Moretti V, Concettoni C, Giusti P, Re L
Institute of Experimental and Clinical Medicine, University of Ancona, Italy.
Pharmacol Res. 1989 Mar-Apr;21(2):223-9. doi: 10.1016/1043-6618(89)90241-7.
Zipeprol, a piperazine ethanol derivative, is a non-essential but widely used (paediatric) antitussive, which is not legally considered as being capable of creating dependence or abuse liability. A first group of experimental results was obtained assaying the displacement of 1 nM [3H]naloxone by zipeprol vs morphine on the rat brain homogenate fractions. A second group was carried out on the longitudinal muscle of guinea-pig ileum, using the field stimulation technique, either in the absence or in the presence of naloxone 1 x 10(-5)M or in the absence or in the presence of yohimbine 1 x 10(-5)M. Further investigations concerning the pharmacological and the biochemical characterization of the mechanisms involved in abuse liability were carried out by means of the in vitro inhibition of ACh response on the guinea-pig ileum preparation. The results indicate zipeprol as a moderate opioid agonist, which also shows a direct anticholinergic effect, independent of presynaptic alpha 2 interaction.
齐哌丙醇是一种哌嗪乙醇衍生物，是一种非必需但广泛使用的（儿科）镇咳药，法律上不认为其具有产生依赖性或滥用倾向。通过测定齐哌丙醇与吗啡对大鼠脑匀浆组分中1 nM [³H]纳洛酮的置换作用，获得了第一组实验结果。第二组实验在豚鼠回肠纵肌上进行，采用场刺激技术，分别在不存在或存在1×10⁻⁵M纳洛酮的情况下，以及在不存在或存在1×10⁻⁵M育亨宾的情况下进行。通过体外抑制豚鼠回肠制剂中乙酰胆碱反应，进一步研究了与滥用倾向相关机制的药理学和生化特性。结果表明齐哌丙醇是一种中度阿片类激动剂，它还表现出直接的抗胆碱能作用，与突触前α₂相互作用无关。
