Giudice A, Herbert J M, Maffrand J P, Manara L, Manzoni L, Le Fur G
Arzneimittelforschung. 1996 Apr;46(4):407-12.
SR 27417 (CAS 136468-36-5, N-(2-dimethylaminoethyl)-N-(3-pyridinylmethyl)[4-(2,4,6-triisop ropylphenyl) thiazol-2-yl]amine), a highly potent platelet-activating factor (PAF) receptor antagonist, was tested for its ability to prevent macroscopic and histologically assessed gastrointestinal (GI) lesions in rats induced by PAF as compared to the reference compound apafant. Both compounds were orally effective but SR 27417 prevented the gut lesioning effects of PAF at lower doses than apafant. In addition, a dose of apafant (1.5 mg/kg) that showed almost maximal effect when given 30 min before PAF, had lost most of its protective action by 3 h, while SR 27417 at a comparably effective dose (0.5 mg/kg) retained substantial ability to prevent gut lesions in all the GI tract segments investigated, 18 h after administration. These findings suggest that SR 27417 is a potent and long lasting inhibitor of PAF-induced gastrointestinal lesions in rats.
SR 27417（化学物质登记号136468-36-5，N-（2-二甲基氨基乙基）-N-（3-吡啶基甲基）[4-（2,4,6-三异丙基苯基）噻唑-2-基]胺）是一种高效的血小板活化因子（PAF）受体拮抗剂，与参比化合物阿帕泛相比，对其预防PAF诱导的大鼠宏观和组织学评估的胃肠道（GI）损伤的能力进行了测试。两种化合物口服均有效，但SR 27417在比阿帕泛更低的剂量下就能预防PAF的肠道损伤作用。此外，阿帕泛剂量为1.5mg/kg，在PAF给药前30分钟给予时显示出几乎最大的效果，但到3小时时其大部分保护作用已经丧失，而SR 27417在同等有效剂量（0.5mg/kg）下，给药18小时后在所有研究的胃肠道段中仍保留有预防肠道损伤的显著能力。这些研究结果表明，SR 27417是一种对PAF诱导的大鼠胃肠道损伤有效的长效抑制剂。
