盐酸戊乙奎醚对豚鼠离体膀胱和家兔在体膀胱的作用

目的研究盐酸戊乙奎醚im及ig对麻醉及清醒家兔在体膀胱以及豚鼠离体膀胱的抑制收缩作用。方法在体采用家兔膀胱内插入球囊,im及ig后,于多个时间点给予乙酰胆碱(Ach)。测量膀胱内压;离体采用测量盐酸戊乙奎醚给药后豚鼠离体膀胱条自主收缩及乙酰胆碱激动收缩的最大张力,计算抑制50%收缩的盐酸戊乙奎醚浓度。结果盐酸戊乙奎醚能抑制由Ach引起的膀胱内压上升,对抗Ach对离体膀胱条的收缩作用,并能抑制离体膀胱条的自主收缩。结论盐酸戊乙奎醚能有效缓解膀胱的痉挛状态。     

槲皮素对兔离体肠平滑肌张力的影响及其机制

目的:观察槲皮素对兔离体回肠平滑肌肌张力的影响,并探讨其作用机制。方法:试验采用经典的离体小肠灌流技术,观察槲皮素(quercetin,Que)对回肠平滑肌自主收缩活动以及乙酰胆碱(acetylcholine,Ach)、氯化钡及组胺(histamine)所致痉挛性收缩肠平滑肌张力的影响。结果:槲皮素(20,60,100mol.L-1)能剂量依赖性的抑制家兔离体小肠平滑肌自发性收缩,对乙酰胆碱,组胺和氯化钡所致的兔离体肠痉挛性收缩也具有剂量依赖性抑制作用。在无钙台式液中,槲皮素可明显抑制Ach引起的回肠平滑肌收缩(P<0.01),亦能使氯化钙量效曲线下移。槲皮素对Bay K8644(0.5mol.L-1)引起的回肠平滑肌收缩亦有明显抑制作用(P<0.01)。结论:槲皮素明显抑制了家兔离体小肠平滑肌的收缩活动,其机制与抑制外钙内流及内钙释放有关。     

蜂斗菜不同提取物对豚鼠离体回肠收缩的影响

目的 比较蜂斗菜不同提取物对豚鼠离体回肠收缩的影响。方法 采用豚鼠离体回肠实验,以组胺、乙酰胆碱不同激动剂为研究模型,比较蜂斗菜CO₂超临界提取物、80%乙醇提取物、80%乙醇提取物的不同极性提取物及乙酸乙酯提取物经硅胶柱层析分离获得的不同馏分对豚鼠离体回肠的收缩作用,计算各个提取物对豚鼠回肠收缩幅度的抑制率。结果 蜂斗菜不同提取物对组胺、乙酰胆碱所致的豚鼠离体回肠收缩有显著拮抗作用,其中乙酸乙酯提取物硅胶柱色谱的馏分抑制作用最强。结论 蜂斗菜不同提取物均能抑制组胺、乙酰胆碱引起的豚鼠离体回肠收缩作用,脂溶性成分抑制作用最强,其机制可能与M、H₁受体的抑制有关。     

大黄素对动物离体回肠收缩作用的影响

大黄素对豚鼠、大鼠和家兔离体回肠的作用均与剂量相关,＜29.6μmol/L时收缩幅度随剂量增加而增强(P＜0.01和P＜0.05);＞29.6μmol/L时收缩幅度逐渐减弱直至停止;大黄素对家兔离体回肠的收缩频率无明显影响(P＞0.05);大黄素增强回肠收缩幅度的作用可被低剂量的阿托品拮抗,提示大黄素有类似乙酰胆碱的作用,但作用较弱.实验表明大黄素对豚鼠、大鼠和家兔离体回肠具有双向调节作用,这种作用对肠麻痹及痉挛可能有调节性治疗作用.     

盐酸戊乙奎醚对胃解痉作用的药效学研究

研究盐酸戊乙奎醚(PQN)肌肉注射及灌胃给药对麻醉及清醒家兔在体胃及豚鼠离体胃条的抑制收缩作用。结果表明，PQN能抑制由乙酰胆碱(Ach)和氯贝胆碱引起的胃内压上升，拮抗Ach对离体胃条的收缩作用，并能抑制离体胃条的自主收缩。     

二苯氰胂对毒蕈碱性受体的抑制作用

目的研究了日本在我国遗弃的化学武器———二苯氰胂(DC)对离体豚鼠回肠纵肌和毒蕈碱性受体的作用机制,为评估DC的毒理学作用及其对环境的影响提供依据。方法取豚鼠8只,分离豚鼠回肠纵肌16条,分4组,用累积给药法,从低到高分别给予不同浓度的DC,记录离体豚鼠回肠纵肌收缩的幅度,求出DC作用于离体回肠纵肌的EC50值,并通过DC与乙酰胆碱(AChR)的相互作用,研究DC的作用机制。在放射性配体-受体结合实验中,从10只大鼠大脑中提取受体,通过DC与[3H]QNB的竞争结合作用,研究了DC对毒蕈碱性受体的作用。结果DC可抑制离体豚鼠回肠纵肌的收缩作用,其对离体豚鼠回肠纵肌的EC50值为(7.335±2.377)×10-7mol/L,AChR可收缩离体豚鼠回肠,并可反转DC引起离体豚鼠回肠纵肌的舒张作用。在放射性配体-受体结合实验中,DC与毒蕈碱性受体结合的Ki值为(9.19±1.52)nmol/L,IC50值为(16.00±2.65)nmol/L。结论DC可作用于mAChR受体上,初步断定为AChR的拮抗剂。     

二苯氰胂对豚鼠回肠纵肌和蛙坐骨神经腓肠肌的作用

目的　第二次世界大战后 ,日本在我国遗留大量的二苯氰胂 (DC) ,为了销毁日本遗弃化学武器和制定相应的环境标准 ,本研究通过DC对离体豚鼠回肠纵肌和蛙坐骨神经腓肠肌的毒性作用 ,对DC的毒性作用方式和作用机制进行初步研究。方法①DC对离体豚鼠回肠纵肌的毒性作用。豚鼠体重为 30 0～ 4 5 0g ,♀♂各半。豚鼠回肠纵肌标本的制备与常规相同。每只豚鼠制取纵肌标本 2条 ,用累积给药法 ,测得DC对标本的作用强度 ,并通过 : DC抑制电刺激回肠引起纵肌收缩后 ,加入肾上腺素、乙酰胆碱 ; 当纵肌收缩抑制到 80 %时 ,加入乙酰胆碱 ; 先加乙酰胆碱 ,当电刺激回肠纵肌收缩恢复到正常时 ,加入DC ,当纵肌收缩到 80 %时 ,再加入 2倍剂量的乙酰胆碱。②DC对蛙坐骨神经腓肠肌的毒性作用。实验动物为蟾蜍。坐骨神经腓肠肌标本的制备与常规相同。给药方式 :把药液加在大小厚薄相等的棉条上 ,容量为 0 .1mL ,覆盖坐骨神经。结果　①DC抑制电刺激离体豚鼠回肠纵肌收缩作用的ED50 值为 734(971～ 4 98)nmol;②肾上腺素不能抑制DC对豚鼠回肠纵肌的作用 ,乙酰胆碱可以抑制DC对豚鼠回肠纵肌的作用 ;低浓度的乙酰胆碱可以抑制DC对豚鼠回肠纵肌的作用 ;先加入乙酰胆碱 ,乙酰胆碱可促进豚鼠回肠纵肌的收缩。当纵肌收缩恢复正常后 ,     

辛夷挥发油的抗过敏实验研究

目的：研究辛夷挥发油的抗过敏作用。方法：采用磷酸组织胺（HA）、氯化乙醇胆碱（Ach）所致豚鼠离体回肠收缩实验，卵白蛋白（OA）引起的致敏豚鼠离体回肠实验及大鼠肥大细胞脱颗粒实验法。结果：辛夷挥发油能显著抑制HA、Ach引起的豚鼠离体回肠收缩，对致敏豚鼠离体回肠的过敏性收缩有较强的抑制作用，并能明显阻止大鼠肥大细胞脱颗粒。结论：辛夷挥发油具有较强的抗过敏作用。     

蒙药紫花高乌头醇提物对豚鼠离体气管平滑肌的作用及机制

目的观察蒙药紫花高乌头醇提物对豚鼠离体气管平滑肌张力的影响,探讨紫花高乌头醇提物的平喘机制。方法用离体气管环法观察紫花高乌头醇提物高、中、低3种不同剂量作用于由乙酰胆碱(Ach)预收缩的豚鼠离体气管平滑肌,观察其对平滑肌张力的影响及对Ach诱发的离体气管平滑肌收缩的量效曲线的影响。结果蒙药紫花高乌头醇提物可舒张由Ach诱发的豚鼠离体气管平滑肌收缩,且舒张作用随剂量增加而加强。紫花高乌头醇提物能使Ach诱发的豚鼠离体气管平滑肌收缩效应的量效曲线右移,最大效能降低。结论蒙药紫花高乌头醇提物对豚鼠离体气管平滑肌有舒张作用,可能与非竞争性拮抗Ach的收缩作用有关。     

款冬花不同提取物对豚鼠离体回肠收缩作用的研究

目的研究比较款冬花各个不同提取物对豚鼠离体回肠收缩的作用。方法通过石油醚、乙酸乙酯、CO2超临界萃取等方法制备款冬花多个提取物,将离体豚鼠回肠悬吊于克-亨试液中,观察给药后豚鼠回肠的收缩作用,计算豚鼠回肠收缩幅度抑制率。结果款冬花各个不同提取物均能降低组胺引起的豚鼠离体回肠收缩幅度。结论款冬花各个提取物能明显抑制豚鼠回肠收缩运动。     

Vascular and myocardial effects of mecinarone

The effects of mecinarone on the contractions induced by noradrenaline, potassium and calcium were studied with the isolated aorta and central artery of the rabbit ear. In our experimental conditions mecinarone was found to act as a competitive antagonist of calcium. It preferentially inhibited the noradrenaline-evoked contraction induced in the rabbit ear artery and had a smaller effect on the extracellular calcium-induced contraction of depolarized arterial smooth muscle. In the isolated guinea pig heart, mecinarone produced a reversible decrease in the rate of rise of the ascendant phase of the action potential without significantly changing the resting potential. In hearts inactivated by depolarisation, mecinarone inhibited the contractions restored by isoproterenol without suppressing the calcium action potential. These results suggest that the mode of action of mecinarone is different from that of verapamil or nifedipine but is comparable to that of chlorpromazine, although mecinarone has no sedative effect.     

Cyclosporine A preparations and their vehicles induce contraction of the guinea pig gallbladder in vitro: the role of cyclooxygenase metabolites.

The aim of this study was to establish whether prostanoids play a role in the contraction induced by cyclosporine A (CyA) preparations in the guinea pig isolated gallbladder strips. It was also aimed to study the effects of the preparations and their solvents on the acetylcholine-evoked rhythmic contractions of the guinea pig isolated sphincter of Oddi (SO). Isometric contractions were recorded. CyA parenteral and oral preparations and their vehicles, Cremophor-EL and Labrafil caused concentration-dependent and sustained contractions (74.2 +/- 6.2, 58.4 +/- 6.3, 88.9 +/- 4.9 and 47.5 +/- 6.2% of maximum KCl contraction, respectively) of gallbladder strips, but not of SO. Quinacrine, indometacin and ridogrel inhibited the contraction induced by CyA preparations and their vehicles in gallbladder strips (for CyA parenteral preparation, 34.7 +/- 6.7, 1.4 +/- 0.9, 19.0 +/- 6.4% of maximum KCl contraction, respectively). The drug and its vehicles changed neither the initial contraction nor the amplitude and frequency of the phasic contractions induced by acetylcholine in SO preparations. The results indicate that the drug is able to contract the gallbladder strips and the vehicles contribute to the contracting effect of CyA. Prostanoids may be responsible for the CyA-induced contraction of the gallbladder.     

双喘通药理作用的研究

本文比较了双喘通与喘通的平喘作用。二者弛张豚鼠离体气管平滑肌作用和对抗组织胺收缩豚鼠离体气管平滑肌作用,在低浓度时相近,在较高浓度时双喘通强于喘通。延长组织胺气雾对豚鼠致喘时间的作用,喘通强于双喘通。心得安不能阻断双喘通对离体气管和离体子宫平滑肌的弛张作用,但能阻断喘通的作用。双喘通可拮抗 Ach 和 BaCl_2对离体气管和离体肠管平滑肌的收缩作用。双喘通对豚鼠离体回肠具有弛张作用和解痉作用。双喘通给小鼠静脉注射 LD_(50)为10.0±0.2mg/kg,灌胃给药 LD_(50)为64.0±8.6mg/kg。     

国产扑喘息敏(Procaterol)的药理研究

扑喘息敏5×10~(-5)-2×10~(-3)mg/ml 对豚鼠离体气管有直接弛张作用,4×10~(-4)-4×10~(-3)mg/ml 可对抗组织胺收缩离体气管的作用,5mg/kg ip 可延长组织胺对豚鼠所致呼吸困难的潜伏期,20mg/kg iv 对麻醉兔有明显而暂时的降血压作用,2.5×10~(-3)mg/ml 可使豚鼠离体心脏收缩幅度增大,心率增加,1×10~(-2)mg/ml 可使灌流液流量和心率增加,3.6×10~(-2)mg/ml、9×10~(-2)mg/ml 可使部分豚鼠离体回肠收缩幅度增大,频率增加,张力增加。扑喘息敏给小白鼠ip,LD_(50)为390.5±20.3mg/kg。     

盐酸丙哌维林对膀胱平滑肌收缩的影响(英文)

观察了盐酸丙哌维林 ( Pro)对离体豚鼠膀胱平滑肌自动节律性收缩和 KCl诱导离体豚鼠膀胱平滑肌收缩的影响 ;同时观察了 Pro对家犬在体膀胱自动节律性收缩的影响 .Pro在 1 ,1 0 μmol· L-1浓度时 ,对离体豚鼠膀胱平滑肌自动节律性活动具有兴奋作用 ,可使自动节律性收缩频率增加 ,幅度加大 ;在 1 0 0μmol· L-1浓度时则表现为抑制作用 ,可完全抑制豚鼠膀胱平滑肌的自动节律性收缩 ,同时可使平滑肌松弛 ,基础张力降低 .Pro对 KCl引起的豚鼠离体膀胱平滑肌的收缩具有明显的抑制作用 ,在 1 ,1 0 ,1 0 0 μmol· L-1浓度时对 KCl诱导豚鼠离体膀胱平滑肌收缩的抑制率分别为 ( 7.4±6.5) % ,( 31 .3± 1 2 .8) % ,( 68.4± 7.1 ) % ,其 IC50 为( 2 5.2± 4.7) μmol·L-1.十二指肠给 Pro对在体家犬膀胱自动节律性收缩具有明显的抑制作用 ,60 ,30mg· kg-1可明显降低膀胱自动节律性收缩频率和幅度且具有剂量依赖性 ,与药前比有显著性差异 ,60 mg· kg-1药后 1 0 min即可起效 ,药效可持续 90min,Pro在上述剂量下对血压 ,心率无明显影响 .本实验结果提示 Pro在低剂量时对离体膀胱自动节律性收缩具有一定的兴奋作用 ,在高剂量时则表现为明显的抑制作用 ;Pro对 KCl诱导的豚鼠离体膀胱平滑肌收缩和膀胱扩张诱导的家?     

Contractile effect of 1-O-hexadecyl-2-O-acetyl-sn-glycero-3-phosphocholine on strips of isolated rat intestine

The contractile effects of AGEPC were examined on various regions of rat isolated intestine. The duodenum, jejunum and ileum showed only the tonic component of contraction to AGEPC at the low dose (<10⁻⁹ m) but at the high dose (10⁻⁷ m) biphasic contractions were induced, consisting of a phasic followed by a tonic component. In the colon, however, the AGEPC-induced maximum contraction was comparable in magnitude to that produced by acetylcholine; also the contraction profile was different from that elicited from the other regions of the intestine. Low doses of AGEPC caused a slow, sustained contraction and at high doses phasic and tonic components were not dissociated.     

The antispasmodic activity of Buddleja scordioides and Buddleja perfoliata on isolated intestinal preparations

The antispasmodic activity of extracts from the aerial parts of Buddleja scordioides and Buddleja perfoliata (family: Scrophulariaceae) was studied on isolated tissue preparations from rabbit and guinea pig intestine. The chloroformic extract from the plants exhibited a significant relaxation on the spontaneous contraction of isolated rabbit jejunum at concentrations ranging from 1 to 400 mug/ml, and also caused an inhibitory effect on both K(+) and Ca(2+) induced contractions in the same tissue. The extracts at moderate doses (50 mug/ml) reduced 5-hydroxytryptamine (5-HT), acetylcholine and histamine induced contractions on isolated guinea pig ileum. Therefore, B. scordioides and B. perfoliata possess similar relaxant mechanism of action, in view of the fact that both inhibit K(+) induce contraction and act through serotoninic, muscarinic and histaminic receptors. So, these data support the idea that the extracts may interfere either with calcium mobilization from intracellular stores, or with calcium interaction with regulatory proteins (e.g., calmodulin), or in other steps in the calcium signaling pathway. This leads us to suggest that the spasmolytic effect of both Buddleja species on smooth muscular contractility are due to the same or similar compounds occurring in these two species, which might be present in similar quantities.     

Myosin light chain phosphorylation and Mn2+-dependent acetylcholine-induced contractions in guinea pig vas deferens

We have reported that noradrenaline but not K+ induced a sustained and dose-dependent contraction without extracellular Ca2+ and Mn2+ in Ca2+-depleted Mn2+loaded vas deferens from the guinea pig. The Mn2+dependent noradrenaline-induced contractions developed without an increase in phosphorylation of 20-kDa myosin light chain. To clarify whether such an unusual Mn2+dependent contraction was induced only by noradrenaline or not, we examined effects of acetylcholine on Ca2+-depleted Mn2+-loaded guinea pig vas deferens. Acetylcholine (1 microM(-1) mM) induced a sustained dose-dependent contraction without extracellular Ca2+ or Mn2+. W-7 (10 microM or 100 microM) and wortmannin (1 microM) both reduced the Mn2+dependent acetylcholine-induced contractions similarly to Ca2+-dependent acetylcholine-induced contractions in isolated vas deferens without either Ca2+ depletion or Mn2+ loading. However, the Mn2+-dependent acetylcholine-induced contractions developed without a significant increase in the phosphorylation of the myosin light chain determined by urea-glycerol polyacrylamide gel electrophoresis and immunoblotting. These results indicate that acetylcholine as well as noradrenaline induces Mn2+-dependent contraction and are consistent with our previous assumption that Mn2+ may preferentially support receptor-mediated contractions in the guinea pig isolated vas deferens. The results also suggest that the activation of myosin light chain kinase is essential for the development of Mn2+-dependent acetylcholine-induced contractions, and that Mn2+ may accelerate formation of non-phosphorylated attached cross-bridges during receptor activation.     

硫酸寡糖对豚鼠气管平滑肌的作用

目的 观察硫酸寡糖对组胺(His)、乙酰胆碱(Ach)引起的正常豚鼠离体气管平滑肌收缩的影响、对卵白蛋白(OVA)致敏豚鼠离体气管平滑肌受到OVA攻击时引起收缩的影响及对吸入His引起的正常整体豚鼠哮喘的影响。方法 采用豚鼠离体气管片法、致敏豚鼠离体气管Schultz-Dale法和整体动物引喘法。结果 硫酸寡糖能显著抑制His引起的正常豚鼠离体气管平滑肌收缩,但对Ach引起的正常豚鼠离体气管平滑肌收缩无显著抑制作用;能显著抑制OVA诱发的致敏豚鼠离体气管平滑肌的收缩;能显著延长His引喘潜伏期,使抽搐动物数减少。结论 硫酸寡糖具有抗His、抗过敏和平喘作用。