A series of new 2 (alkylthio) 5,7 dimethyl 1,2,4 triazolopyrimidines and 3 (alkylthio) 5,7 dimethyl 1,2,4 triazolopyrimidines have been synthesized. These derivatives were evaluated for inhibitory effects on...A series of new 2 (alkylthio) 5,7 dimethyl 1,2,4 triazolopyrimidines and 3 (alkylthio) 5,7 dimethyl 1,2,4 triazolopyrimidines have been synthesized. These derivatives were evaluated for inhibitory effects on 85 7 mmol·L 1 K + and 10 4 mmol·L -1 NE (nor epinephrine) induced contraction of rat aorta strips.展开更多
文摘A series of new 2 (alkylthio) 5,7 dimethyl 1,2,4 triazolopyrimidines and 3 (alkylthio) 5,7 dimethyl 1,2,4 triazolopyrimidines have been synthesized. These derivatives were evaluated for inhibitory effects on 85 7 mmol·L 1 K + and 10 4 mmol·L -1 NE (nor epinephrine) induced contraction of rat aorta strips.
文摘利用荧光标记法及分子模拟法,研究了氟虫腈与昆虫γ-氨基丁酸(aminobutyric acid,GABA)受体的相互作用。荧光标记试验结果显示,氟虫腈与家蝇脑内GABA受体有较强的相互作用,其最大结合量[RT]值和亲和常数K_d值分别为(21.3±2.5)pmol/mg protein和(109±9)nmol/L。分子模拟结果显示:氟虫腈与果蝇RDL受体间形成3条氢键;两者之间的CDOCKER的相互作用能为–137.93 k J/mol。试验和理论两方面均证实,氟虫腈对昆虫GABA受体的强亲和性是导致氟虫腈对昆虫产生高毒性的重要原因。