Nicotredole 是一种口服有效的消炎剂,与 Phenylbutazone 的抗炎作用相当。它仅具有弱的致溃疡活性。它可用于缓解疼痛方面的研究。
产品描述
Nicotredole (Tryptamide) is an orally active analgesic and anti-inflammatory agent. Nicotredole exhibits evident anti-inflammatory effects of potency comparable with Phenylbutazone. Nicotredole has only weak ulcerogenic activity.
体外活性
Nicotredole inhibits prostaglandin synthetase activity in vitro assay[1].
体内活性
Nicotredole displays antiinflammatory effects in carrageenin-induced rat paw oedema [1] . Nicotredole reverses pyrogen-induced hyperthermia in rats, elicits analgesic effects in rats, prolongs the time of hexobarbital sleep in rats and inhibits locomotor activity in rats and mice [1] . Nicotredole (i.p.) has LD50s of 1260 mg/kg and 1980 mg/kg for male rats and male mice, respectively [1] . Nicotredole (p.o.) has LD50s of 8.5 g/kg and 9.3 g/kg for male rats and male mice, respectively [1] . Nicotredole (25 mg/kg; p.o. or i.p.) undergoes fast absorption (t 1/2 =4.92-17.5 min) and elimination (t 1/2 =55.72-74.52 min), can reach C max (11-13 μg/cm 3 ) after 30 min, and gives AUC values in the range of 21.40-27.30 (μgoh/cm 3 ) [2] .
Cas No.
29876-14-0
分子式
C16H15N3O
分子量
265.31
别名
尼可曲多;尼可曲朵;Tryptamide
储存和溶解度
DMSO:25 mg/mL (94.23 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years