sertindole对细胞外的影响多巴胺、乙酰胆碱和内侧前额叶皮质谷氨酸的有意识的老鼠:比较利培酮与机制的探索。

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莫克威滕LM, Arnt J

sertindole对细胞外的影响多巴胺、乙酰胆碱和内侧前额叶皮质谷氨酸的有意识的老鼠:比较利培酮与机制的探索。

精神药理学(Berl)。2009年9月,206 (1):39-49。doi: 10.1007 / s00213 - 009 - 1578 - 4。Epub 2009 6月9。

PubMed ID

19506838 (在PubMed

]

文摘

理由是:第二代抗精神病药物对认知有有益的影响。最近的研究,此外,表明微分的影响第二代抗精神病药物在执行认知功能障碍。目的:评估第二代抗精神病药物的影响,sertindole,在细胞外水平的多巴胺(DA),乙酰胆碱(ACh)和谷氨酸(Glu)大鼠内侧前额叶皮层(mPFC)。利培酮进行了研究比较。此外,选择性血清素5 - (2),5 - (2 c)和5(6)受体拮抗剂,鉴于单独和结合优惠DA D(2)受体拮抗剂,氟哌啶醇,进一步阐明这两种药物的作用。材料与方法:老鼠敏锐地与车辆或药物治疗,细胞外神经递质水平在评估了微量透析可把时程延长自由移动的动物。结果:Sertindole和利培酮显著增加细胞外的DA水平。氟哌啶醇;5 - (2 a)受体拮抗剂,M100907;5 - (2 c)受体拮抗剂,SB242084; and the 5-HT(6) receptor antagonist, GSK-742457, induced minor increases in levels of DA, but the three latter compounds raised the DA levels notably in combination with haloperidol. Sertindole and risperidone significantly increased the extracellular levels of ACh but only sertindole raised the extracellular levels of Glu. The selective 5-HT(6) receptor antagonist, SB-271046, significantly increased the extracellular levels of Glu. CONCLUSION: Sertindole and risperidone markedly increased extracellular levels of DA in mPFC. The built-in 5-HT(2A)/5-HT(2C)/D(2) receptor antagonism of the two drugs might be involved in this action. Both drugs increased the extracellular levels of ACh but only sertindole enhanced Glu levels. The high affinity of sertindole for the 5-HT(6) receptor compared to risperidone may differentiate sertindole from risperidone.

DrugBank数据引用了这篇文章

药物靶点

药物	目标	类	生物	药理作用	行动
Sertindole	5 -羟色胺受体6	蛋白质	人类	是的	拮抗剂	细节
Sertindole	多巴胺D2受体	蛋白质	人类	是的	拮抗剂	细节