- 日
- 関
English Journal
- Synthesis and biological evaluation of novel chiral diazepine derivatives as bombesin receptor subtype-3 (BRS-3) agonists incorporating an antedrug approach.
- Matsufuji T1, Shimada K2, Kobayashi S2, Ichikawa M2, Kawamura A2, Fujimoto T2, Arita T2, Hara T3, Konishi M3, Abe-Ohya R3, Izumi M3, Sogawa Y3, Nagai Y4, Yoshida K4, Abe Y5, Kimura T6, Takahashi H2.
- Bioorganic & medicinal chemistry.Bioorg Med Chem.2015 Jan 1;23(1):89-104. doi: 10.1016/j.bmc.2014.11.018. Epub 2014 Nov 21.
- Novel compounds based on the lead BRS-3 agonists from our HTS compounds 2a and 2b have been synthesized with the focus on obtaining peripheral BRS-3 agonists. To identify potent anti-obesity compounds without adverse effects on the central nerve system, a labile carboxylic ester with an antedrug fun
- PMID 25497965
- Design and synthesis of 5-[(2-chloro-6-fluorophenyl)acetylamino]-3-(4-fluorophenyl)-4-(4-pyrimidinyl)isoxazole (AKP-001), a novel inhibitor of p38 MAP kinase with reduced side effects based on the antedrug concept.
- Hasumi K1, Sato S1, Saito T1, Kato JY1, Shirota K2, Sato J3, Suzuki H3, Ohta S4.
- Bioorganic & medicinal chemistry.Bioorg Med Chem.2014 Aug 1;22(15):4162-76. doi: 10.1016/j.bmc.2014.05.045. Epub 2014 Jun 3.
- Inhibitors of p38 mitogen-activated protein (MAP) kinase, which are closely involved in the production of inflammatory cytokines, are considered promising curative drugs for chronic inflammatory disorders. However, there is also a growing concern regarding its systemic side effects. To reduce the oc
- PMID 24938496
- Inhibition by new glucocorticoid antedrugs [16α, 17α-d] isoxazoline and [16α, 17α-d]-3'-hydroxy-iminoformyl isoxazoline derivatives of chemotaxis and CCL26, CCL11, IL-8, and RANTES secretion.
- Errahali YJ1, Thomas LD, Keller TC 3rd, Lee HJ.
- Journal of interferon & cytokine research : the official journal of the International Society for Interferon and Cytokine Research.J Interferon Cytokine Res.2013 Sep;33(9):493-507. doi: 10.1089/jir.2012.0129. Epub 2013 May 16.
- The underlying inflammation present in chronic airway diseases is orchestrated by increased secretion of CC and CXC chemokines that selectively recruit the leukocyte populations into the pulmonary system. Human chemokines, eotaxins (CCL11 and CCL26), RANTES, and interleukin (IL)-8, are dramatically
- PMID 23679817
Japanese Journal
- Antedrug Budesonide by Intrapulmonary Treatment Attenuates Bleomycin-Induced Lung Injury in Rats with Minimal Systemic Adverse Effects
- Kohno Masayuki,Haramoto Mari,Nakajima Oumi [他],Yang Liying,Hinotsu Shiro,Yokohira Masanao,Imaida Katsumi,Kawakami Koji
- Biological and Pharmaceutical Bulletin 33(7), 1206-1211, 2010
- … To improve this situation, we used an animal model of pulmonary injury and early fibrosis and investigated whether the combination of an intrapulmonary inhalation device with antedrug budesonide (BUD) administered to the lung had greater efficacy and fewer systemic adverse effects compared to long-acting dexamethasone (DEX). … This study suggests that antedrug BUD by intrapulmonary treatment has local anti-inflammatory and antifibrotic effects with minimal systemic adverse effects. …
- NAID 130000300288
- 虫垂瘻からのステロイド antedrug 注入療法を施行した潰瘍性大腸炎の3例
- 宮澤 智徳,岡本 春彦,谷 達夫,飯合 恒夫,畠山 勝義,本間 照,杉村 一仁,青柳 豊
- 日本大腸肛門病学会雑誌 59(4), 203-207, 2006-04-01
- … We present three cases of steroid hormone (SH) dependent total-colitis-type ulcerative colitis (UC) patients who underwent antedrug SH injection therapy via appendicostomy.<BR>Case 1 : A 21-year-old woman. …
- NAID 10018167527
- 22 虫垂瘻からのSteroid antedrug腸内投与が奏効した潰瘍性大腸炎の2例(I.一般演題,第75回新潟消化器病研究会)
- 宮澤 智徳,亀山 仁史,岩谷 昭,早見 守仁,桑原 明史,小出 則彦,山崎 俊幸,飯合 恒夫,岡本 春彦,須田 武保,畠山 勝義,本間 照,朝倉 均
- 新潟医学会雑誌 118(7), 364, 2004-07-10
- NAID 110004780569
Related Links
- Antedrug 科学的修飾により作用増強された局所適用の外用剤として用いられる薬物.投与部位では活性を有し,体内に入ると速やかに代謝されて不活化するか、または活性が低くなる.全身的副作用を軽減する目的で開発された薬剤。
- antedrug アンテドラッグ ←→prodrug 分子構造を化学的に修飾し、作用を増強した局所適用の薬剤。投与部位では薬剤本来の強い作用を示すが、体内に吸収されると速やかに低活性型や不活性型に変化する性質を持つ 。副腎皮質ホルモン ...
Related Pictures
★リンクテーブル★
[★]
- 英
- 関
- 英
- antedrug