间硝苯地平在麻醉兔体内的药动学和药效学

麻醉兔静脉注射间硝苯地平后，观察其药动学和药效学。其药物动力学符合二室开放模型。收缩压与舒张压的下降程度均与血药浓度呈显著正相关，而心率的变化却与血药浓度并不显著相关。     

ACTIONS OF THE SLOW CHANNEL ACTIVATOR, BAY-K-8644, ON THE ELECTRICAL ACTIVITY OF 3-DAY-OLD EMBRYONIC CHICK HEARTS

In order to assess the effects of Bay-K-8644 on electrical activities of young embryonic chick hearts in which the rising phase of the action potential (AP) depends on tetrodotoxin-insensitive slow Na+ currents, slow AP were recorded in spontaneously beating 3-day-old embryonic chick hearts. Bay-K-8644(10(-6) mol/l) caused increases in the maximum rate of rise, amplitude, and duration of the slow AP; there was a slow increase in the spontaneous firing rate. Thus, Bay-K-8644 stimulates Na+ influx through TTX-insensitive slow channels.     

Neuronal differentiation of Ca channel by nerve growth factor

The inhibitory effect of nicardipine, a potent Ca²⁺ channel blocker in muscular cells, on the Ca²⁺ channel of clonal rat pheochromocytoma cells (PC12h) and cultured rat adrenal medullary cells was studied during the neuronal differentiation mediated by nerve growth factor (NGF). Nicardipine at nM-order concentrations suppressed the high-K⁺-evoked, Ca²-dependent release of preloaded [³H]norepinephrine from PC12h cells and adrenal medullary cells, whereas it scarcely inhibited the release from the cultured rat brainstem cells. The inhibitory actions of nicardipine on both PC12h and newborn rat adrenal medullary cells were significantly decreased after these cells were cultured in the presence of NGF. These results suggest that the changes in Ca²⁺ channel are accompanied by the neuronal differentiation mediated by NGF.     

气相色谱法测定右旋棉酚衍生物的含量

目的:建立右旋棉酚衍生物含量测定的气相色谱法。方法:采用气相色谱内标法,色谱柱为5%Phenyl Methyl Siloxane毛细管柱,氢火焰离子化检测器,载气为氮气,程序升温:初始温度为200℃,保持2min,然后以20℃·min-1的速度上升到240℃,保持3min;甲硝唑为内标,以内标法计算右旋棉酚衍生物的含量。结果:右旋棉酚衍生物检测浓度线性范围为80.06～480.36μg·mL-(1R2=0.9994),平均加样回收率为96.67%,RSD=1.4%。结论:该法灵敏、简便、快速,适用于右旋棉酚衍生物的含量测定。     

Dendritic calcium channels and hippocampal long-term depression

The authors examine the potential role of the different sources of dendritic Ca²⁺ influx in long-term depression (LTD) of synaptic efficacy. Recent data on the location and functional distribution of voltage-gated Ca²⁺ channels obtained from fluorescence imaging and patch clamp experiments are presented. This is followed by a discussion of the existing evidence for different sources of Ca²⁺ playing a role in the induction of LTD. The authors conclude that a number of key issues need to be resolved before any conclusions are drawn as to the involvement of any specific route of Ca²⁺ entry in LTD. © 1996 Wiley-Liss, Inc.     

Medication compliance and clinical outcomes of fixed‐dose combinations vs free combinations of an angiotensin II receptor blocker and a calcium channel blocker in hypertension treatment

Using the National Health Insurance Research Database of Taiwan, the authors identified 1136 patients taking fixed‐dose combination and 4544 patients taking free combinations of an angiotensin II receptor blocker and a dihydropyridine calcium channel blocker from January 2009 to December 2012. At a mean follow‐up of 2.1 years, the fixed‐dose combination was associated with improved medication adherence and persistence and better survival free from major adverse cardiac events and hospitalization for heart failure compared with the free combination regimens.     

新型二氢吡啶类化合物的合成及其抗乙型肝炎病毒活性研究

目的合成全新的二氢吡啶类化合物,并对其抗乙型肝炎病毒（HBV）复制活性进行研究,以获得新型的抗病毒药物先导物。方法以芳杂环取代的二氢嘧啶类化合物为模板,通过比较分子场分析,设计全新的二氢吡啶类化合物。以乙酰乙酸乙酯,芳香酸为起始原料,分别经胺化、烷基化反应,再与芳香醛缩合关环得到最终目标化合物,并对其体外抑制HBV的活性进行试验。结果合成了未见文献报道的全新二氢吡啶类化合物13个,经1HNMR和MS确定了结构,部分化合物显示了对HBV DNA复制的抑制作用。化合物6f表现出较强的抑制病毒复制活性,体外活性优于阳性对照药拉米夫定。结论二氢吡啶类化合物做为一类全新结构的抗HBV化合物,值得进行深入研究。     

Ge—132衍生物合成、结构及生物活性研究(Ⅱ)

合成了3种未见报导的有机锗倍半氧化物—β—酚酯基乙基锗倍半氧化物,用多种现代分析方法证实了它们的组成和结构。体外细胞培养实验结果表明,3 el 种化合物对Ha 细胞分裂有明显的抑制作用,对二倍体细胞分裂基本无影响,并发现不同芳基的Ge—132衍生物对Hela 细胞分裂的抑制作用不同,说明不仅有机锗倍半氧化物中的—Ge—(?)部分而且芳基取代基团也参与一定的生物作用。