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新型抗炎/镇痛药F-776(5-(4-氯苯基)-β-羟基-2-呋喃丙酸)的评估

Evaluation of a new anti-inflammatory/analgesic compound F-776, 5-(4-chlorophenyl)-beta-hydroxy-2-furanpropanoic acid.

作者信息

Goldenberg M M, Boise K L, Ilse A C

出版信息

Arch Int Pharmacodyn Ther. 1980 Feb;243(2):331-50.

PMID:6966489
Abstract

F-776, 5-(4-chlorophenyl)-beta-hydroxy-2-furanpropanoic acid, is a nonsteroidal anti-inflammatory, analgesic, and antipyretic drug which does not produce stomach ulcers. It's spectrum of activity includes full anti-inflammatory efficacy in bilaterally adrenalectomized rats; and ED50 value in the carrageenin hindpaw edema assay comparable to that of fenoprofen and ibuprofen; effectiveness in preventing and in diminishing developing and established adjuvant-induced polyarthritis in rats, respectively; significant reduction of granulation tissue formation around cotton pellets; significant decrease in erythema resulting from ultraviolet irradiation of guinea-pig skin; analgesia as determined in the rat paw pressure procedure; antipyretic activity in rats with yeast-induced fever; and an uricosuric effect noted at higher than anti-inflammatory doses. F-776 is not an immunosuppressant as determined in the experimental allergic encephalomyelitis rat model. Its mechanism of action is as yet undetermined. In conclusion, F-776 represents a new nonulcerogenic anti-inflammatory, analgesic, and antipyretic compound with potential utility in different arthritic conditions.

摘要

F - 776,即5 -(4 - 氯苯基)-β-羟基-2 - 呋喃丙酸,是一种不会引发胃溃疡的非甾体抗炎、镇痛和解热药物。其活性谱包括:对双侧肾上腺切除的大鼠具有完全的抗炎功效;在角叉菜胶致后爪水肿试验中的半数有效量(ED50)与非诺洛芬和布洛芬相当;分别对预防和减轻大鼠佐剂性关节炎的发展和已形成的病症有效;显著减少棉球周围肉芽组织的形成;显著减轻豚鼠皮肤紫外线照射引起的红斑;在大鼠 paw 压力试验中测定有镇痛作用;对酵母诱导发热的大鼠有解热活性;在高于抗炎剂量时具有促尿酸尿作用。在实验性变应性脑脊髓炎大鼠模型中确定F - 776不是免疫抑制剂。其作用机制尚未确定。总之,F - 776是一种新型的无溃疡形成作用的抗炎、镇痛和解热化合物,在不同的关节炎病症中具有潜在应用价值。

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