The anti-inflammatory activity and the mode of action of
M73101, a new non-
steroid analgesic anti-inflammatory agent, were investigated in experimental animals and compared with those of reference drugs.
M73101 inhibited the increase in vascular permeability induced by
acetic acid and its activity was more potent than that of
phenylbutazone.
M73101 showed a marked inhibitory effect against rat paw
edema induced by various phlogistic agents (
carrageenin,
dextran,
histamine,
serotonin and
bradykinin) and the activities were equal to or more potent than those of
aminopyrine,
mepirizole and
tiaramide HCl.
M73101 also inhibited the
edema induced by mustard, scalding and anti-rat rabbit serum in rats. In addition, the anti-edematous effect of
M73101 on
carrageenin-induced rat paw
edema was not influenced by spinalectomy or
adrenalectomy, indicating that the anti-inflammatory action of
M73101 was not mediated by the central nervous system and the adrenals. Local and
oral administration of
M73101 inhibited significantly the leucocyte migration into the fluid of CMC pouch in rats and the activity was more potent than
phenylbutazone, suggesting that the anti-inflammatory effect of
M73101 was due to the direct action at the inflamed site. On the other hand,
M73101 did not show any marked activities on the experimental chronic inflammatory models. From these results, it is suggested that
M73101 may be useful for clinical application as a basic
analgesic, anti-inflammatory
drug with remarkable anti-inflammatory activity in acute and subacute cases. The mechanism of the anti-inflammatory action of
M73101 probably involves inhibition of an increase in vascular permeability and leucocyte migration.