Błaszczyk B, Giełdanowski J, Patkowski J, Kowalczyk-Bronisz S H
Arch Immunol Ther Exp (Warsz). 1979;27(6):749-63.
Preclinical pharmacological studies of two acridine derivatives, dihydrochloride N10-oxide 1-nitro-9-/3-dimethylaminopropylamino/-acridine (C-666) and dihydrochloride 1-nitro-9-[(2-dimethylamino)-1-methylethylamino]-acridine (C-829) are reported. Both compounds are characterized by biological activity, poor absorption from the gastrointestinal tract and local irritant action. Quality differences in an effect of both investigated acridine derivatives on the central nervous system were noted. C-666 proved to be deprived of the effect typical of the central component compounds while C-829 demonstrated mostly sedative activity. Clear dissociation in the effect of these both compounds was seen in in vitro experiments on isolated smooth muscle organs. C-666 acted spasmolytically on the motory action of intestine muscles while C-829 acted spastically. Both preparations had clearly hipotensic influence which can be due to the vascular effect and to their affinity with the intramyocardium transmitting system. Neither a distinctive effect on reproductivity of animals nor the teratogenic action were observed in the functional experiments.
报道了两种吖啶衍生物,即N10 - 氧化物二盐酸盐1 - 硝基 - 9 - [(3 - 二甲基氨基丙基)氨基] - 吖啶(C - 666)和二盐酸盐1 - 硝基 - 9 - [(2 - 二甲基氨基) - 1 - 甲基乙氨基] - 吖啶(C - 829)的临床前药理学研究。这两种化合物的特点是具有生物活性、胃肠道吸收差和局部刺激作用。注意到两种被研究的吖啶衍生物对中枢神经系统作用的质量差异。事实证明,C - 666不具有典型的中枢成分化合物的作用,而C - 829主要表现出镇静活性。在对离体平滑肌器官的体外实验中,可以看到这两种化合物作用的明显差异。C - 666对肠道肌肉的运动作用起解痉作用,而C - 829起痉挛作用。两种制剂都有明显的降压作用,这可能归因于血管效应以及它们与心肌内传导系统的亲和力。在功能实验中,未观察到对动物生殖力的显著影响或致畸作用。