Atkinson E R, Bullock F J, Granchelli F E, Archer S, Rosenberg F J, Teiger D G, Nachod F C
J Med Chem. 1975 Oct;18(10):1000-3. doi: 10.1021/jm00244a010.
Norapomorphine and ten of its N-substituted derivatives were prepared by modifications of procedures described earlier. In a dog emesis test the N-ethyl and N-n-propyl compounds had minimum effective doses of 0.00025 and 0.0005 mg/kg, respectively, when administered iv, sc, or im. In a modified Irwin mouse profile screen the minimum effective iv dose was 0.013 mg/kg for the N-ethyl and 0.0024 mg/kg for the N-n-propyl compound; percutaneous absorption was also observed in mice. All compounds examined caused the stereotyped apomorphine behavior syndrome but hypotensive effects were not serious.
通过改进先前所述的方法制备了去甲阿扑吗啡及其十种N-取代衍生物。在犬催吐试验中，N-乙基和N-正丙基化合物静脉注射、皮下注射或肌肉注射时的最小有效剂量分别为0.00025和0.0005 mg/kg。在改良的欧文小鼠综合筛选试验中，N-乙基化合物的最小有效静脉注射剂量为0.013 mg/kg，N-正丙基化合物为0.0024 mg/kg；在小鼠中也观察到了经皮吸收。所有检测的化合物均引起典型的阿扑吗啡行为综合征，但降压作用不严重。
