Sakuma Y, Muramoto K, Harada K, Katayama S, Tsunoda H, Katayama K
Tsukuba Research Lab., Eisai Co., Ltd., Ibaraki, Japan.
Prostaglandins. 1991 Dec;42(6):541-55. doi: 10.1016/0090-6980(91)90016-9.
The effects of the platelet-activating factor (PAF) antagonist, E6123, on anaphylactic responses in guinea pigs and mice were investigated. E6123 inhibited i.v. antigen (Ag)- or inhaled Ag-induced bronchoconstriction in passively and actively sensitized guinea pigs after oral administration at 3 and 10 micrograms/kg, respectively. E6123 inhibited Ag inhalation-induced airway hyperreactivity in guinea pigs after oral administration at 30 micrograms/kg. E6123 protected mice from anaphylactic death with an ED50 value (p.o.) of 7 micrograms/kg. The inhibitory effects of E6123 described above were very potent compared to those of the PAF-antagonists WEB2347 and Y-24180. The present results suggest that E6123 may be beneficial for the treatment of asthma, a condition in which PAF is assumed to be involved.
研究了血小板活化因子（PAF）拮抗剂E6123对豚鼠和小鼠过敏反应的影响。E6123分别以3微克/千克和10微克/千克的剂量口服给药后，可抑制被动和主动致敏豚鼠静脉注射抗原（Ag）或吸入Ag诱导的支气管收缩。E6123以30微克/千克的剂量口服给药后，可抑制豚鼠吸入Ag诱导的气道高反应性。E6123可保护小鼠免于过敏性死亡，其口服半数有效剂量（ED50）为7微克/千克。与PAF拮抗剂WEB2347和Y-24180相比，上述E6123的抑制作用非常显著。目前的结果表明，E6123可能对治疗哮喘有益，因为哮喘被认为与PAF有关。
