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上海第二医科大学!上海200025
纸质出版日期:1999-11-01
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[1]胡雅儿,施菊,夏宗勤.M2受体cDNA转染CHOm2细胞的某些药理学和生物学特性[J].核技术,1999(11):642-646.
Pharmacological and biological properties of CHOm2 cells transfected with M2-receptor suptype[J]. Nuclear techniques, 1999, (11): 642-646.
转染m1、m2和m4cDNA的CHO细胞膜受体与3H-QNB结合,能给出典型的饱和曲线,Hill系数接近1。单位点竞争结合表明,对PZP抑制能力为CHOm1>CHOm4>CHOm2,对METH抑制强度为CHOm2>CHOm4>CHOm1。与药理学PZP对M1受体的亲和力最高和METH对M2的亲和力最高是一致的。CHOm2对Forskolin和Carbachol影响。AMP的结果,证明该M受体亚型信号传导系统的完整性,因此是研究M受体亚型与其信号传导的较好模型,也可用于筛选M受体亚型的药物。
~3H-QNB Saturation analysis revealed typical single-site saturation curve inCHO cell line transfected with cDNA of m1
m2or m4 receptors
with Hill numbersof nearly 1. Inhibition study of ~3H-QNB binding to muscarinic receptors inmembranes of these cells revealed that PZP had an affinity of m1>m4>m2 in theCHO cells
while METH had an affinity of m2>m4>m1. Using the m2 transfectedcells
carbachol could partially inhibit the foskolin induced cAMP elevation
indicating that there was a complete pathway for the trasduction of signals raised byagonist stimulation of M2 receptors. The time course of M2 receptor density in m2transfected CHO cell lines showed a peak value at about 48h and then dropped downgradually. The above results suggest that the cell lines could be used as models forthe study of structure and function of single subtypes of muscarinic receptors as wellas for screening of drugs.
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