目的探讨血浆和肽素及精氨加压素受体(AVPR)基因多态性对脑出血后脑梗死的预测价值。方法选择147例基底核脑出血患者为研究对象,检测血浆和肽素浓度及AVPR基因多态性。根据4周后头颅MRI结果分为再发脑梗死组55例和未发脑梗死组92例,比...目的探讨血浆和肽素及精氨加压素受体(AVPR)基因多态性对脑出血后脑梗死的预测价值。方法选择147例基底核脑出血患者为研究对象,检测血浆和肽素浓度及AVPR基因多态性。根据4周后头颅MRI结果分为再发脑梗死组55例和未发脑梗死组92例,比较两组患者临床资料、血浆和肽素浓度及AVPR基因多态性,采用logistic回归分析影响脑出血后脑梗死的因素,并进行logistic回归模型拟合能力分析及最佳临界点的确定。结果两组患者临床资料的差异均无统计学意义(均P>0.05)。再发脑梗死组血浆和肽素浓度高于未发脑梗死组(P<0.05),A等位基因频率及AA基因型分布频率亦高于未发脑梗死组(均P<0.05)。经ROC曲线分析,血浆和肽素AUC为0.746,灵敏度为63.0%,特异度为82.8%,最大约登指数为0.458;log is tic回归模型拟合能力AUC为0.921,灵敏度为83.4%,特异度为88.3%,最大约登指数为0.717。结论脑出血后脑梗死发生与血浆和肽素及AVPR基因多态性有关,和肽素-AVPR基因模型对脑出血后脑梗死有一定的预测价值。展开更多
Series of novel derivatives of desloratadine designed as arginine vasopressin receptor antagonists were synthesized and structurally characterized by melting points,^1H NMR and HRMS.Their in vivo diuretic activities w...Series of novel derivatives of desloratadine designed as arginine vasopressin receptor antagonists were synthesized and structurally characterized by melting points,^1H NMR and HRMS.Their in vivo diuretic activities were evaluated on rats,and several target compounds showed promising diuretic results, especially compounds 8,18,27 and 31.Further in vitro bonding assay and cAMP assay showed that these compounds had a higher affinity to vasopressin V2 receptor than VI a receptor.Our studies indicated that desloratadine may be an active substructure for novel arginine vasopressin receptor antagonist development.展开更多
Women with nocturia are more sensitive to desmopressin, a synthetic arginine vasopressin (AVP) analogue, with significant antidiuretic responses to desmopressin orally disintegrating tablet (ODT) 25 μg, compared with...Women with nocturia are more sensitive to desmopressin, a synthetic arginine vasopressin (AVP) analogue, with significant antidiuretic responses to desmopressin orally disintegrating tablet (ODT) 25 μg, compared with men who require 58 μg to achieve similar responses. In children the current desmopressin dose recommendation to treat primary nocturnal enuresis (PNE) is the same for boys and girls. This post hoc analysis of data from a randomised, doubleblind single-dose study of 84 children with PNE aged 6 - 12 years explored gender differences in sensitivity to desmopressin in children. Following water loading to suppress endogenous AVP, placebo or desmopres-sin 30, 60, 120, 240, 360 or 480 μg was administered when urinary production reached >0.13 mL/min/kg. The endpoints of urinary osmolality and duration of urinary-concentrating action (DOA) (above three thresholds: 125, 200 and 400 mOsm/kg) were analysed to compare efficacy in boys and girls, in each treatment group. The DOA and urinary osmolality were similar in both genders in the desmopressin 120 - 480 μg groups. Boys receiving desmopressin ODT 30 - 60 μg tended to increased urinary osmolality and experienced 1 - 2 hours longer DOA than girls. The same pattern of higher values in boys compared with girls was seen for all measures of urinary osmolality. Conclusion: In a limited sample of pre-pubertal children the antidiuretic response to desmopressin was largely similar between genders, in contrast to findings in adults.展开更多
文摘目的探讨血浆和肽素及精氨加压素受体(AVPR)基因多态性对脑出血后脑梗死的预测价值。方法选择147例基底核脑出血患者为研究对象,检测血浆和肽素浓度及AVPR基因多态性。根据4周后头颅MRI结果分为再发脑梗死组55例和未发脑梗死组92例,比较两组患者临床资料、血浆和肽素浓度及AVPR基因多态性,采用logistic回归分析影响脑出血后脑梗死的因素,并进行logistic回归模型拟合能力分析及最佳临界点的确定。结果两组患者临床资料的差异均无统计学意义(均P>0.05)。再发脑梗死组血浆和肽素浓度高于未发脑梗死组(P<0.05),A等位基因频率及AA基因型分布频率亦高于未发脑梗死组(均P<0.05)。经ROC曲线分析,血浆和肽素AUC为0.746,灵敏度为63.0%,特异度为82.8%,最大约登指数为0.458;log is tic回归模型拟合能力AUC为0.921,灵敏度为83.4%,特异度为88.3%,最大约登指数为0.717。结论脑出血后脑梗死发生与血浆和肽素及AVPR基因多态性有关,和肽素-AVPR基因模型对脑出血后脑梗死有一定的预测价值。
基金project was supported by National 973 Plan(Nos. 2010CB735602 and 2012CB724002)National Major Scientific and Technological Special Project for "Significant New Drugs Development"(No.2011ZX09401-009)
文摘Series of novel derivatives of desloratadine designed as arginine vasopressin receptor antagonists were synthesized and structurally characterized by melting points,^1H NMR and HRMS.Their in vivo diuretic activities were evaluated on rats,and several target compounds showed promising diuretic results, especially compounds 8,18,27 and 31.Further in vitro bonding assay and cAMP assay showed that these compounds had a higher affinity to vasopressin V2 receptor than VI a receptor.Our studies indicated that desloratadine may be an active substructure for novel arginine vasopressin receptor antagonist development.
文摘Women with nocturia are more sensitive to desmopressin, a synthetic arginine vasopressin (AVP) analogue, with significant antidiuretic responses to desmopressin orally disintegrating tablet (ODT) 25 μg, compared with men who require 58 μg to achieve similar responses. In children the current desmopressin dose recommendation to treat primary nocturnal enuresis (PNE) is the same for boys and girls. This post hoc analysis of data from a randomised, doubleblind single-dose study of 84 children with PNE aged 6 - 12 years explored gender differences in sensitivity to desmopressin in children. Following water loading to suppress endogenous AVP, placebo or desmopres-sin 30, 60, 120, 240, 360 or 480 μg was administered when urinary production reached >0.13 mL/min/kg. The endpoints of urinary osmolality and duration of urinary-concentrating action (DOA) (above three thresholds: 125, 200 and 400 mOsm/kg) were analysed to compare efficacy in boys and girls, in each treatment group. The DOA and urinary osmolality were similar in both genders in the desmopressin 120 - 480 μg groups. Boys receiving desmopressin ODT 30 - 60 μg tended to increased urinary osmolality and experienced 1 - 2 hours longer DOA than girls. The same pattern of higher values in boys compared with girls was seen for all measures of urinary osmolality. Conclusion: In a limited sample of pre-pubertal children the antidiuretic response to desmopressin was largely similar between genders, in contrast to findings in adults.
