吸收和射流奎纳克林,候选人朊病毒疾病的治疗,血脑屏障。
文章的细节
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引用
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Dohgu年代,山内,中国人F,泽田师傅Y, Higuchi年代,Naito M, Tsuruo T, Shirabe年代,丹羽宇一郎M, Katamine年代,Kataoka Y
吸收和射流奎纳克林,候选人朊病毒疾病的治疗,血脑屏障。
细胞摩尔一般人。2004年4月,24(2):205 - 17所示。
- PubMed ID
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15176436 (在PubMed]
- 文摘
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1。临床试验的奎纳克林克雅二氏症患者现在在进步。渗透率的药物通过血脑屏障(BBB)是一个行列式的朊病毒疾病的治疗效果。奎纳克林运输在BBB的机理研究使用老鼠大脑内皮细胞(MBEC4)。2。通过MBEC4奎纳克林细胞的渗透性是低于荧光素钠,BBB-impermeable标记。奎纳克林的basolateral-to-apical运输是大于其apical-to-basolateral运输。在22 (P-gp)抑制剂,环孢霉素或维拉帕米,apical-to-basolateral运输奎纳克林增加。奎纳克林MBEC4细胞的吸收增强的环孢霉素或维拉帕米。3所示。 Quinacrine uptake was highly concentrative, this event being carried out by a saturable and carrier-mediated system with an apparent Km of 52.1 microM. Quinacrine uptake was insensitive to Na+-depletion and changes in the membrane potential and sensitive to changes in pH. This uptake was decreased by tetraethylammonium and cimetidine, a substrate and an inhibitor of organic cation transporters, respectively. 4. These findings suggest that quinacrine transport at the BBB is mediated by the efflux system (P-gp) and the influx system (organic cation transporter-like machinery).
beplay体育安全吗DrugBank数据引用了这篇文章
- 药物转运蛋白
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药物 转运体 类 生物 药理作用 行动 阿的平 溶质载体家庭22个成员2 蛋白质 人类 未知的抑制剂细节