Amanuma F, Okuyama S, Aihara H, Kameyama T
J Pharmacobiodyn. 1985 Aug;8(8):687-93. doi: 10.1248/bpb1978.8.687.
FI-302, N-(3-piperidinopropyl)-4-methyl-6-trifluoromethyl-furo[3,2-b]indol e-2-carboxamide, is a new non-steroidal anti-inflammatory compound. The analgesic effect of FI-302 was investigated in comparison with those of non-steroidal anti-inflammatory drugs (NSAIDs). In the tail pressure, hot plate and D'Amour and Smith methods, FI-302 showed a potent analgesic effect, its efficacy being about 2 to 7 times greater than those of aminopyrine, mepirizole and tiaramide. On the other hand, in these methods, aspirin, ibuprofen and phenylbutazone had little or no effect. FI-302 showed a potent inhibitory effect on the vocalization response produced by electrical stimulation. Moreover, the analgesic effect of FI-302 after intracerebroventricular injection was about 58 to 278 times more potent than those of tiaramide and ibuprofen, and about 1/6 that of morphine. However, the analgesic effect of FI-302 was not antagonized by levallorphan. From these results, it appears that FI-302 has potent analgesic effects which may be produced by both peripheral and central mechanisms, but it is a non-narcotic compound. Consequently, FI-302 should be suitably applicable for clinical purposes.
FI-302,即N-(3-哌啶丙基)-4-甲基-6-三氟甲基-呋喃并[3,2-b]吲哚-2-甲酰胺,是一种新型非甾体抗炎化合物。将FI-302的镇痛效果与非甾体抗炎药(NSAIDs)的镇痛效果进行了比较研究。在尾压法、热板法以及达莫尔和史密斯法中,FI-302显示出强效镇痛作用,其效力约为氨基比林、美匹立唑和替拉米特的2至7倍。另一方面,在这些方法中,阿司匹林、布洛芬和保泰松几乎没有效果或完全没有效果。FI-302对电刺激引起的发声反应显示出强效抑制作用。此外,脑室内注射后FI-302的镇痛效果比替拉米特和布洛芬强约58至278倍,约为吗啡的1/6。然而,纳络芬不能拮抗FI-302的镇痛作用。从这些结果来看,FI-302似乎具有强效镇痛作用,可能由外周和中枢机制共同产生,但它是一种非麻醉性化合物。因此,FI-302应适合用于临床目的。