Anti-inflammatory, analgesic and ulcerogenic activities of CS-
600
and its active metabolite were investigated in rats. Anti-carrageenin edema activity of CS-
600
(ID
50: 1.2 mg/kg) was as potent as that of the active metabolite (ID
50: 1.3 mg/kg) . Analgesic effect of CS-
600
(ID
50: 0.76 mg/kg) on scald pain was also equipotent to that of the metabolite (ID
50: 1.1 mg/kg) . However, gastrointestinal irritancy of CS-
600
(UD
50: 16.1 mg/kg for the stomach and 11.5 mg/kg for the intestine) was lower than that of the active metabolite (UD
50: 3.2 mg/kg for the stomach and 3.1 mg/kg for the intestine) . When [
14C] CS-
600
was injected into a ligated jejunum in rats, most radioactivity was found as the unchanged CS-
600
in the portal blood. These findings indicate that CS-
600
is absorbed from the intestine in the less irritating form and that it is converted rapidly to the active metabolite which shows the potent pharmacological efficacy.
抄録全体を表示