- 简介
2-苯基-4-喹啉羧酸(药品名辛可芬)，为解热、镇痛、治风湿病的药物，但临床应用表明该药疗效差，毒副作用大，卫生部已于1982年9月决定淘汰之。各国化学工作者已致力于其衔生物的制备与研究，以期改进其性能。
- 生物活性
Cinchophen是一种止痛药，经常用于治疗痛风。
- 体外研究
Cinchophen（2 - 苯基喹啉-4 - 羧酸）是一个功能强大的抗菌剂。 兽医将Cinchophen和泼尼松龙组合使用，治疗动物的关节炎。由于发现cinchophen会引起严重的肝损伤， 1930s停止了该药在人体的使用。
- 体内研究
Cinchophen (oral gavage; 25-44 mg/kg; twice daily) combines prednisolone ( 0.125-0.220 mg/kg; twice daily) for 14 days is effective in dogs with osteoarthritis and well tolerated. The combination exhibits significantly improved lameness, weight bearing, joint mobility and stiffness scores and is similar in clinical efficacy to phenylbutazone.The kinetics and efficacy of a cinchophen prednisolone combination preparation (PLT) is tested. Cinchophen administation at a dose rate of 12.5 mg/kg intravenously exhibits a volume of distribution (V
d
area) of 0.13 L/kg, shows a clearance rate (Cl) of 0.15 L/h and a half-life (t
1/2β
) of 7.92 hours. The plasma concentration time curve (AUC0-∞) is 1187.0 μ/ml.h in dogs.
Cinchophen administation (oral gavage; 12.5 mg/kg; single dose) exhibits a mean maximum plasma concentration (C
max
) of 77.75 μg/ml and the time of Cmax (t
max
) is 2.76 hours. The plasma concentration time curve (AUC
0-∞
) is almost as large following oral as intravenous administration indicating an oral bioavailability (F) of 87.21%.
- 化学性质
白色或淡黄色结晶性粉末。粉点213-216℃。1g该品可溶于约400ml氯仿、100ml乙醚、120ml乙醇，几乎不溶于水。味微苦，几乎无臭。露置阳光下易起变化。
- 解热镇痛药。用于急慢性关节炎、风湿痛、神经痛、腰痛、痛风、头痛等。
