慢性钙拮抗剂治疗对大鼠纹状体多巴胺识别位点的影响。

Effect of chronic calcium antagonist treatment on dopamine recognition sites in rat striatum.

作者信息

Govoni S, Di Giovine S, Moresco R M, Battaini F, Trabucchi M

机构信息

Institute of Pharmacological Sciences, University of Milan, Italy.

出版信息

Neurosci Lett. 1988 Apr 22;87(1-2):173-7. doi: 10.1016/0304-3940(88)90165-6.

DOI:10.1016/0304-3940(88)90165-6

PMID:3380334

Abstract

The effects of nimodipine and flunarizine administration (18 days 15 mg/kg/day p.o.) on striatal dopamine recognition sites in rats were investigated in vivo. In vitro flunarizine but not nimodipine displaces [3H]spiroperidol binding. After in vivo treatment both drugs induce a significant increase in the number of sulpiride displaceable spiroperidol binding sites (flunarizine, +114%, nimodipine +61%) concomitant with an increase in the dissociation constant. Binding parameters return toward control values after 1 week of suspension of the treatment. The results suggest that the repeated in vivo treatment with nimodipine and flunarizine may significantly interact with dopaminergic transmission leading to adaptive changes of the dopamine recognition sites.

摘要

在体内研究了给予尼莫地平与氟桂利嗪（18天，15毫克/千克/天，口服）对大鼠纹状体多巴胺识别位点的影响。在体外，氟桂利嗪而非尼莫地平可取代[3H]螺哌啶的结合。体内治疗后，两种药物均可使舒必利可取代的螺哌啶结合位点数量显著增加（氟桂利嗪增加114%，尼莫地平增加61%），同时解离常数也增加。治疗中断1周后，结合参数恢复至对照值。结果表明，重复给予尼莫地平与氟桂利嗪进行体内治疗可能会与多巴胺能传递发生显著相互作用，从而导致多巴胺识别位点的适应性变化。