分别观察了胰岛素抵抗和高血糖水平对己糖胺途径限速酶GFAT活性的影响.在alloxan高血糖小鼠模型中,与正常对照组比较,血清果糖胺水平升高了15.9%,肾组织GFAT活性升高了32.8%;经胰岛素治疗后,血清果糖胺水平降低了9.7%,其肾组织GFAT活性...分别观察了胰岛素抵抗和高血糖水平对己糖胺途径限速酶GFAT活性的影响.在alloxan高血糖小鼠模型中,与正常对照组比较,血清果糖胺水平升高了15.9%,肾组织GFAT活性升高了32.8%;经胰岛素治疗后,血清果糖胺水平降低了9.7%,其肾组织GFAT活性也降低了l9.4%.在高糖高脂饲料诱导的胰岛素抵抗的IR小鼠中,与同批正常对照组比较,正糖钳实验中稳态时葡萄糖输注率G IR值降低了69.3%,胰岛素耐量实验中的AUC值升高了38.1%,其肾脏组织GFAT活性也增加了26.6%.在胰岛素诱导的具有胰岛素抵抗的IR-H IR c细胞模型中,与正常H IR c细胞比较,其10、25 nmol/L胰岛素诱导的葡萄糖摄取能力分别降低了25.3%、21.1%,而GFAT活性分别增加了29.7%、46.5%.可见,GFAT活性与一段时间的平均血糖水平和胰岛素抵抗状态密切正相关.展开更多
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
A model of transmembrane helices of dopamine D2 receptor was constructed using the X ray coordinates of bacteriorhodopsin (BR) as a template. Based on the results from the model and the site directed mutagenesis exp...A model of transmembrane helices of dopamine D2 receptor was constructed using the X ray coordinates of bacteriorhodopsin (BR) as a template. Based on the results from the model and the site directed mutagenesis experience, the binding pocket, including nine amino acid residues beside indispensable Asp86, Ser141 and Ser144 residues, was defined. In order to testify the 3D structure of dopamine D2 receptor and specially test the binding sites, two sets of D2 receptor agonists (one was rigid and the other flexible) were selected for docking. A good result of correlation between logIC 50 and binding energy E b indicates that the predicted model is reliable for the investigation of the receptor ligand interaction and design of new active molecules.展开更多
文摘分别观察了胰岛素抵抗和高血糖水平对己糖胺途径限速酶GFAT活性的影响.在alloxan高血糖小鼠模型中,与正常对照组比较,血清果糖胺水平升高了15.9%,肾组织GFAT活性升高了32.8%;经胰岛素治疗后,血清果糖胺水平降低了9.7%,其肾组织GFAT活性也降低了l9.4%.在高糖高脂饲料诱导的胰岛素抵抗的IR小鼠中,与同批正常对照组比较,正糖钳实验中稳态时葡萄糖输注率G IR值降低了69.3%,胰岛素耐量实验中的AUC值升高了38.1%,其肾脏组织GFAT活性也增加了26.6%.在胰岛素诱导的具有胰岛素抵抗的IR-H IR c细胞模型中,与正常H IR c细胞比较,其10、25 nmol/L胰岛素诱导的葡萄糖摄取能力分别降低了25.3%、21.1%,而GFAT活性分别增加了29.7%、46.5%.可见,GFAT活性与一段时间的平均血糖水平和胰岛素抵抗状态密切正相关.
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A model of transmembrane helices of dopamine D2 receptor was constructed using the X ray coordinates of bacteriorhodopsin (BR) as a template. Based on the results from the model and the site directed mutagenesis experience, the binding pocket, including nine amino acid residues beside indispensable Asp86, Ser141 and Ser144 residues, was defined. In order to testify the 3D structure of dopamine D2 receptor and specially test the binding sites, two sets of D2 receptor agonists (one was rigid and the other flexible) were selected for docking. A good result of correlation between logIC 50 and binding energy E b indicates that the predicted model is reliable for the investigation of the receptor ligand interaction and design of new active molecules.
