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首页> 外文期刊>Life sciences >THE VESAMICOL RECEPTOR LIGAND (+)-META-[I-125]IODOBENZYLTROZAMICOL ((+)-[I-125]-MIBT) REVEALS BLUNTING OF THE STRIATAL CHOLINERGIC RESPONSE TO DOPAMINE D2 RECEPTOR BLOCKADE IN THE 6-HYDROXYDOPAMINE (6-OHDA)-LESIONED RAT - POSSIBLE IMPLICATIONS FOR PA
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THE VESAMICOL RECEPTOR LIGAND (+)-META-[I-125]IODOBENZYLTROZAMICOL ((+)-[I-125]-MIBT) REVEALS BLUNTING OF THE STRIATAL CHOLINERGIC RESPONSE TO DOPAMINE D2 RECEPTOR BLOCKADE IN THE 6-HYDROXYDOPAMINE (6-OHDA)-LESIONED RAT - POSSIBLE IMPLICATIONS FOR PA

机译：vesmicicol受体配体（+）-meta- [I-125]碘代苄基三氮杂酚（（+）-[i-125] -mibt）揭示了6-羟基双胍（6-羟基多巴胺）对多巴胺D2受体嵌段的胆碱胆碱反应的支化作用）的老鼠-PA的可能含义

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Previous studies of radiolabelled vesamicol receptor (VR) ligands suggest that the latter may be used, in conjunction with dopamine D2 antagonists, to measure changes in striatal cholinergic function in vivo. In the present study, the radiolabelled VR ligand (+)-meta-[I-125]iodobenzyltrozamicol {(+)[I-125]MIBT} was used to assess striatal cholinergic function in the unilateral 6-hydroxydopamine (6-OHDA)-treated rat. In control animals, the levels of this radiotracer monitored at 3 hr post injection displayed bilateral symmetry in the striatum, cerebral cortex and cerebellum. However, in animals pretreated with the dopamine antagonist spiperone (2 mg/kg ip), the radiotracer concentration in the striatal hemisphere ipsilateral to the 6-OHDA lesion increased by 23% (p = 0.068) while the concentration in the contralateral striatum was elevated by 87% (p < 0.0001). Since the nigrostriatal dopaminergic system modulates striatal cholinergic function, and dopamine D2 receptor blockade is known to result in increased striatal cholinergic function, the refractoriness of striatal cholinergic neurons following the loss of nigrostriatal dopaminergic innervation confirms the existence of a dopaminergic-cholinergic imbalance in Parkinson's disease. Therefore, the combination of a D2:antagonist and radiolabelled VR ligand may provide a potentially useful method for assessing the effects of dopamine depletion in Parkinson's disease. [References: 26]
机译：放射性标记的vesamicol受体（VR）配体的先前研究表明，后者可与多巴胺D2拮抗剂一起用于体内测量纹状体胆碱能功能的变化。在本研究中，使用放射性同位素标记的VR配体（+）-间-[I-125]碘苄基曲扎米醇{（+）[I-125] MIBT}评估单侧6-羟基多巴胺（6-OHDA）的纹状体胆碱能功能治疗的大鼠。在对照动物中，注射后3小时监测的这种放射性示踪剂的水平在纹状体，大脑皮层和小脑中显示出双侧对称。但是，在接受多巴胺拮抗剂spiperone（2 mg / kg ip）预处理的动物中，与6-OHDA病变同侧的纹状体半球中的放射性示踪剂浓度增加了23％（p = 0.068），而对侧纹状体中的放射性示踪剂浓度却升高了降低了87％（p <0.0001）。由于黑质纹状体多巴胺能系统调节纹状体胆碱能功能，并且已知多巴胺D2受体阻滞会导致纹状体胆碱能功能增强，因此，黑质纹状体多巴胺能神经支配力丧失后纹状体胆碱能神经元的难治性证实了多巴胺能失调性胆碱能疾病的存在。 。因此，D2：拮抗剂和放射性标记的VR配体的组合可能为评估多巴胺耗竭在帕金森氏病中的作用提供潜在的有用方法。 [参考：26]

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