Brooks R R, Miller K E, Pelosi S S, Pong S F, Anthony D R, Goldenberg M M
Norwich Eaton Pharmaceuticals, Inc., a Procter & Gamble Company, Norwich, NY.
Arzneimittelforschung. 1988 Jan;38(1):59-65.
5-[5-(4-Chlorophenyl-2-furanyl)]dihydro-2(3H)-furanone (F-1044), a nonsteroidal antiinflammatory drug related to orpanoxin, lacks the usual acid moiety of such agents. F-1044 had antiinflammatory activity equivalent to ibuprofen's and orpanoxin's in the carrageenin-induced paw edema model in normal and adrenalectomized rats. Antiinflammatory activity was also expressed in the guinea pig UV-induced erythema and rat established arthritis models. F-1044 was a more potent analgesic than ibuprofen and orpanoxin in the rat paw pressure assay. In contrast to the reference agents, F-1044 raised the pain threshold of both the yeast-injected and non-injected paws, suggesting a central component to its analgesic action. F-1044 was more potent than ibuprofen and orpanoxin in the rat brewer's yeast pyresis model. Based on its low activity in inhibiting bradykinin-induced bronchoconstriction in guinea pigs and low gastric irritation activity in rats. F-1044 appears to have a mechanisms of action that involves more than simple inhibition of prostaglandin synthesis. Thus F-1044 is a nonsteroidal antiinflammatory agent with unique chemical and pharmacological features.
5-[5-(4-氯苯基-2-呋喃基)]二氢-2(3H)-呋喃酮（F-1044）是一种与奥帕诺辛相关的非甾体抗炎药，缺乏此类药物常见的酸性部分。在正常和肾上腺切除的大鼠角叉菜胶诱导的足爪水肿模型中，F-1044具有与布洛芬和奥帕诺辛相当的抗炎活性。在豚鼠紫外线诱导的红斑和大鼠实验性关节炎模型中也表现出抗炎活性。在大鼠足爪压力试验中，F-1044是比布洛芬和奥帕诺辛更强效的镇痛药。与参比药物不同，F-1044提高了注射酵母和未注射酵母的足爪的痛阈，表明其镇痛作用有中枢成分。在大鼠啤酒酵母发热模型中，F-1044比布洛芬和奥帕诺辛更有效。基于其在豚鼠中抑制缓激肽诱导的支气管收缩的低活性以及在大鼠中的低胃刺激活性，F-1044似乎具有不止简单抑制前列腺素合成的作用机制。因此，F-1044是一种具有独特化学和药理学特性的非甾体抗炎药。
