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目的:观察咪唑啉类药物长期处理后大脑组织中咪唑啉2受体(I_2R)密度和亲和力的变化以及对胶质纤维酸性蛋白(GFAP)表达的影响。方法:将大鼠随机分成生理盐水组、胍丁胺组、育亨宾组、咪唑克生组、左旋咪唑组及2-(2-苯并呋喃基)-2-咪唑啉(2-BFI)组,腹腔注射×2周。采用放射性配体结合试验检测大脑和脑干匀浆中I_2R B_(max)和K_d变化,免疫组化测定小脑和颈髓中GFAP的表达。结果:反映I_2R密度的B_(max)值,咪唑克生、2-BFI和左旋咪唑组较NS组分别上调了80%、93%和122%(均P<0.01)。反映受体亲和力的K_d值,各组间无明显差异。咪唑克生、2-BFI和左旋咪唑组中GFAP表达比生理盐水组明显增加(均P<0.01)。结论:咪唑克生、2-BFI和左旋咪唑表现为拮抗剂特性;I_2R可能参与调节GFAP表达。
OBJECTIVE: To observe the changes of density and affinity of imidazoline 2 receptor (I_2R) and the effect on the expression of glial fibrillary acidic protein (GFAP) in long-term treatment of imidazoline drugs. Methods: The rats were randomly divided into normal saline group, agmatine group, yohimbine group, midazolam group, levamisole group and 2- (2-benzofuranyl) -2-imidazoline Group, intraperitoneal injection × 2 weeks. Radioligand binding assay was used to detect the changes of B_ (max) and K_d of I_2R in brain and brainstem homogenates. The expression of GFAP in cerebellum and cervical spinal cord was detected by immunohistochemistry. Results: The B max values of I_2R density were increased by 80%, 93% and 122% respectively in the Imidazol, 2-BFI and levamisole groups (all P <0.01). K_d value of receptor affinity showed no significant difference between the groups. The expression of GFAP in imidazole, 2-BFI and levamisole groups was significantly higher than that in saline group (all P <0.01). CONCLUSION: Imidaclocide, 2-BFI and levamisole exhibit antagonist properties; I_2R may be involved in the regulation of GFAP expression.