伪麻黄碱和麻黄三对离体豚鼠心房作用的机理研究

以麻黄碱作比较，研究伪麻黄碱对豚鼠离体左右心房的作用。结果伪麻黄碱（1－100umol/L）和麻黄碱（1－100umol/L）均剂量依赖性回快离体豚鼠右心房率，增强离体豚鼠左心房收缩力，作用分别受预 先给予普萘洛尔（0.1umol/L）和利血平化动物的 显著抑制；此外，麻黄碱对左心房的作用受预先给 酚妥拉明（10umol/L）抑制，而为伪麻黄碱的作用的作用均不受影响。     

伪麻黄碱与麻黄碱对豚鼠气管条的快速耐受作用

目的：研究交叉应用伪麻黄碱和麻黄碱后,豚鼠气管条的快速耐受作用。方法：采用豚鼠气管条离体实验,结果：两碱交叉应用后,其舒张豚鼠气管条的曲线上计算出的PD2值均显著减小（P＜0．05和P＜0．01）。结论：交叉应用伪麻黄碱与麻黄碱对豚鼠气管条产生快耐受性。     

小檗碱对大鼠肛尾肌多种受体的阻断作用

大鼠肛尾肌对苯福林,乙酰胆碱及5-羟色胺均可引起收缩,而异丙肾上腺素及组织胺则仅在高浓时才引起收缩,苯福林及乙酰胆碱所致的收缩反应可分别被小檗碱及阿托品所阻断,但后者的阻M受体及阻α受体所需剂量相差极大。小檗碱可使苯福林的量效曲线平行右移,最大反应不变,其pA_2值为6.4。阿托品可竞争性地阻断乙酰胆碱的作用,其pA_2值为8.7,小檗碱对乙酰胆碱量效曲线的影响与阿托品不同,属非竞争性拮抗,即使量效曲线右移,最大反应压低,其压低程度与小檗碱浓度成正比,其pD′~2值为4.6。     

小檗碱对大鼠肛尾肌多种受体的阻断作用

大鼠肛尾肌对苯福林,乙酰胆碱及5-羟色胺均可引起收缩,而异丙肾上腺素及组织胺则仅在高浓时才引起收缩,苯福林及乙酰胆碱所致的收缩反应可分别被小檗碱及阿托品所阻断,但后者的阻M受体及阻α受体所需剂量相差极大。小檗碱可使苯福林的量效曲线平行右移,最大反应不变,其pA₂值为6.4。阿托品可竞争性地阻断乙酰胆碱的作用,其pA₂值为8.7,小檗碱对乙酰胆碱量效曲线的影响与阿托品不同,属非竞争性拮抗,即使量效曲线右移,最大反应压低,其压低程度与小檗碱浓度成正比,其pD′²值为4.6。     

麻黄挥发油对麻黄碱和伪麻黄碱经Caco-2细胞转运特征的影响

摘要：目的:基于"性味药理"研究思路,选取麻黄挥发油和生物碱作为其辛温解表主要功效成分,从药物吸收转运角度研究麻黄解表发散的作用原理。方法:采用Caco-2细胞转运模型,HPLC同步对比分析麻黄挥发油加入对麻黄碱和伪麻黄碱从板顶端（AP）→底端（BL）及BL→AP的双向转运过程的影响,计算表观渗透系数,并分析挥发油对其转运特征的影响。结果:麻黄碱和伪麻黄碱的Caco-2细胞表观渗透系数(Papp)与浓度无显著关系。麻黄碱的Papp（AP→BL）约为19×10-6cm·s-1,伪麻黄碱的Papp（AP→BL）约为16×10-6cm·s-1,吸收作用均较好,外排率均值为0.72,推测其转运过程主要为被动转运过程。麻黄挥发油促进麻黄碱和伪麻黄碱的转运吸收,其对伪麻黄碱促进吸收作用更为显著。结论:挥发油和生物碱在麻黄解表发散功效可能存在协同作用。     

在毁脊髓大鼠和肛尾肌上甲基莲心碱对α_1受体激动剂作用的影响

甲基莲心碱(Nef)使甲氧胺(Met)升高毁脊髓大鼠血压的量效曲线平行右移,用大鼠肛尾肌标本、观察Nef的α_1受体阻断作用,发现Nef 1,10,30μmol9·L~(-1)和哌唑嗪(Pra)3,10,30 nmol·L~(-1)一样,使去氧肾上腺素(Phe)累积量效曲线平行右移,不明显压低最大反应,测得Nef的pA_2值为6.9,Nef对高钾去极化收缩的胆囊及Oddi括约肌有抑制作用,以对炎性标本作用为强,结果提示Nef能阻断x_1,受体,能松弛由高钾去极化收缩的胆道平滑肌。     

柱前荧光标记高效液相色谱法对血浆中ι－麻黄碱和d－伪麻黄碱的定量分析

ι－麻黄碱和ｄ－伪麻黄碱是生药麻黄中早为人知而至今仍被广泛用于临床的一对手性异构生物碱。由于二者为生药麻黄中的主要成分但药理活性不同，为便于临床监控及有效用药，高分辨高灵敏度的检测方法的开发迫在眉睫。本文以易于得到的ｄａｎｓｙｌｃｈｌｏｒｉｄｅ为柱前荧光标识试剂，在确定了最佳衍生化及分离条件的基础上，建立了理想的色谱分析系统（线性检测范围１～８００ｎｇ·ｍｌ－１）。同时运用此方法，完成了对静注ι－麻黄碱和ｄ－伪麻黄碱后豚鼠血浆内该对手性异构体水平的考查，并且定量检测了服用中成药小青龙合剂后人血浆中的该对手性异构体。     

性激素对体外子宫肌瘤细胞作用机理的实验研究

目的 :探讨性激素对子宫肌瘤细胞的作用机理。方法 :取活体子宫肌瘤组织进行细胞分离与原代培养至细胞汇合成片 ,分别加入不同浓度的雌二醇、睾酮 ,测定培养液中胰岛素样生长因子 -I(IGF -I)、胰岛素样生长因子结合蛋白 -3(IGFBP -3)的浓度 ,并与不加性激素组对照比较。结果 :对照组IGF -I、IGFBP -3分别为(344.25±52.18)μg/L和(9.22±0.33)μg/L ,雌二醇组为(292.25±15.65)μg/L和(8.28±0.46)μg/L ,睾酮组为(441.00±36.17)μg/L和(9.26±0.36)μg/L。与对照组相比 ,雌二醇抑制IGFBP -3的产生 (P<0.01) ;而睾酮则促进IGF -I的产生(P<0.01)。结论 :雌二醇抑制子宫肌瘤细胞产生IGFBP -3 ;而睾酮则促进IGF -I的产生 ,但对IGFBP -3的产生作用不明显     

RP-HPLC测定小儿麻甘冲剂水煎液中麻黄碱和伪麻黄碱的含量

目的:应用RP-HPLC检测了小儿麻甘冲剂水煎液中麻黄碱、伪麻黄碱的含量.方法:样品经超声提取,色谱柱用pherisorb CN,流动相用0.001 mol·L-1二丁胺磷酸水溶液(pH3.5),检测波长214 nm.结果:麻黄碱、伪麻黄碱浓度分别在20.32～325.12 μg·ml-1和6.88～110.0 μg·ml-1范围内线性良好,回收率分别为87.5%～89.8%和88.8%～90.2%.结论:该法可适用于含麻黄制剂中麻黄碱,伪麻黄碱的含量测定.     

EFFECTS OF HYDROXOCOBALAMIN AND HAEMOGLOBIN ON NO-MEDIATED RELAXATIONS IN THE RAT ANOCOCCYGEUS MUSCLE

1. The effects of hydroxocobalamin (Vitamin B_12a) on relaxations produced by nitric oxide (NO), some NO-donating compounds and nitrergic nerve stimulation in isolated preparations of the rat anococcygeus muscle were compared with the effects of haemoglobin. 2. Hydroxocobalamin (30 μmol/L) significantly reduced relaxations induced by NO (0.1–3 μmol/L) and sodium nitroprusside (SNP; 0.01–0.3 μmol/L) but did not affect relaxations induced by glyceryl trinitrate (GTN; 0.01–1 μmol/L), S-nitrosocysteine (0.1–0.3 μmol/L) or stimulation of nitrergic nerves. A higher concentration of hydroxocobalamin (100 μmol/L) slightly reduced nitrergic nerve stimulation-induced relaxations. 3. Haemoglobin (10 μmol/L) blocked relaxation induced by NO and reduced relaxations induced by SNP, GTN, S-nitrosocysteine and nitrergic nerve stimulation. 4. When nitrergic nerve stimulation-induced relaxations had been partially reduced by the NO synthase inhibitor l-NAME (5–10 μmol/L), hydroxocobalamin had only a weak and transient inhibitory effect. 5. Noradrenergic contractions induced by field stimulation were not affected by hydroxocobalamin (30 μmol/L), but were enhanced by haemoglobin (10 μmol/L). 6. The results suggest that the transmitter released from nitrergic nerves in anococcygeus muscles resembles NO-releasing compounds such as S-nitrosocysteine and GTN but not SNP or free NO.     

新麻满鼻剂的计算机导数分光光度测定

采用普通（手动式）分光光度计，结合自编计算机程序经微机数据处理及图形分析较好地完成了新麻滴鼻剂的0～2阶导数光谱的绘制，并选择二阶导数分光光度法对其主要成份盐酸麻黄碱的含量进行了分析测定，有效地消除了尼泊金乙酯的干扰，平均回收率为100．95％，变异系数为0．55％，操作简便、结果准确，便于应用推广。     

EFFECTS OF ARGININOSUCCINIC ACID ON NITRIC OXIDE-MEDIATED RELAXATIONS IN RAT AORTA AND ANOCOCCYGEUS MUSCLE

1. Argininosuccinic acid (ASA), a naturally occurring NG derivative of arginine, and the nitric oxide synthase (NOS) inhibitor NG-nitro-L-arginine methyl ester (L-NAME) were compared for their ability to reduce responses to nitric oxide (NO) derived from endothelial cells (aorta) and nitrergic nerves (anococcygeus muscle). 2. In isolated rings of rat aorta, endothelium-dependent relaxation responses to acetylcholine were abolished by L-NAME (0.1 mmol/L) and were reduced by ASA (0.1 and 0.3 mmol/L). Relaxations induced by sodium nitroprusside (SNP) were not affected by L-NAME but were reduced by ASA. 3. In rat isolated anococcygeus muscles, relaxations elicited by nitrergic nerve stimulation at 1 Hz were abolished by L-NAME (0.1 mmol/L) but were only slightly reduced by ASA (1 mmol/L). The effect of ASA was not sustained. L-Arginine (1 mmol/L) prevented the effect of L-NAME but not that of ASA. Neither ASA or L-NAME inhibited SNP-induced relaxation in the anococcygeus muscle. 4. The results suggest that ASA inhibits NOS but this does not totally account for its effects in reducing NO-mediated relaxations produced by the endothelium-dependent vasodilator acetylcholine in rat aortic rings and stimulation of nitrergic nerves in the rat anococcygeus muscle.     

麻黄碱—PVC膜电极的制备及其应用

本文介绍麻黄碱四苯硼盐—聚氯乙烯膜电极的制备及其应用于盐酸麻黄碱注射液和片剂的测定。电极膜由11%的电活性物质、44.4%的邻苯二甲酸二辛酯增塑剂和44.4%的聚氯乙烯组成。制成的电极的电位响应在盐酸麻黄碱浓度在10^-1～10^-3M范围内符合Nernst方程,检限下限为5.7×10^-5M。电极的重现性、稳定性良好,响应迅速,寿命也较长。用此电极按直接电位法测定盐酸麻黄碱注射液及片剂,步骤简捷,精密度良好,结果与容量法一致。     

THE EFFECTS OF m-AMSA ON RAT ISOLATED HEART

m-AMSA (4'[9-acridinylamino]methansulphon-m-anisidide) is a new cytoxic agent now under clinical trial. We used the rat isolated perfused heart model in order to investigate the cardiac effects of m-AMSA. The results of the dose-response study indicate that m-AMSA has an acute moderate negative inotropic effect. The 90% effect (25% decrease in developed force compared to the control) was observed at drug concentration of 1.5 micrograms/ml. The refractory period (as measured by stimuli of twice diastolic threshold intensity) increased progressively as the drug concentration was increased (up to 2.5 micrograms/ml). Measurements of the strength-duration and strength-interval relationship showed that m-AMSA induced a significant reduction (P less than 0.005) in excitability and prolongation of refactoriness. We suggest that m-AMSA has a membranal cardiotoxic effect in addition to its known intracellular cytotoxic effect.     

硝苯地平及克罗卡因对离体大鼠膀胱和主动脉平滑肌的影响

用体外大鼠胸主动脉条和膀胱条的制备,比较了钙拮抗剂硝苯地平(nifedipine)和钾通道开放剂克罗卡因(cromakalin)对受体激活和KCl引起的平滑肌收缩的作用。结果表明,对NE引起的大鼠主动脉收缩,nifedipine的抑制作用明显强于cromakalim;而用氨甲酰胆碱(carbachol)激动胆碱能M 受体引起大鼠膀胱环形肌和纵形肌收缩时,两者的抑制作用无明显差异。由KCl 27.5mmol·L^-1去极化引起收缩时,nifedipine对大鼠膀胱环形肌、纵形肌及血管这3种组织的舒张作用均明显比cromakalim强。提示:在由受体介导的收缩中,cromakalim对膀胱组织的舒张作用较强,而nifedipine对血管平滑肌则作用更强;但在由KCl去极化引起的收缩中,nifedipine对血管和膀胱这两种组织的抑制作用较强。