トラニラスト

外観

わずかにうすい黄色〜うすい黄緑色又はうすい褐色, 結晶〜粉末

溶解性

エタノール溶状：試験適合

用途

ケミカルメディエーター遊離 抑制作用を有します。

用途

ケミカルメディエーター遊離 抑制作用を有します。

効能

抗アレルギー薬, 喘息治療薬, メディエーター遊離抑制薬

商品名

トラメラス (ニッテン); トラメラス (日本点眼薬研究所); リザベン (キッセイ薬品工業); リザベン (キッセイ薬品工業)

化学的特性

Pale Green Solid

使用

Tranilast is a compound that exhibits anti-inflammatory and immunomodulatory effects by inhibiting lipid mediator and cytokine release from inflammatory cells and interfering with PDGF- and TGF-β1-induced proliferation and migration of vascular medial smooth muscle cells. Tranilast suppresses production of prostaglandin D2 (IC50 = 0.1 mM), prostaglandin E2 (IC50 = ~1-20 μM), thromboxane B2 (IC50 = ~10-50 μM), TGF-β1 (IC50 = ~100-200 μM), and interleukin-8 (IC50 = ~100 μM) in in vitro models as well as attenuates of the proinflammatory activity of human monocytes. While originally marketed as an antiallergenic drug, the efficacy of tranilast in preventing restenosis after percutaneous coronary intervention has been tested in a large-scale clinical trial. Additionally, tranilast inhibits VEGF-induced angiogenetic activities (i.e., proliferation, migration and tube formation of vascular endothelial cells) with IC50 values of 22, 18 and 193 μM, which may prove therapeutic for various retinal diseases.[Cayman Chemical]

定義

ChEBI: An amidobenzoic acid that is anthranilic acid in which one of the anilino hydrogens is replaced by a 3,4-dimethoxycinnamoyl group.

生物活性

Antiallergic via inhibition of chemical mediator release from mast cells. Most recently shown to be an effective inhibitor of angiogenesis. Demonstrated to antagonize the effects of angiotensin II on human arteries, possibly by an interaction at the level of the AT 1 receptor.