产品
编 号:F173831
分子式:C20H20ClF6NO
分子量:439.82
产品类型
结构图
CAS No: 148687-76-7
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产品详情
生物活性:
L-733060 hydrochloride is a potent tachykinin NK1 receptor antagonist. L-733060 hydrochloride inhibits neurogenic plasma extravasation at doses that do not cause adverse cardiovascular effects in rodents and also acts as an antitumoral agent.
体内研究:
L-733060 (10-1000 μg/kg; i.v.) inhibits electrically stimulated plasma extravasation in dura mater of rats.L-733060 (300-3000 μg/kg; i.v.) has no significant hypotensive or bradycardic effects are observed at doses of <3000 μg/kg in conscious or anaesthetised rats.Animal Model:Male Sprague-Dawley rats (200 g) with electrical stimulation of the trigeminal ganglion
Dosage:10, 100, 1000 mg/kg
Administration: I.v. injection
Result:Produced a significant dose-related inhibition of plasma extravasation with an ID50 of 212±19 μg/kg.
体外研究:
L-733060 (30-300 nM) inhibits the [Ca2+]i mobilisation caused by substance P (100 nM) in a concentration-dependent manner in human tachykinin NK1 receptor-transfected CHO cells.L-733060 (2.5-20 μM; 48 and or 96 h) results in a concentration-dependent cytotoxicity in COLO 858 cells.L-733060 (10-30 μM; 24 and 48 h) inhibits MEL H0 cells proliferation with IC50s of 27.5 μM and 18.9 μM at 24 h and 48 h, respectively.L-733060 (20-50 μM; and or 72 h) inhibits COLO 679 cells growth with IC50s of 33.8 μM and 31.5 μM at 30 h and 72 h, respectively.