In vitro effects of gallamine on dissociation kinetics of (3H)N-methylscopolamine and (3H)pirenzepine from rat brain muscarinic receptors.
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没食子胺对 (3H)N-甲基东莨菪碱和 (3H)哌仑西平从大鼠脑毒蕈碱受体解离动力学的体外影响。
DOI：
10.3109/10799898609073923
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发表时间：
1986
期刊：
影响因子：
--
通讯作者：
J. Christophe
中科院分区：
文献类型：
--
作者：
M. Gillard;M. Waelbroeck;J. Christophe
在大鼠海马、纹状体和皮质中，Gallamine可抑制（~ 3 H）N-甲基东莨菪碱（~ 3 H）NMS）和（~ 3 H）哌仑西平（~ 3 H）PZ的结合。没食子胺和（3 H）PZ之间的竞争曲线表明，没食子胺识别同类受体（希尔系数接近1），而竞争曲线，使用（3 H）NMS作为示踪剂，是兼容的两类没食子胺受体（希尔系数低于0.7）。后者的现象可以解释，至少部分地，通过抑制作用所施加的gallamine对（3 H）NMS的koff。在10 μ M的没食子胺浓度下已经观察到这种效果，并且在1 mM时达到100%（没食子胺浓度仅使（3 H）PZ的k off降低30%）。放射性配体的性质而不是M1 - M2受体的相对丰度可能是造成这种差异的原因。Gallamine抑制脑M1和M2受体（即对哌仑西平具有高和中等亲和力的受体）的（3 H）NMS解离速率的效力低于心脏M2受体（即对哌仑西平具有低亲和力的受体）。
Gallamine inhibited the binding of both (3H)N-Methylscopolamine ((3H)NMS) and (3H)Pirenzepine ((3H)PZ) in the hippocampus, striatum and cortex of rat brain. Competition curves between gallamine and (3H)PZ suggested that gallamine recognized an homogeneous class of receptors (Hill coefficient close to 1) whereas competition curves, using (3H)NMS as tracer, were compatible with two classes of gallamine receptors (Hill coefficient below 0.7). The latter phenomenon could be explained, at least partially, by the inhibitory effect exerted by gallamine on the k off of (3H)NMS. This effect was already observed at a 10 microM gallamine concentration and reached 100% at 1 mM (a gallamine concentration reducing the k off of (3H)PZ by 30% only). The nature of the radioligand rather than the relative abundance of M1 - M2 receptors was probably responsible for this discrepancy. Gallamine inhibited the (3H)NMS dissociation rate from brain M1 and M2 receptors (i.e. receptors with high and intermediate affinity for pirenzepine) with a lower potency than from cardiac M2 receptors (i.e. receptors with low affinity for pirenzepine).
经典毒蕈碱拮抗剂的四元形式区分毒蕈碱受体亚群：与没食子胺定义的亚群的相关性。
DOI：
10.1016/0006-291x(85)90319-5
发表时间：
1985
影响因子：
3.1
作者：
Ellis,J;Lenox,RH
通讯作者：
Lenox,RH