Pharmacological studies of the new antiinflammatory agent 3-formylamino-7-methylsulfonylamino-6-phenoxy-4H-1-benzopyran-4-o ne. 1st communication: antiinflammatory, analgesic and other related properties.
The antiinflammatory, analgesic and antipyretic activities of 3-formylamino-7-methylsulfonylamino-6-phenoxy-4H-1-benzopyran-4-on e (T-614, CAS 123663-49-0) were investigated in various animal models and compared with those of nimesulide, indomethacin and ibuprofen. The antiinflammatory potency of T-614 on carrageenin-induced paw edema, paper disk granuloma and established adjuvant arthritis was greater than that of ibuprofen, but slightly lower than those of nimesulide and indomethacin. In acute inflammatory models, unlike indomethacin, T-614 suppressed the edemas provoked by dextran and bromelain in rats, but its inhibitory action on ultraviolet erythema in guinea-pigs was weak. Although the analgesic activity of T-614 was hardly demonstrated in writhing tests in mice, its potency against the inflammatory pain such as Randall-Selitto test, adjuvant-induced hyperalgesia and antigen-induced arthritic pain in rats was superior to that of ibuprofen. Moreover, it had a potent analgesic effect on urate-induced synovitis in dogs. T-614 exerted a prompt and strong antipyretic effect in both yeast-induced febrile rats and lipopolysaccharide-induced febrile rabbits. T-614 had virtually no gastrointestinal ulcerogenic action and did not affect water and sodium excretion in rats. T-614 is a novel antiinflammatory compound with different pharmacological properties from that of the reference drugs.
Tanaka
K
K
Research Laboratories, Toyama Chemical Co., Ltd., Japan.
Shimotori
T
T
Makino
S
S
Aikawa
Y
Y
Inaba
T
T
Yoshida
C
C
Takano
S
S
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology* / Q000633:toxicity; D001169:Arthritis, Experimental / Q000188:drug therapy; D001578:Benzopyrans / Q000494:pharmacology* / Q000633:toxicity; D004285:Dogs; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D004890:Erythema / Q000517:prevention & control; D005260:Female; D005334:Fever / Q000139:chemically induced / Q000517:prevention & control; D006099:Granuloma / Q000517:prevention & control; D006168:Guinea Pigs; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D010147:Pain Measurement; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar; D013276:Stomach Ulcer / Q000139:chemically induced; D013449:Sulfonamides / Q000494:pharmacology* / Q000633:toxicity; D014882:Water-Electrolyte Balance / Q000187:drug effects
D000894:Anti-Inflammatory Agents, Non-Steroidal; D001578:Benzopyrans; D013449:Sulfonamides; C077313:T 614; C012655:nimesulide