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應用
TPPU已被用作可溶性环氧化物水解酶(SEH)抑制剂,用于表征其在啮齿动物中的药代动力学(PK)和药效学特性。它还被用作SEH抑制剂,用于研究其对神经组织中12,13-二羟基-9Z-十八烯酸(12,13-DiHOME)浓度的影响。
生化/生理作用
TPPU 是一种强效 sEH 抑制剂 (IC 50 = 3.7 nM),已证明其在食蟹猴中具有非常有利的 PK 属性。sEH 可将环氧二十碳三烯酸 (EET) 转化为二羟基月桂三烯酸 (DHET),sEH 抑制剂显示抗炎和抗动脉粥样硬化作用。
訊號詞
Danger
危險聲明
危險分類
Acute Tox. 3 Oral
儲存類別代碼
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
Prostaglandins & other lipid mediators, 121(Pt A), 131-137 (2015-06-29)
Epoxides from polyunsaturated fatty acids (PUFAs) are potent lipid mediators. In vivo stabilization of these epoxides by blockade of the soluble epoxide hydrolase (sEH) leads to anti-inflammatory, analgesic and normotensive effects. Therefore, sEH inhibitors (sEHi) are a promising new class
The oxidized linoleic acid metabolite 12, 13-DiHOME mediates thermal hyperalgesia during inflammatory pain
Biochimica et Biophysica Acta - Molecular and Cell Biology of Lipids, 1863(7), 669-678 (2018)
Oral treatment of rodents with soluble epoxide hydrolase inhibitor 1-(1-propanoylpiperidin-4-yl)-3-[4-(trifluoromethoxy) phenyl] urea (TPPU): Resulting drug levels and modulation of oxylipin pattern
Prostaglandins & other lipid mediators, 121 (2015)
Biochimica et biophysica acta. Molecular and cell biology of lipids, 1863(7), 669-678 (2018-04-07)
Eicosanoids play a crucial role in inflammatory pain. However, there is very little knowledge about the contribution of oxidized linoleic acid metabolites in inflammatory pain and peripheral sensitization. Here, we identify 12,13-dihydroxy-9Z-octadecenoic acid (12,13-DiHOME), a cytochrome P450-derived linoleic acid metabolite
Journal of molecular neuroscience : MN, 67(3), 364-372 (2019-01-16)
High level of corticosterone (CORT) is toxic to neurons and plays an important role in depression-like behavior and chronic stress. Our previous study showed that TPPU, a soluble epoxide hydrolase (sEH) inhibitor (sEHI), induces an antidepressant effect in animal models.
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