Characterization of Hepatobiliary Transport Systems of a Novel α4β1/α4β7 Dual Antagonist, TR-14035

Minoru Tsuda-Tsukimoto; Tomoji Maeda; Takashi Iwanaga; Toshiyuki Kume; Ikumi Tamai

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Characterization of Hepatobiliary Transport Systems of a Novel α4β1/α4β7 Dual Antagonist, TR-14035

机译：新型α4β1/α4β7双重拮抗剂TR-14035的肝胆运输系统特性

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摘要

Our previous pharmacokinetic studies have demonstrated that TR-14035, a novel dual antagonist for α4β1/α4β7 integrin, selectively and strongly accumulated in the liver and was mainly excreted in bile as an unchanged drug. In the present study, we investigated the hepatobiliary transport system in detail.

机译：我们以前的药代动力学研究表明，TR-14035是α4β1/α4β7整联蛋白的新型双重拮抗剂，在肝脏中选择性而强烈地积聚，并作为未改变的药物主要在胆汁中排泄。在本研究中，我们详细研究了肝胆运输系统。

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来源
《Pharmaceutical Research》 |2006年第11期|2646-2656|共11页
作者
Minoru Tsuda-Tsukimoto; Tomoji Maeda; Takashi Iwanaga; Toshiyuki Kume; Ikumi Tamai;
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作者单位

Exploratory DMPK Exploratory Toxicology ampamp DMPK Research Laboratories Tanabe Seiyaku Co. Ltd. 2-2-50 Kawagishi Toda Saitama 335-8505 Japan;

Faculty of Pharmaceutical Sciences Tokyo University of Science Chiba Japan;

Faculty of Pharmaceutical Sciences Tokyo University of Science Chiba Japan;

Exploratory DMPK Exploratory Toxicology ampamp DMPK Research Laboratories Tanabe Seiyaku Co. Ltd. 2-2-50 Kawagishi Toda Saitama 335-8505 Japan;

Faculty of Pharmaceutical Sciences Tokyo University of Science Chiba Japan;

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原文格式 PDF
正文语种 eng
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关键词
genetic polymorphism; hepatobiliary transport; MRP2; OATP;

机译：遗传多态性;肝胆运输;MRP2;OATP;

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专利

1. Characterization of hepatobiliary transport systems of a novel alpha4beta1/alpha4beta7 dual antagonist, TR-14035. [J] . Tsuda-Tsukimoto M, Maeda T, Iwanaga T, Pharmaceutical research . 2006,第11期

机译：新型alpha4beta1 / alpha4beta7双重拮抗剂TR-14035的肝胆运输系统的表征。
2. Synthesis and SAR of N-benzoyl-L-biphenylalanine derivatives: discovery of TR-14035, a dual alpha(4)beta(7)/alpha(4)beta(1) integrin antagonist. [J] . Sircar I, Gudmundsson KS, Martin R, Bioorganic and medicinal chemistry . 2002,第6期

机译：N-苯甲酰基-L-联苯丙氨酸衍生物的合成和合成孔径雷达：TR-14035，双alpha（4）beta（7）/ alpha（4）beta（1）整合素拮抗剂的发现。
3. Establishment of a set of double transfectants coexpressing organic anion transporting polypeptide 1B3 and hepatic efflux transporters for the characterization of the hepatobiliary transport of telmisartan acylglucuronide. [J] . Ishiguro N, Maeda K, Saito A, Drug Metabolism and Disposition: The Biological Fate of Chemicals . 2008,第4期

机译：建立一套共表达有机阴离子转运多肽1B3和肝外排转运蛋白的双重转染子，以表征替米沙坦acyluclucuronide的肝胆转运。
4. Acquired Alterations of Hepatobiliary Transport Systems in Human Cholestatic Liver Diseases: Potential Targets of Pharmacotherapy* [C] . M.trauner, P. Fickert, G. Zollner, Falk Symposium . 2003

机译：在人胆固醇肝病中获得肝胆输送系统的改变：药物治疗的潜在目标*
5. Polyamine transport in Chinese hamster ovary cells: Characterization of a mammalian polyamine transport system [D] . Byers, Timothy Lee 1988

机译：中国仓鼠卵巢细胞中的多胺转运：哺乳动物多胺转运系统的表征
6. Evaluation of the Endothelin Receptor Antagonists Ambrisentan Bosentan Macitentan and Sitaxsentan as Hepatobiliary Transporter Inhibitors and Substrates in Sandwich-Cultured Human Hepatocytes [O] . Eve-Irene Lepist, Hunter Gillies, William Smith, -1

机译：内皮素受体拮抗剂AmbrisentanBosentanMacitentan和Sitaxsentan作为夹心培养的人肝细胞中肝胆转运蛋白抑制剂和底物的评估
7. Evaluation of the endothelin receptor antagonists ambrisentan, bosentan, macitentan, and sitaxsentan as hepatobiliary transporter inhibitors and substrates in sandwich-cultured human hepatocytes. [O] . Eve-Irene Lepist, Hunter Gillies, William Smith, 2014

机译：评价内皮素受体拮抗剂安立生坦，波生坦，马西坦和西他生坦作为肝胆转运蛋白抑制剂和夹心培养的人肝细胞中的底物。

Characterization of Hepatobiliary Transport Systems of a Novel α4β1/α4β7 Dual Antagonist, TR-14035

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