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目的:观察左旋咪唑(LMS)在体外实验中能否与正常大鼠脑组织咪唑啉2受体(I_2R)结合;LMS在体内长期处理能否引起大鼠脑内I_2R的变化。方法:通过正常大鼠脑组织I_2R与放射性配基的竞争结合实验,测定其平衡解离常数(K_i)及50%的放射性配基结合被取代所需的竞争剂浓度(IC_(50)),观察LMS与I_2R在体外的结合能力。通过LMS长期体内处理大鼠脑组织I_2R饱和结合实验,测定LMS长期处理大鼠和对照组大鼠脑组织I_2R密度和亲和力的变化。结果:体外实验发现,LMS能与[~3H]-2BFI竞争结合大鼠脑组织的I_2R,且具有浓度依赖性。IC_(50)值为1.292×10~(-5)mol·L~(-1),K_i值为9.796×10~(-6)mol·L~(-1)。大鼠体内长期LMS处理,其脑组织I_2R密度明显上调(P<0.05),而亲和力两组相比差异无统计学意义。结论:左旋咪唑在体外能与脑组织I_2R直接结合,可能是I_2R的配基。左旋咪唑长期作用于体内能引起脑组织I_2R密度的上调。
OBJECTIVE: To observe whether LMS can bind to I 2 R (I 2 R) in normal rat brain in vitro and whether long-term administration of LMS can induce changes of I 2 R in rat brain in vitro. Methods: The competitor concentration (IC 50) of I 2 R and the radioligand was determined by the competitive binding assay of normal rat brain I 2 R and 50% radioligand binding. To observe the binding ability of LMS and I_2R in vitro. Through LMS long-term in vivo treatment of rat brain I 2 R saturation binding assay LMS long-term treatment rats and control group I 2 R density and affinity of the brain tissue. Results: In vitro experiments showed that LMS could compete with [~ 3H] -2BFI for binding to I_2R in rat brain in a concentration - dependent manner. The value of IC 50 was 1.292 × 10 -5 mol·L -1 and the value of K_i was 9.796 × 10 -6 mol·L -1. Long-term in vivo LMS treatment of rats, the brain tissue I 2 R density was significantly increased (P <0.05), while the affinity between the two groups was no significant difference. Conclusion: Levamisole can directly bind to I_2R in brain tissue, which may be the ligand of I_2R. Long-term effect of levamisole in the body can cause the I 2 R density of brain tissue increased.