摘要
研究双环硫化磷酸酯类化合物在大鼠及家蝇神经节结合部位有抗GABA(γ-氨基丁酸)作用,并对其进行了放射性配体与大鼠及家蝇GABA受体的结合活性测定,研究其抑制活性和生物选择性.以2-苯基丙二酸二乙酯为原料,经酰化、还原及环合3步反应得到10个3-烃基-4-苯基双环笼状磷酸酯类化合物,所有化合物均通过1H NMR和MS进行了结构确认,采用放射性配体—受体结合试验,测定了10个化合物抑制[3H]EBOB(4'-乙炔基-4-正丙基原苯甲酸酯)与家蝇及大鼠GABA受体的结合活性,结果表明部分化合物在10-5mol/L具有较好的抑制活性,且在大鼠与家蝇GABA受体之间有一定的选择性.
The anti-γ-aminobutyric acid（GABA）effects of the bicyclophosphorothionate compounds on theganglion sites of rats and houseflies were explored,and the binding activities between the radioligands andGABA receptor were tested to study the inhibitory activities and biological selectivity of the bicyclophosphorothi-onate compounds.Ten 3-hydroxy-4-phenyl-bicyclophosphate compounds were synthesized by using 2-phenyl-diethylmalonate as a starting material via acylation,reduction and cyclization,and their structures were deter-mined by1 H nuclear magnetic resonance spectrocopy and mass spectrometry.In addition,the radioligand bind-ing assay was performed to evaluate the potencies of the bicyclophosphorothionate compounds to inhibit thebinding of[3H]ethynylbicycloorthobenzoate to GABA receptors of rats and houseflies,and the resultsshow that these compounds have relatively high binding activities and certain selectivity to GABA receptors ofrats and houseflies at the concentration of 10-5mol/L.
出处
《武汉工程大学学报》
CAS
2016年第4期319-323,共5页
Journal of Wuhan Institute of Technology
基金
国家自然科学基金资助项目(20572084)
