Tanaka K, Shimotori T, Makino S, Aikawa Y, Inaba T, Yoshida C, Takano S
Research Laboratories, Toyama Chemical Co., Ltd., Japan.
Arzneimittelforschung. 1992 Jul;42(7):935-44.
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.
在多种动物模型中研究了3-甲酰氨基-7-甲基磺酰氨基-6-苯氧基-4H-1-苯并吡喃-4-酮（T-614，CAS 123663-49-0）的抗炎、镇痛和解热活性，并与尼美舒利、吲哚美辛和布洛芬进行了比较。T-614对角叉菜胶诱导的爪肿胀、纸片肉芽肿和已形成的佐剂性关节炎的抗炎效力大于布洛芬，但略低于尼美舒利和吲哚美辛。在急性炎症模型中，与吲哚美辛不同，T-614可抑制大鼠右旋糖酐和菠萝蛋白酶引起的肿胀，但其对豚鼠紫外线红斑的抑制作用较弱。虽然在小鼠扭体试验中几乎未显示出T-614的镇痛活性，但其对大鼠炎症性疼痛（如Randall-Selitto试验、佐剂诱导的痛觉过敏和抗原诱导的关节炎疼痛）的效力优于布洛芬。此外，它对犬尿酸盐诱导的滑膜炎有强效镇痛作用。T-614对酵母诱导的发热大鼠和脂多糖诱导的发热兔均有迅速而强烈的解热作用。T-614几乎没有胃肠道致溃疡作用，且不影响大鼠的水和钠排泄。T-614是一种新型抗炎化合物，其药理特性与参比药物不同。
