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采用放射配基受体结合分析法，以氚标记二苯羟乙酸奎宁酯为放射配基，通过受体饱和实验、结合与解离动力学实验和竞争抑制实验，分别测定了大白鼠前脑组织中的Ｍ－胆碱能受体的最大结合容量（Ｂｍａｘ）为１６．６８ｐｍｏｌ／ｇ膜蛋白，平衡解离常数（Ｋｄ）为０．３７ｎｍｏｌ／Ｌ；在３７℃环境下，其半结合和半解离时间为２．５ｍｉｎ和３２．５ｍｉｎ，动力学结合速率常数（Ｋ＿１）为０．１３ｍｉｎ￣（－１）（ｎｍｏｌ／Ｌ）￣（－１），解高速率常数（Ｋ＿２）为０．０４２ｍｉｎ￣（－１）。此外，观察了常用三环抗抑郁剂的半最大抑制浓度（Ｉｃ＿５０）和竞争抑制常数（Ｋｉ），探讨抑制药物与Ｍ－胆碱受体结合特性。
Radioligand receptor binding assay was used to determine the binding capacity of tris-labeled quinine glycoside to radioligand. The receptor saturation, binding and dissociation kinetics and competition inhibition were measured respectively Tissue M-cholinergic receptor maximum binding capacity (Bmax) of 16.68pmol / g membrane protein, equilibrium dissociation constant (Kd) of 0.37nmol / L; at 37 ℃ environment, its half-binding and The half-dissociation time was 2.5 min and 32.5 min, and the kinetic binding rate constant (K_1) was 0.13 min -1 (nmol / L) -1. The solution rate constant (K 2) was 0 .042min ~ (-1). In addition, we observed the half maximal inhibitory concentration (Ic_50) and competitive inhibition constant (Ki) of commonly used tricyclic antidepressants, and explored the inhibition of drug binding to M-choline receptors.