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作者企图在呱啶的季铵化衍生物中筛选具有强效解痉作用、而扩瞳及流涎等付反应很弱的药物。一系列药理实验表明,SA-504是一个强效抗胆碱药,有希望符合这方面的要求。体外试验证明,其抑制烟碱或钡盐引起的豚鼠回肠收缩作用与阿托品相似。二者对抗烟碱的痉挛作用,在低剂量时均为竞争性,在高剂量时则均为非竞争性。SA-504和阿托品的抗烟碱和抗乙酰甲胆碱效力的比值分别为1/5.5和1/5.4。二者如此相近,提示它们还有直接对抗烟碱的作用,而主要是抗毒
The authors attempt to screen the quaternized derivatives of piperidine with potent antispasmodic drugs, while drugs such as dilated pupils and drooling are very weak. A series of pharmacological experiments show that, SA-504 is a potent anticholinergic, hopefully meet the requirements in this area. In vitro experiments show that its inhibition of nicotine or barium salt caused by contraction of guinea pig ileum and atropine similar. The anticonvulsant effect of both against nicotine is competitive at low doses and noncompetitive at high doses. The ratio of anti-nicotine and anti-methacholine potency to SA-504 and atropine was 1 / 5.5 and 1 / 5.4, respectively. The two are similar, suggesting that they also have a direct anti-nicotine effect, but mainly anti-drug