Ramachandran J
Endocr Res. 1984;10(3-4):347-63. doi: 10.1080/07435808409036506.
The detection and characterization of the physiologically relevant receptors for corticotropin (ACTH) in rat adrenocortical cells is described. By the use of a radioligand with full biological potency and high specific radioactivity (1800 +/- 75 Ci/mmol), a single class of receptors with an apparent Kd of 1.41 +/- 0.21 nM was detected and the number of sites was estimated to be 3840 +/- 1045 per cell. The binding curve was superimposable on the concentration-response curve for cAMP but dissociated from that for steroidogenesis. These data are best explained by the receptor-reserve model in which occupancy of a small fraction of the receptors is sufficient for inducing maximal steroidogenesis.
本文描述了大鼠肾上腺皮质细胞中促肾上腺皮质激素(ACTH)生理相关受体的检测与特性。通过使用具有完全生物活性和高比放射性(1800±75 Ci/mmol)的放射性配体,检测到一类表观解离常数(Kd)为1.41±0.21 nM的受体,每个细胞的受体位点数量估计为3840±1045个。结合曲线与环磷酸腺苷(cAMP)的浓度-反应曲线重叠,但与类固醇生成的曲线分离。这些数据最好用受体储备模型来解释,即一小部分受体的占据就足以诱导最大程度的类固醇生成。