左旋咪唑对大鼠脑组织咪唑啉2受体-配体结合试验的影响  

Effects of levamisole on imidazoline I_2 receptors binding assay in brain of rats

作　　者：殷为勇[1] 郑荣远[1] 陈国钱[1] 韩钊[1] 潘建春[2] 李云峰[3] 陈洪霞[3] 

机构地区：[1]温州医学院附属第一医院神经科,温州325000 [2]温州医学院药学院药理学教研室,温州325000 [3]北京军事医学科学院毒物药物研究所,北京100850

出　　处：《中国临床药学杂志》2007年第6期338-340,共3页Chinese Journal of Clinical Pharmacy

基　　金：国家自然科学基金(30470611);浙江省自然科学基金(Y204133)资助

摘　　要：目的研究左旋咪唑(LMS)对大鼠脑组织咪唑啉2受体(I_2R)的影响。方法采用受体-配体竞争结合试验,观察LMS与受体的结合能力;采用受体-配体饱和试验,测定LMS处理大鼠和对照组大鼠脑内I_2R最大受体结合容量(B_(max))和平衡解离常数(K_d)变化。结果LMS抑制了放射性配基[~3H]idazoxan与大鼠脑组织内I_2R的结合,其半数抑制浓度(IC_(50))为4.04×10^(-7)mol·L^(-1)。LMS长期处理大鼠,脑内I_2R亲和力上调63%。结论LMS能与I_2R结合,长期应用LMS能通过刺激I_2R而改变了受体亲和力。AIM To study the effects of levamisole on imidazoline I2 receptors in brain of rats.METHODS The potency of levamisole binding to imidazoline I2 receptors in brain of rats was evaluated by using competitive binding assays,the maximal binding capacity （Bmax）and dissociation constant （Kd）of imidazoline I2 receptors were measured in long-term treatment of levamisole and in control group by using saturated binding assay.RESULTS Levamisole inhibited the binding of [^3H]idazoxan to imidazoline I2 receptors,with a IC50（concentration of drug displacing 50%specific binding）of 4.04×10^-7mol·L^-1.The affinity of imidazoline I2 receptors,labeled by [^3H]idazoxan,was significantly higher in the levamisole group than in control （Kd increased by 63%）.CONCLUSION Levamisole can bind to imidazoline I2 receptors,and long-term administration of levamisole significantly increased the binding affinity of imidazoline I2 receptors.

关 键 词：左旋咪唑 咪唑啉2受体 受体-配体结合 

分 类 号：R96[医药卫生—药理学]