Bluth R
Pharmazie. 1982 Apr;37(4):285-9.
Using four screening methods (writhing syndrome, electrical stimulation of the root of the tail, tail-flick test and hot-plate test), the author studied the analgetic activities of 3-amino-4-mercapto-6-methylpyridazine (1; pyridazine S1) and several standard pharmaca. When applied subcutaneously, 1 showed an activity that was almost equal to that of aminophenazone. When administered orally, the activity of 1 was comparable to that of phenylbutazone. Indometacin and aminophenazone were more potent than 1; and acetylsalicylic acid and phenacetin were less potent. The synergism of 1 and codeine is superadditive as demonstrated by means of the tail-flick test and the writhing syndrome. When applied orally, 1 and phenacetin have the lowest acute toxicity as evidenced by the LD50 values. Acetylsalicylic acid, indometacin, phenylbutazone and aminophenazone are more toxic. From the results obtained it follows that, of all the substances tested, 1 has the greatest therapeutic index.
作者采用扭体综合征、电刺激尾根、甩尾试验和热板试验这四种筛选方法,研究了3-氨基-4-巯基-6-甲基哒嗪(1;哒嗪S1)和几种标准药物的镇痛活性。皮下给药时,1的活性几乎与氨基比林相当。口服给药时,1的活性与保泰松相当。吲哚美辛和氨基比林比1更有效;而乙酰水杨酸和非那西丁的效力则较低。通过甩尾试验和扭体综合征证明,1与可待因的协同作用具有超加和性。口服给药时,根据半数致死量值证明,1和非那西丁的急性毒性最低。乙酰水杨酸、吲哚美辛、保泰松和氨基比林毒性更大。从所得结果可以看出,在所有测试物质中,1具有最大的治疗指数。