The novel analgesic filenadol ,4'-methylenedioxyphenyl)-1-morpholinopr
opan-2-ol) inhibited phenyl-p-benzoquinone-induced writhing in mice wi
th ID50 values of 68.8 (p.o.), 1.67 (i.v.) and 0.48 (i.c.v.) mg/kg. Hy
peralgesia induced by arachidonic acid, PGE(2) or LTB(4) in this test
was also decreased by filenadol (ID50 = 24.4, 3.7 and 50.1 mg/kg p.o.,
respectively). This compound was effective on PGE(2), LTB(4), bradyki
nin, PAF or IL-1 beta-induced decrease in pain threshold in the rat pa
w pressure model and almost totally suppressed the writhing induced by
zymosan in mice, while peritoneal production of 6-ketoPGF(1 alpha), w
as inhibited by 48.5-62 % and only at 100 mg/kg significant inhibition
of LTC(4) was achieved. The late phase of formalin-induced pain respo
nse in mice was prevented by filenadol, without affecting the oedema.
Filenadol is an antinociceptive agent that reduces the hyperalgesic ef
fects of inflammatory mediators besides inhibiting partially the synth
esis of eicosanoids.