去甲乌药碱的药理作用与心脏β－AR关系的初步研究

附子有效成分去甲乌药碱（ＤＭＣ）的药理作用以及与肾上腺素能β受体（β－ＡＲ）的关系的研究表明，０．５ｍｇ·ｋｇ－１的ＤＭＣ可使正常小鼠心肌β－ＡＲ轻度上调，与异丙肾上腺素（ＩＳＯ）相比，ＤＭＣ能轻度激动ｃＡＭＰ，使其血浆含量升高，升高的峰值时间在１０ｍｉｎ左右。ＤＭＣ的最小激动量为０．５ｍｇ·ｋｇ－１，最大激动量为５ｍｇ·ｋｇ－１。ＤＭＣ对１２５Ｉ－ＰＩＮ的竞争抑制实验表明，在１×１０－６～１×１０－５ｍｏｌ·Ｌ－１时，ＤＭＣ可抑制１２５Ｉ－ＰＩＮ与β－ＡＲ结合，与心得安比较抑制浓度大４～５个数量级。与ＩＳＯ合并用药观察血浆ｃＡＭＰ浓度变化提示，０．５ｍｇ·ｋｇ－１ＤＭＣ与小剂量（０．１ｍｇ·ｋｇ－１）和较大剂量（１ｍｇ·ｋｇ－１）的ＩＳＯ合用时，既无协同作用，也未见拮抗作用。

吲哚洛尔对帕罗西汀治疗抑郁症显效时间的影响

目的 :观察吲哚洛尔对帕罗西汀治疗抑郁症显效时间的影响。方法 :将符合CCMD Ⅱ R抑郁症诊断标准的患者 3 6例随机分为治疗组和对照组 ,分别予吲哚洛尔及安慰药联用帕罗西汀 ,采用汉密尔顿抑郁量表 (HAMD)、临床疗效总评量表 (CGI)及副作用量表 (TESS)评定。结果 :第 1,第 2周末治疗组减分率明显高于对照组 ,差异有显著性 (P<0 .0 5 ) ;两组总有效率及副作用相当 (P >0 .0 5 )。 结论 :吲哚洛尔能缩短帕罗西汀的显效时间。

^(125)Ⅰ-左旋吲哚洛尔的质量控制及其比活度的衰变校正

从方法学角度完善１２５Ⅰ－ＰＩＮ标记物制备的质量控制。共制备１５批１２５Ⅰ－ＰＩＮ 标记物。放化纯度为９０±４．２％，标记率４３．９±１４．９％。每批标记物均用小鼠肺或脑作饱和实 验，了解标记物情况。对１２５Ⅰ－ＰＩＮ放化纯度动态跟踪表明，１２５Ⅰ－ＰＩＮ标记物的有效期可达两 个半衰期。同时从理论和实验上探讨有载体和无载体Ｎａ１２５Ⅰ标记配基比活度的校正方法。

手性固定相反相高效液相色谱法拆分吲哚洛尔对映体

采用新型商品反相手性色谱柱Chiral PAKR AD-RH,建立了β-受体阻滞剂类药物吲哚洛尔的手性拆分方法.考察了流动相组成、pH、柱温、流速及缓冲盐浓度对吲哚洛尔手性拆分的影响.通过优化实验条件,吲哚洛尔达到基线分离,可用于常规分析.在此基础上,进一步考察了制备条件,取得了满意的结果.

Autoradiographic Analysis of β-Adrenoceptors in Endomyocardial Biopsy Samples

We have studied the [125I] Pindolol ([125I]-PIN) binding to β-adrenergic receptors on endomyocardial biopsy samples through autoradiographic analysis. Minusculc amount of human endomyocardial tissues Was sectioned and incubated in [125I]-PIN, emulsion-coatcd covcrslips Were attached to the slides and then developed, fixed and staincd after exposure. The grain density was quantified using a computer image analyzer.The autoradiograms demonstrated the sites of cardiac β-receptorbinding with clear grains, and the non-specific binding was below 10%-20%' of the total binding. Linearregression analysis for the plot of specific cpm against specific grains at each concentration of [125I]-PINgave ay value of 0.99. Using this technique, we identified down-regulation of cardiac β-receptors inpatients with dilated cardiomyopathy (DCM) as compared with that of normal human subjects.

Protective Effects of Berberine on Cerebral Ischemia in Mice and Rats

We have studied the [125I] Pindolol ([125I]-PIN) binding to β-adrenergic receptors on endomyocardial biopsy samples through autoradiographic analysis. Minusculc amount of human endomyocardial tissues Was sectioned and incubated in [125I]-PIN, emulsion-coatcd covcrslips Were attached to the slides and then developed, fixed and staincd after exposure. The grain density was quantified using a computer image analyzer.The autoradiograms demonstrated the sites of cardiac β-receptorbinding with clear grains, and the non-specific binding was below 10%-20%' of the total binding. Linearregression analysis for the plot of specific cpm against specific grains at each concentration of [125I]-PINgave ay value of 0.99. Using this technique, we identified down-regulation of cardiac β-receptors inpatients with dilated cardiomyopathy (DCM) as compared with that of normal human subjects.

The Presence of Phases and the Inability of the Classical Compartment Models to Provide Pharmacokinetic Parameters of Physiological Significance for Lipophilic Drugs

The first biphasic open one-compartment pharmacokinetic model is described. Its analytical solutions to drug concentration were developed from parameters of an open two-compartment pharmacokinetic model. The model is used to explain the unusually large compartment volumes and apparent volumes of distribution of lipophilic drugs, as well as to identify which of the pharmacokinetic parameters of the classical compartment models are biologically relevant.

β－阻断剂及其代谢产物的气相色谱分析研究 Ⅱ．GC／MS分析卡替洛尔、吲哚洛尔、噻吗洛尔及其代谢产物

本文用ＧＣ／ＭＳ法研究了国际奥委会药物禁用表中新增药卡替洛尔、吲哚洛尔及噻吗洛尔，从人尿中检出了药物原型及数种代谢产物，讨论了衍生化方法及代谢情况并给出了回收率及检测限数据。