Talampanel,一种新颖的非竞争性AMPA拮抗剂,在大鼠创伤性脑损伤后神经保护。

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刘Belayev L,阿隆索,Y, Chappell,赵W,金斯堡博士Busto R

Talampanel,一种新颖的非竞争性AMPA拮抗剂,在大鼠创伤性脑损伤后神经保护。

J创伤。2001年10月,18 (10):1031 - 8。

PubMed ID

11686490 (在PubMed

]

文摘

(Talampanel [(R) 7-acetyl-5) - 4-aminophenyl 8日9-dihydro-8-methyl-7H-1, 3-dioxolo [4, 5 h][2、3]苯二氮)是一种口服有效的非竞争性拮抗剂AMPA谷氨酸兴奋性氨基酸受体的亚型。本研究的目的是确定talampanel治疗是否会保护大鼠创伤性脑损伤(TBI)模型。24小时在创伤性脑损伤之前,大界面旁矢状面的定位在正确的大脑皮层。第二天,禁食大鼠氟烷麻醉有3%,70%,一氧化二氮和氧平衡;机械通风和生理调节;和受到parieto-occipital旁矢状面的大伤(1.5 - -2.0 atm)。代理(talampanel丸注入4毫克/公斤随后注入4毫克/公斤/小时超过72 h)或车辆管理输液开始30分钟或创伤后3小时以内。创伤性脑损伤后七天,大脑被perfusion-fixed,各级日冕部分数字化,挫伤测量领域。talampanel治疗,创伤后制定了30分钟,显著降低挫伤总面积相比vehicle-treated老鼠(0.54 + / - 0.25和1.79 + / - 0.42平方毫米,分别)。talampanel治疗开始在3 h时,失去了药物的神经保护作用。 In addition, treatment with talampanel starting at 30 min significantly attenuated neuronal damage in all three subsectors of the hippocampal CA1 sector compared to vehicle-treated rats (normal-neuron counts, right (ipsilateral) medial CA1: 80.3 +/- 2.0 [talampanel] vs. 66.3 +/- 2.1 [vehicle] (mean +/- SEM); middle CA1: 71.5 +/- 2.0 vs. 60.3 +/- 2.2; lateral CA1: 74.5 +/- 3.0 vs. 63.0 +/- 3.2, respectively). By contrast, when talampanel treatment was begun at 3 h, normal pyramidal-neuron counts were almost identical in both groups. Our findings document that talampanel therapy instituted 30 min after trauma significantly reduces histological damage.

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药物

Talampanel