Imaizumi M, Miyazaki S, Watanabe Y, Machida H
Biology Laboratory, Research & Development Division, Yamasa Corp., Chiba, Japan.
Arzneimittelforschung. 1994 Mar;44(3):285-8.
The newly synthesized compound, 1-amino-5-bromouracil (ABU, CAS 127984-93-4), showed unique anxiolytic activity in rats and mice. Its minimum effective dose was 10 mg/kg p.o. in the Geller type conflict test in rats, and it showed anxiolytic activity at a dose of 20 mg/kg i.p. in the Vogel type conflict test in mice. ABU also induced loss of the righting reflex in mice. The ED50, a dose level that induces loss of the righting reflex in 50% of mice, was 86.4 mg/kg p.o. On the other hand, ABU showed only weak activities both potentiating the drug-induced anesthesia and myorelaxing in comparison with diazepam. Furthermore ABU did not show an affinity for benzodiazepine receptor. Thus, the pharmacological profile of ABU is concluded to be different from that of diazepam.
新合成的化合物1-氨基-5-溴尿嘧啶(ABU,CAS 127984-93-4)在大鼠和小鼠中表现出独特的抗焦虑活性。在大鼠的盖勒型冲突试验中,其口服最小有效剂量为10mg/kg,在小鼠的沃格尔型冲突试验中,腹腔注射20mg/kg剂量时显示出抗焦虑活性。ABU还可诱导小鼠翻正反射消失。使50%的小鼠翻正反射消失的半数有效剂量(ED50)口服为86.4mg/kg。另一方面,与地西泮相比,ABU在增强药物诱导的麻醉和肌松方面仅表现出微弱活性。此外,ABU对苯二氮䓬受体没有亲和力。因此,得出ABU的药理特性与地西泮不同的结论。