Use of dendrimer prodrugs to bypass efflux transporters

机译：使用树枝状大分子前药绕过外排转运蛋白

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An enhancement of the A→B apparentrnpermeability coefficient, Papp, and decrease in thernB→A Papp of propranolol (a model P-glycoproteinrnsubstrate1) across Caco-2 cell monolayers wasrnobserved when propranolol was covalently boundrnto G3 PAMAM dendrimer. Dendrimers may bernuseful in enhancing the bioavailability of drugsrnthat are substrates for efflux transporters.

机译：当普萘洛尔与G3 PAMAM树状大分子共价结合时，在整个Caco-2细胞单层中，普萘洛尔的A→B表观渗透系数Papp增强，而普萘洛尔（模型P-糖蛋白底物1）的rnB→A Papp降低。树枝状大分子在增强药物的生物利用度方面可能是有用的，所述药物是外排转运蛋白的底物。

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来源
《Controlled Release Society 31st annual meeting transactions: abstracts》|2004年|1-2|共2页
会议地点 Honolulu HI(US)
作者
Rachaneekorn Jevprasesphant; Jeffrey Penny; David Attwood; Antony DEmanuele;
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作者单位

School of Pharmacy and Pharmaceutical Sciences, University of Manchester,rnManchester, M13 9PL, UK;

School of Pharmacy and Pharmaceutical Sciences, University of Manchester,rnManchester, M13 9PL, UK;

School of Pharmacy and Pharmaceutical Sciences, University of Manchester,rnManchester, M13 9PL, UK;

School of Pharmacy and Pharmaceutical Sciences, University of Manchester,rnManchester, M13 9PL, UK Antony@Demanuele.net;

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原文格式 PDF
正文语种 eng
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关键词
Dendrimers; Caco-2 cells; propranolol; rnP-glycoprotein; transepithelial transport;

机译：树枝状聚合物Caco-2细胞；普萘洛尔; rnP-糖蛋白;经上皮运输;

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专利

1. The use of a dendrimer-propranolol prodrug to bypass efflux transporters and enhance oral bioavailability [J] . DEmanuele A, Jevprasesphant R, Penny J, Journal of Controlled Release: Official Journal of the Controlled Release Society . 2004,第3期

机译：使用树枝状大分子普萘洛尔前药绕过外排转运蛋白并增强口服生物利用度
2. The use of a dendrimer-propranolol prodrug to bypass efflux transporters and enhance oral bioavailability [J] . DEmanuele A, Jevprasesphant R, Penny J, Journal of Controlled Release: Official Journal of the Controlled Release Society . 2004,第3期

机译：使用树枝状大分子普萘洛尔前药绕过外排转运蛋白并增强口服生物利用度
3. Zidovudine and ursodeoxycholic acid conjugation: Design of a new prodrug potentially able to bypass the active efflux transport systems of the central nervous system [J] . DalpiazA., PaganettoG., PavanB., Molecular pharmaceutics . 2012,第4期

机译：齐多夫定和熊去氧胆酸共轭：一种新的前药设计，可能能够绕过中枢神经系统的主动外排转运系统
4. Use of dendrimer prodrugs to bypass efflux transporters [C] . Controlled Release Society annual meeting . 2004

机译：使用树突前药物来绕过流出运输车
5. Role of basolateral efflux transporters in intestinal absorption of drugs and prodrugs. [D] . Ming, Xin. 2008

机译：基底外侧外向转运蛋白在药物和前药的肠道吸收中的作用。
6. Dendrimer Prodrugs [O] . Soraya da Silva Santos, Elizabeth Igne Ferreira, Jeanine Giarolla 2016

机译：树枝状前药
7. In vitro models of the human blood-brain barrier and the impact of efflux transporters on neurological disorders: the work of Cioni et al. (2012)A commentary on: Expression of tight junction and drug efflux transporter proteins in an in vitro model of human blood-brain barrierCioni C, Turlizzi E, Zanelli U, Oliveri G, Annunziata P. Front. Psychiatry 2012; 3, 47 [O] . Silke eVogelgesang, Gabriele eJedlitschky 2014

机译：人体血脑屏障的体外模型和外排转运蛋白对神经系统疾病的影响：Cioni等人的工作。（2012）评论：在人血脑屏障Cioni C，Turlizzi E，Zanelli U，Oliveri G，annunziata p. Front的体外模型中紧密连接和药物外排转运蛋白的表达。精神病学2012; 3,47

Use of dendrimer prodrugs to bypass efflux transporters

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