Bluth R
Pharmazie. 1981 Oct;36(10):698-702.
The author determined the distribution coefficients (in n-octanol/water) and the RM values (thin-layer chromatographically, using two solvent systems) of 17 newly synthetized pyridazines. These determinations evidenced that the majority of these compounds are relatively polar. Altogether the acute toxicity of the compounds under investigation may be regarded as weak, because LD50 values could be determined for only 10 of the orally applied 17 pyridazines. The characteristic features of acute toxicity caused by high doses of the compounds under investigation were a stimulation of the central nervous system associated with convulsions or a depressant action on the central nervous system. The screening tests performed to date do not permit to classify the compounds under investigation into defined groups of substances action on the central nervous system. In conjunction with data from the literature, the possible mechanisms of the attack of these novel pyridazines on the central nervous system are discussed.
作者测定了17种新合成哒嗪类化合物的分配系数(正辛醇/水体系中)以及Rf值(采用两种溶剂系统进行薄层色谱分析)。这些测定结果表明,这些化合物大多具有相对较高的极性。总体而言,所研究化合物的急性毒性较弱,因为在经口给予的17种哒嗪类化合物中,仅能测定出10种的半数致死量(LD50)值。高剂量所研究化合物引起的急性毒性的特征表现为伴有惊厥的中枢神经系统兴奋作用或对中枢神经系统的抑制作用。迄今为止所进行的筛选试验尚无法将所研究化合物归类为对中枢神经系统有明确作用类型的物质。结合文献数据,讨论了这些新型哒嗪类化合物作用于中枢神经系统的可能机制。