Sjödin L
J Biol Stand. 1985 Jul;13(3):199-210. doi: 10.1016/s0092-1157(85)80003-2.
Receptors for glucagon on rat liver membranes were characterized. They bound [125I] glucagon rapidly in a specific and saturable way. Addition of unlabelled glucagon displaced [125I] glucagon from the binding sites in a concentration dependent way. Concentrations from 10(-9) to 10(-8) M of glucagon caused a linear reduction of binding of labelled glucagon. This concentration interval was used for a three-point assay which fulfilled statistical requirements for validity. Individual assays normally resulted in potency estimates of high precision and statistical weight. Mean values for glucagon activity of preparations tested by receptor assay were within the fiducial limits (P = 0.95) for corresponding activity determined by the rabbit blood glucose method. The receptor assay is less time consuming and requires only part of one rat liver while the in vivo assay uses 16 rabbits. Thus, the receptor assay is less resource demanding and should serve well as a screening instrument for control of potency of glucagon preparations.
对大鼠肝细胞膜上的胰高血糖素受体进行了特性研究。它们以特异性和可饱和的方式快速结合[125I]胰高血糖素。加入未标记的胰高血糖素会以浓度依赖性方式将[125I]胰高血糖素从结合位点上置换下来。10(-9)至10(-8)M浓度的胰高血糖素会使标记胰高血糖素的结合呈线性减少。该浓度区间用于三点测定,该测定满足有效性的统计要求。单个测定通常会得出高精度和统计权重的效价估计值。通过受体测定法测试的制剂的胰高血糖素活性平均值在通过兔血糖法测定的相应活性的置信限(P = 0.95)范围内。受体测定法耗时较少,只需要大鼠肝脏的一部分,而体内测定法需要16只兔子。因此,受体测定法对资源的需求较少,应能很好地作为控制胰高血糖素制剂效价的筛选工具。