Poulin P, Lederis K, Pittman Q J
Department of Medical Physiology, Faculty of Medicine, University of Calgary, Alberta, Canada.
J Neurochem. 1988 Mar;50(3):889-98. doi: 10.1111/j.1471-4159.1988.tb02996.x.
[Arg8]-Vasopressin (AVP) has been shown to exert characteristic central physiological actions in the ventral septal area of the rat brain. This study reports the characterization of receptors for AVP in synaptic plasma membranes prepared from the ventral septal area, the lateral septum, and the hippocampus. Binding of [3H]AVP was temperature and time dependent, linearly related to protein concentration, saturable, and specific. Scatchard plot analysis suggested the presence of a population of binding sites in the three brain areas with dissociation constants and maximal binding capacities, respectively, of 1.06 +/- 0.39 nM and 24.0 +/- 7.01 fmol/mg of protein (mean +/- SEM; n = 3 for the ventral septal area, 0.92 +/- 0.13 nM and 47.0 +/- 4.96 fmol/mg of protein (n = 3) for the lateral septum, and 0.91 +/- 0.14 nM and 25 +/- 5.02 fmol/mg of protein (n = 3) for the hippocampus. In all three brain regions, the rank order of potencies of several vasopressin analogs, unrelated peptides, and other compounds for competitive displacement of ligand indicated a receptor with properties resembling those of the V1-like receptor for AVP. These data document the presence of a high-affinity, V1-like vasopressin receptor in the rat ventral septal area for which the pharmacological properties are similar to those previously reported in physiological studies.
[精氨酸8] - 加压素（AVP）已被证明在大鼠脑腹侧隔区发挥特征性的中枢生理作用。本研究报告了从腹侧隔区、外侧隔区和海马体制备的突触质膜中AVP受体的特性。[3H]AVP的结合具有温度和时间依赖性，与蛋白质浓度呈线性相关，具有饱和性和特异性。Scatchard图分析表明，在这三个脑区存在一群结合位点，其解离常数和最大结合容量分别为：腹侧隔区1.06±0.39 nM和24.0±7.01 fmol/mg蛋白质（平均值±标准误；n = 3），外侧隔区0.92±0.13 nM和47.0±4.96 fmol/mg蛋白质（n = 3），海马体0.91±0.14 nM和25±5.02 fmol/mg蛋白质（n = 3）。在所有三个脑区中，几种加压素类似物、无关肽和其他化合物竞争性取代配体的效力顺序表明存在一种受体，其特性类似于AVP的V1样受体。这些数据证明在大鼠腹侧隔区存在一种高亲和力的V1样加压素受体，其药理学特性与先前生理学研究中报道的相似。
