1972 年 92 巻 1 号 p. 1-10
The anti-inflammatory effect of bimetopyrol [2-methyl-4, 5-bis (p-methoxyphenyl) pyrrole], a newly synthesized pyrrole compound, was examined. Bimetopyrol is effective against carrageenin-induced rat paw edema ; the potency is 9.6 (6.2-15.8) and 5.4 (4.3-7.1) times more potent than phenylbutazone when given orally in tragacanth suspension and in olive oil solution, respectively. The spectrum of anti-inflammatory and other pharmacological activities of this compound is generally in common with those of other nonsteroidal anti-rheumatic drugs. Thus, bimetopyrol suppresses ultraviolet-induced erythema in guinea pigs and acetic acid-induced writhing in mice, and increases pain threshold in the yeast-injected rat paw. Also, it prevents the yeast-induced fever in rats. Bimetopyrol is not effective against permeability changes induced by serotonin, bradykinin, and dextran, again in agreement with the data obtained by indomethacin or phenylbutazone. As further comparative studies between bimetopyrol and other anti-inflammatory drugs, histological examination on cotton pellet granuloma and emigration rate of leucocytes were investigated both in vivo and in vitro and characteristic aspects of bimetopyrol were discussed. The acute LD 50 of this compound was calculated as 2, 300 mg/kg by oral administration in male rats.