Zimin I A, Kapitsa I G, Voronina T A, Kovalev G I
Eksp Klin Farmakol. 2010 Nov;73(11):2-5.
The influence of the new antiparkinsonian drug hemantane on D1 receptors in striatum, 5-HT1A receptors in hippocampus, and 5-HT2A receptors in frontal cortex of intact and MPP+-treated (3 microg/0.6 ml dist., intranigral) rats was studied. Hemantane (20 mg/kg, i.p.) was administrated subchronically for 7 days (beginning a day after MPP+ injection). A modulatory effect of hemantane on D1, 5-HT1A and 5-HT2A receptors was revealed. It was found that hemantane increased the binding site density (Bmax) of D1 and 5-HT1A receptors and decreased the binding site density of 5-HT2A receptors without changing the affinity (Kd) to the selective ligands. These results demonstrate that subchronic administration of hemantane leads to the functional rearrangement of dopamine and serotonin receptors in the brain of both intact and MPP+-treated rats.
研究了新型抗帕金森病药物海曼烷对完整大鼠以及经1-甲基-4-苯基吡啶离子(MPP⁺)处理(3微克/0.6毫升蒸馏水,黑质内注射)的大鼠纹状体中D1受体、海马体中5-羟色胺1A(5-HT1A)受体以及额叶皮质中5-羟色胺2A(5-HT2A)受体的影响。海曼烷(20毫克/千克,腹腔注射)连续亚慢性给药7天(在MPP⁺注射后一天开始)。结果显示出海曼烷对D1、5-HT1A和5-HT2A受体具有调节作用。研究发现,海曼烷增加了D1和5-HT1A受体的结合位点密度(Bmax),并降低了5-HT2A受体的结合位点密度,而对选择性配体的亲和力(Kd)没有改变。这些结果表明,亚慢性给予海曼烷会导致完整大鼠和MPP⁺处理大鼠大脑中多巴胺和血清素受体的功能重排。