51543-40-9
基本信息
(R)-氟比洛芬
氟比洛芬 EP標準品
(R)-2-氟比洛芬
(R)-(-)-2-氟-Α-甲基-4-聯苯乙酸
(R)-(-)-2-氟-ALPHA-甲基-4-聯苯乙酸
(R)-FL
MPC 7869
Flurizan
Furbiprofen
Tarenflurbil
Flurbiprofene
l-Flurbiprofen
2-Flurbiprofen
(R)-FLURBIPROFEN
物理化學性質
常見問題列表
其他不良反應有惡心、腹瀉、腹痛、視力模糊、尿路感染征候、皮炎等。少數有肝轉氨酶增高,繼續(xù)用藥,可能發(fā)展,亦可保持不變或消失。滴入眼時有輕度的刺痛感和燒灼感及(或)視覺紊亂。因影響血小板聚集而延長出血時間,有眼科手術應用本藥后增加眼內出血傾向的報道。動物實驗中,氟比洛芬50~100 mg/kg,用藥3月,可引起腎乳頭壞死。對人類亦可有此作用。
IC50: 75 μM (RXRα)
Tarenflurbil ((R)-Flurbiprofen) can significantly reduce Aβ secretion, but at the same time, increases the level of intracellular Aβ. The binding between [ 3 H]9-cis-RA and RXRα is competitively inhibited by both unlabeled (R)-Flurbiprofen and 9-cis-RA. (R)-Flurbiprofen can interfere with the interaction between RXRα and 9-cis-retinoid acid (9-cis-RA), and that 9-cis-RA decreases Tarenflurbil ((R)-Flurbiprofen)’s reduction of Aβ secretion. Tarenflurbil ((R)-Flurbiprofen) treatment significantly increases the levels of intracellular Aβ species. The well characterized, nonsteroidal anti-inflammatory drug (nonsteroidal anti-inflammatory drug), Tarenflurbil ((R)-Flurbiprofen) affects only Aβ and not Notch β formation, indicating that second generation GSMs and nonsteroidal anti-inflammatory drug-based GSMs have different modes of action regarding Notch processing.
Effects of the early and late onset of treatment with Tarenflurbil ((R)-Flurbiprofen) are assessed in C57BL6/J mice that develop a non-remitting form of the disease, and in SJL mice that develop a relapsing-remitting (RR)-EAE. Tarenflurbil ((R)-Flurbiprofen) completely prevents the development of clinical EAE scores in C57BL6/J mice when the treatment is started within 3 days after immunization. This regimen is referred to as preventive treatment. The effect is dose-dependent, and the minimum daily dose for complete prevention is 5 mg/kg/day. Effects of Tarenflurbil ((R)-Flurbiprofen) are comparable to those of Fingolimod (FTY720, 0.5 mg/kg/day), which is used as the positive control. Tarenflurbil ((R)-Flurbiprofen) also significantly reduces clinical EAE scores in C57BL6/J mice when treatment is started shortly before onset of clinical manifestations, referred to as semi-therapeutic (10 mg/kg/day) and reduces clinical scores when the treatment is initiated after full development of the disease on day 13 (5 mg/g/day).