共查询到19条相似文献,搜索用时 187 毫秒
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α-胺基苄基膦酸酯的合成及其生物活性 总被引:1,自引:0,他引:1
目的寻找具有内皮依赖性舒张血管活性的新结构胺基膦酸酯类化合物。方法运用一种新型的类Mannich反应,以生物电子等排体原理设计合成了一系列α-胺基苄基膦酸酯类化合物,并运用离体大鼠血管环和离体豚鼠回肠收缩实验观察其舒张血管活性及其对M受体的激动作用。结果共合成了7个新的α-胺基苄基膦酸酯类目标化合物,其结构经IR,1H NMR和元素分析确定。初步离体血管环实验和离体豚鼠回肠收缩实验结果显示,化合物2a,2b和2c有一定的舒张血管活性且不激活平滑肌M受体。结论在浓度为1×10-5 mol·L-1时,化合物2b和2c有较强的舒张血管活性,其舒张率分别为(67±21)%,(82±18)%,而且不激动M受体,其中,化合物2b有内皮依赖性的舒张血管反应。 相似文献
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衍生化GC法测定生物转化产品L-山梨糖及其中残余D-山梨醇的含量 总被引:4,自引:0,他引:4
设计了生物转化产品L-山梨糖及其中残余D-山梨醇的衍生化GC测定方法。以乙酸酐—吡啶(1∶1)为衍生化试剂对样品中残余D-山梨醇进行乙酰化GC测定,再以四氢硼钠为还原剂、乙酸酐为乙酰化试剂对样品中L-山梨糖进行还原乙酰化GC测定。结果表明,D-山梨醇及L-山梨糖分别在0.01999~2.999μg及4.00~24.00μg范围内呈线性。本法精密度及回收率均较好,可用于监测L-山梨糖生物转化终点及其成品中L-山梨糖及残余D-山梨醇的含量。 相似文献
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N-乙酰基-L-谷氨酰基-泼尼松龙肾靶向前体药物研究 总被引:1,自引:1,他引:1
目的通过研究N-乙酰基-L-谷氨酰基-泼尼松龙的体内分布,考察该前体药物的肾靶向性。方法小鼠iv后,采用高效液相法,在规定时间段测定各组织脏器的泼尼松龙浓度, 并采用大鼠骨密度的测定仪确证前体药物的副作用。结果小鼠给药后15 min,前体药物组肾脏中泼尼松龙浓度为(86±8) μg·g-1,泼尼松龙组为(57±4) μg·g-1,60 min后前体药物组肾脏药物浓度为 (67±5) μg·g-1;泼尼松龙组(42±4) μg·g-1。大鼠给药30 d后,股骨的骨密度分别为(0.08±0.03) g·cm-2 (泼尼松龙)和(0.14±0.06) g·cm-2(前体药物组)。结论前体药物具有肾靶向性, 并能降低致骨质疏松的副作用。 相似文献
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氟哌啶醇对大鼠离体海马脑片和原代神经元缺糖/缺氧和N-甲基-D-天冬氨酸损伤的保护作用 总被引:3,自引:0,他引:3
目的观察氟哌啶醇对大鼠离体海马脑片和原代神经元的缺糖/缺氧(OGD)和N-甲基-D-天冬氨酸(N-methyl-D-aspartate,NMDA)损伤的潜在保护作用及其机制。方法海马脑片OGD以无葡萄糖的人工脑脊液中通95% N2+5% CO2诱导。通过测定TTC染色后形成的红色产物来分析脑片活性。结果氟哌啶醇(1和10 μmol·L-1)抑制OGD损伤,抑制率分别为17.7%和25%,而D2多巴胺受体拮抗剂多潘立酮无此作用。NMDA也能显著降低海马脑片及原代神经元的活性,而氟哌啶醇可抑制这一损伤作用。结论氟哌啶醇对大鼠离体海马脑片OGD和原代神经元NMDA损伤有保护作用。 相似文献
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给大鼠侧脑室内注射(icv)硝普钠(SNP)、NO的前体物质L-精氨酸(L-Arg)和精-精二肽(Arg-Arg),NO合成酶(NOS)抑制剂NG-硝基-L-精氨酸(NNLA),观察清醒状态大鼠血压和心率的变化,探讨脑内NO对清醒状态大鼠心血管活动的调节作用。实验结果表明,icvSNP(8,16,32μg)使血压升高,并呈剂量效应关系,同时使心率加快。icvL-Arg(200μg)或不同剂量的精-精二肽也使血压升高,心率加快;icvNNLA(100μg)则使血压下降,心率减慢。以上结果提示,在一定范围内提高脑内NO,对心血管活动有正性调节作用,降低脑内NO则对心血管活动有负性调节作用。 相似文献
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氯哌胺(Loperamide)是一种新型止泻药,能拮抗15-M-PGF2α引起的小鼠小肠内碳粉推进加速和腹泻,作用比吗啡和阿托品强,对离体大鼠回肠的抑制作用也比吗啡、阿托品强。氯哌胺能降低肠平滑肌张力,抑制离体大鼠回肠对15-M-PGF2α的反应性,但却增强子宫平滑肌对15-M-PGF2α的反应性。氯哌胺对离体大鼠子宫自发收缩活动低浓度兴奋、高浓度抑制。氯哌胺对15-M-PGF2α促进大鼠空肠水和钠离子分泌也有拮抗作用,此作用不能被纳洛酮翻转。氯哌胺在小鼠的急性半数致死量为77.9 mg/kg。 相似文献
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有机锡化合物抗肿瘤生物活性研究 总被引:5,自引:0,他引:5
有机锡(IV)化合物能明显地抑制大鼠脑组织中PKC活性和肿瘤细胞增殖,且两者之间存在着相关性。抗肿瘤活性的构效关系是:(1)有机基团R决定整个化合物的生物活性,Ph>Et>n-Bu;(2)卤素的电负性影响化合物活性的大小。抗肿瘤活性可能通过[snR2]2+实现。并能部分地阻断HL-60细胞周期中的GI期向S期的移行。[SnPh2F2],[SnPh2(CysOS)]H2O和[SnPh2Cl2·phen(CH3)2]对PKC的IC50值分别为25,15和20 umol·L-1,对HL-60细胞的IC50值分别为0.5,4.0和0.3umol·L-1。但它们无诱导分化HL-60和K562细胞的作用。 相似文献
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本文比较了从中国萝芙木中提出的盐析碱spegatrine(SP) 及其双聚体dispegatrine(DISP)对α1和α2受体亲和力及其效应的影响。结果发现SP和DISP对α受体有亲和力,DISP的作用比SP强一个数量级。DISP对NE引起肛尾肌收缩呈拮抗作用,SP对小剂量NE呈抑制作用,对较大剂量NE表现协同作用,DISP和SP对可乐宁抑制输精管收缩均呈拮抗作用,DISP比SP强3~4倍。表明DISP为非选择性的α受体阻滞剂,而SP为α2受体阳滞剂,对α1受体作用性质尚待阐明。 相似文献
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用核磁共振新技术测定川续断皂甙F和H1两个新皂甙的结构及光谱规律研究 总被引:7,自引:0,他引:7
从川续断(Dipsacus asperoides c.Y.cheng et T.M.Ai)根部的乙醇提取物中得到二个新三萜皂甙,命名为川续断皂甙(asperosaponins)F和H1。川续断皂甙F(I)是含六个糖的皂甙,川续断皂甙H1(II)是含八个糖的皂甙。运用化学方法及光谱(1HNMR,13CNMR,1H-1H COSY,——维多重接力COSY,选择性远程DEPT和三重共振NOE差谱)解析,鉴定其结构分别为3-O-[β-D-吡喃木糖(1→4)-β-D-吡哺葡萄糖(1→4)][α-L-吡喃鼠李糖(1→3)]-β-D-吡喃半乳糖(1→3)-α-L-吡喃鼠李糖(1→2)-α-L-吡喃阿拉伯糖-常春藤皂甙元(I)和3-0-[β-D-吡喃木糖(1→4)-β-D-吡喃葡萄糖(1→4)][α-L-吡喃鼠李糖(1→3)]-β-D-吡喃半乳糖(1→3)-α-L-吡喃鼠李糖(1→2)-α-L一吡喃阿拉伯糖-常春藤皂甙元-28-O-β-D-吡喃葡萄糖(1→6)-β-D-吡喃葡萄糖酯甙(II)。并总结出一些光谱方面的变化规律,可用于糖的鉴定,以及构型、糖链的连接顺序和糖与甙元之间的连接位置的说明。 相似文献
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DANA M. BAKHEET K. E. H. EL TAHIR M. I. AL-SAYED H. A. EL-OBEID K. A. AL-RASHOOD 《Pharmacological research》1999,39(6):463
The influence of N -ethyl- and N -benzyl-1,2-diphenyl ethanolamines (compounds E and B, respectively) was examined on the spontaneously contracting rabbit jejunum and the rat uterus together with their influence on the contractions induced by some spasmogens in the guinea-pig ileum and oxytocics and CaCl2in the pregnant rat uterus. Both E and B inhibited the spontaneous contractions of the rabbit jejunum with ID50values of 0.13 and 0.03 μmol ml−1. Their inhibitory activities were not antagonized by α- or β-adrenoceptor blockers but significantly reversed by CaCl2(0.015 μmol ml−1). The compounds also antagonized nicotine, ACh-, histamine-, 5-HT- and CaCl2-induced contractions by 44–100%. Compound E seemed to be several times more potent than B in inhibiting the spontaneous uterine contractions with an ID50of (7 nmol ml−1). Their inhibitory effects were not antagonized by β2-adrenoceptor or H2-receptor blocking drugs. Both compounds (40 nmol ml−1) antagonized in a competitive manner CaCl2-induced contractions in the K+-depolarised uterus and PGE2and oxytocin-induced uterine contractions. The ID50values were in the range of 1.6–10.7 nmol ml−1. The results suggest that E and B compounds may be considered as putative L-Ca2+channel blockers with certain selectivities. The E compound seemed to be more selective against uterine L-Ca2+channels and the B compound against intestinal smooth muscles. Thus, the compounds may be of potential value in treatment of some colics, the irritant bowel syndrome, dysmenorrhoea and premature deliveries. 1999 Academic Press@p$hr 相似文献
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酞丁安对映体合成及其抗单纯疱疹病毒活性评价 总被引:1,自引:0,他引:1
酞丁安(3-酞酰亚胺-2-氧-正丁醛双缩氨硫脲,TDA)是药物研究所创制的抗病毒新药。为了研究其对映异构体(R),(S)-TDA对病毒活性及毒性是否有差异,并与消旋酞丁安(RS)-TDA的抗病毒活性及毒性进行比较,本文分别用已知构型的(R)-与(S)-丙氨酸为原料,通过缩合等6步反应,得到光学活性的(R)-,(S)-TDA,并与外消旋酞丁安比较其抗病毒活性及毒性。三者的抗单纯疱疹病毒活性与对细胞的毒性差别不大,说明消旋酞丁安临床使用是安全有效的。 相似文献
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报道了九里香中6种香豆精——九里香乙素(murpanidin),九里香丙素(murpanicin),海南九里香内酯(hainanmurpanin),murragatin,merazin hydrate,murralogin的反相高效液相色谱法测定。用Nuckosil—C18键合相柱、乙腈-水-甲醇(30:100:10)为流动相,异补骨脂素为内标,320 nm为检测波长。方法简便易行。 相似文献
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Wang GJ Liao JF Hintz KK Chen WP Su MJ Lin YL Shi CC Chen CF Ren J 《Naunyn-Schmiedeberg's archives of pharmacology》2004,369(3):322-329
Petasites formosanus, an indigenous species of Petasites, has been used to treat cardiovascular diseases such as hypertension for years. We have suggested recently that S-petasin, a major sesquiterpene from P. formosanus, inhibits vascular smooth muscle contraction through inhibition of voltage-dependent Ca2+ channels, a phenomenon possibly responsible for the hypotensive effect of P. formosanus. This study was designed to examine the chronotropic and inotropic actions of S-petasin in the heart in vivo and in vitro. Administration of S-petasin (0.1–1.5 mg/kg i.v.) in anesthetized rats reduced heart rate dose-dependently. This response was consistent with significant suppression of both contractile amplitude and spontaneous firing rate of isolated atria, responses that were not antagonized by atropine (1 µM). Mechanical evaluation in isolated ventricular myocytes showed that S-petasin (0.1 to 100 µM) depressed peak myocyte contraction and intracellular Ca2+ transients concentration-dependently. The duration of myocyte contraction was not affected. Whole-cell voltage clamp analysis revealed that S-petasin inhibited the L-type Ca2+ current (ICa,L) concentration-dependently and shifted the steady-state inactivation curve of ICa,L to more negative potentials. However, a receptor-binding assay failed to identify any significant interaction between S-petasin (0.1–300 µM) and the dihydropyridine binding sites of L-type voltage-dependent Ca2+ channels. Taken together, these data show that the negative chronotropic and inotropic properties of S-petasin that can be ascribed mainly to ICa,L inhibition, but not to blockade of dihydropyridine binding sites of L-type Ca2+ channel or to muscarinic receptor activation. 相似文献