4′-甲基-7-(2-羟基-3-异丙胺基-丙氧基)-黄酮盐酸盐对冠脉血流和家兔实验性心肌梗塞的影响

4′-甲基-7-(2-羟基-3-异丙胺基-丙氧基)-黄酮盐酸盐(代号SIPI-549),是在4′-甲基立可定的基础上,由上海医药工业研究院合成的新化合物。本室已经证明SIPI-549具有明显的抗心律失常作用,且治疗指数较高。本文主要报道其对冠脉血流和实验性心肌梗塞的作用。药品和试剂     

4′-甲基-7-(2-羟基-3-异丙胺基-丙氧基)-黄酮盐酸盐对冠脉血流和家兔实验性心肌梗塞的影响

SIPI-549 is a new cOmpound. In Langendorff's isolated rabbit heart, SIPI-549 significantly increased coronary blood flow (p<0.01), but did not change themyocardium contractibility and heart rate. A study of the uptake of ~(86)Rb by the mouse heart showed a significant increase of nutritional blood flow in the SIPI-549 treated group (p<0.05). On intact dogs, SIPI-549 also showed a significant increase of coronary blood flow (p<.05) and decrease of coronary resistance (p<0.01), but no change of cardiac output and blood presure was observed.In the model of myocardial infarction by high level double-ligation of the anterior descending branch of the left coronary in rabbits, iv SIPI-549 (4.1 mg/kg) significantly reduced the ΣST, NST and NO The size of infarct myocardium was significantly reduced (p<0.05) 24 h after ligation of the coronary artery Similar results were found in the propranolol (1 mg/kg) group. However, no obvious difference between the two groups was observed.     

尼可地尔对不停跳冠脉移植术中患者血流动力学和心肌肌钙蛋白Ⅰ的影响

目的 观察尼可地尔对不停跳冠脉移植术中患者血流动力学和心肌肌钙蛋白Ⅰ(cTnⅠ)的影响。方法 60例择期行不停跳冠脉旁路移植术患者,随机分为对照组(Ⅰ组),尼可地尔10 mg舌下含服组(Ⅱ组)、尼可地尔10 mg舌下含服加20 mg静脉泵注组(Ⅲ组)、尼可地尔20 mg静脉泵注组(Ⅳ组)。分别在麻醉诱导建立监测即刻(T₀)、泵注完尼可地尔或生理盐水后(T₁)、冠脉移植完毕1,2,4,12,24 h(分别记为T₂,T₃,T₄,T₅,T₆)记录心率(HR)、平均动脉压(MAP)、心指数(CI)、肺毛细血管契压(PCWP),同时取静脉血测定心肌肌钙蛋白Ⅰ(cTnⅠ)含量。结果 4组间HR,MAP,PCWP无明显差异(P>0.05);T₄~T₅时,Ⅱ,Ⅲ,Ⅳ组CI明显高于Ⅰ组(P<0.05),Ⅲ组明显高于Ⅱ,Ⅳ组(P<0.05);T₄时,Ⅱ,Ⅲ组cTnⅠ明显低于Ⅰ,Ⅳ组,T₅~T₆时Ⅱ,Ⅲ,Ⅳ组cTnⅠ明显低于Ⅰ组(P<0.05);Ⅲ组明显低于Ⅱ,Ⅳ组。结论 尼可地尔可改善不停跳冠脉旁路移植术患者心脏功能和心肌受损的程度,且和剂量及用药时机有关,对血流动力学无不利影响。     

玉郎伞提取物对心脏血流动力学和冠脉流量的影响

目的：研究玉郎伞提取物(YLS)对冠脉流量(CF)和心脏血流动力学的影响。方法：以比Langcndorff法制备大鼠离体心脏，观察心肌收缩幅度并测定CF。采用心室内插管技术，连接MS2000多媒体生物信号记录系统测定静注YLS前及药后的左心室收缩压(LVSP)、左心室终末舒张压(LVEDP)、心率(HR)、左室压最大上升速率(dp/dtmax)、左室压最大下降速率(-dp/dtmax)、左室开始收缩至dt／dtmax的间隔时间(t-dp/dmax)等血流动力学指标的影响。结果：YLS显著增加冠脉流量(P＜0.05)，明显降低LVSP和dp／dtmax，延长t-dp/dmax，减慢HR及降低心肌的收缩振幅(P＜0.01或P＜0.05)，对LVEDP和-dp/dtmax等舒张性指标无明显影响。结论：YLS具有抑制心肌收缩力、减慢心率和增加冠脉流量作用。     

急性冠脉综合征患者介入应用替罗非班对冠脉血流和心肌灌注的影响

目的观察急性冠脉综合征患者介入治疗中应用替罗非班对冠脉血流的影响。方法接受经皮冠状动脉介入治疗(PCI)急性冠脉综合征患者共82例,分为替罗非班组42例(替罗非班+介入治疗),对照组40例(介入治疗),观察两组患者冠状动脉血流指标如TIMI血流分级、校正的TIMI计帧数(CTFC)、TIMI心肌灌注分级(TMPG)的差别。结果替罗非班组TIMI血流分级、TIMI计帧、TIMI灌注分级均明显优于对照组(P<0.05)。结论急性冠脉综合征患者介入治疗中应用替罗非班可以改善冠脉血流及心肌灌注。     

4′-甲基-7-(2-羟基-3-异丙胺基丙氧基)-黄酮盐酸盐对实验性血栓形成的影响

4′-甲基-7-(2-羟基-3-异丙胺基丙氧基)-黄酮盐酸盐(SIPI-549)对大鼠和家兔实验性血栓形成有剂量(或浓度)依赖性的抑制作用。ⅳ7.5～20.0 mg/kg,使大鼠颈动—静脉旁路血栓湿重减轻。家兔半体内试验(ⅳSIPI-549 10 mg/kg),可使Chandler管中的雪暴现象出现时间和血栓形成时间延长,血栓湿重和干重减轻。家兔体外实验与半体内试验的结果基本一致。     

4′-甲基-7-(2-羟基-3-异丙胺基丙氧基)-黄酮盐酸盐对实验性血栓形成的影响

4′-甲基-7-(2-羟基-3-异丙胺基丙氧基)-黄酮盐酸盐(SIPI-549)对大鼠和家兔实验性血栓形成有剂量(或浓度)依赖性的抑制作用。ⅳ7.5～20.0 mg/kg,使大鼠颈动—静脉旁路血栓湿重减轻。家兔半体内试验(ⅳSIPI-549 10 mg/kg),可使Chandler管中的雪暴现象出现时间和血栓形成时间延长,血栓湿重和干重减轻。家兔体外实验与半体内试验的结果基本一致。     

替格瑞洛对急性ST段抬高型心肌梗死经皮冠脉介入治疗患者冠脉血流及心肌灌注的影响

目的 探讨替格瑞洛对急性ST段抬高型心肌梗死(STEMI)经皮冠脉介入(PCI)治疗患者冠脉血流及心肌灌注的影响.方法 选择2015年1月至2016年7月在我院就诊的STEMI患者80例,均行急诊PCI治疗.将入选患者随机分为观察组40例和对照组40例.观察组患者在急诊PCI术前给予替格瑞洛180mg口服治疗,对照组患者在急诊PCI术前给予氯吡格雷600mg口服治疗.观察两组患者PCI术后TIMI血流分级、术后心肌呈色分级(MBG)、术后90min ST段抬高总回落百分比(sumSTR)及住院治疗期间出血事件.结果HT6K 观察组TIMI3级血流获得率高于对照组(92.5%和75.0%,P<0.05),观察组心肌MBG分级3级获得率高于对照组(80.0%和57.5%,P<0.05),观察组ST段回落率高于对照组(85.0%和60.0%,P<0.05).观察组发生牙龈出血1例、穿刺局部血肿1例,对照组发生皮肤瘀斑1例、穿刺局部血肿1例,两组患者出血发生率比较差异无统计学意义(P>0.05).结论HT6K 替格瑞洛较氯吡格雷更有效改善STEMI患者急诊PCI术后冠脉血流及心肌灌注,且不增加出血风险,安全性较高.     

甲基莲心碱对正常及高血压大鼠血流动力学的影响

iv甲基莲心碱(Nef)6 mg/kg于正常血压、肾性高血压、DOCA盐型高血压大鼠,在血压下降的同时,伴有LVSP,±(dp/dt)max,(dp/dt)P~(-1)的降低,正常血压及肾性高血压大鼠LVSP~-(dp/dt)P~(-1)环缩小,其斜率变小,心率短时变慢,LVEDP变化不明显。iv Nef 2 mg/kg于Wistar高血压大鼠时,仅明显降低血压,而对其它血流动力学指标无明显影响,Nef降低舒张压的作用大于降低收缩压。猫后肢灌流实验证明Nef有明显降低血管阻力的作用。结果表明Nef的降压作用可能由于扩张外周血管所致。     

复方丹参片对家兔实验性心肌梗塞和心肌酶谱的影响

目的观察复方丹参浓缩片对实验动物心肌梗死面积 (质量 )和心肌酶谱的作用。方法连续给家兔灌胃复方丹参浓缩片 1 4 2、0 71、0 35mg·kg-1和复方丹参滴丸 38mg·kg-1以及等容积生理盐水 14d ,然后开胸暴露心脏 ,双重结扎冠状动脉前降支 ,72h取血测定心肌酶谱 (GPT、GOT、LDH、α HBD、LD、CKMB)的变化 ,处死家兔 ,摘取心脏 ,剪去心房及大血管 ,称质量 ,将心肌切成若干片 ,0 5 % (w)N -BT染色 15min ,将暗蓝色心肌小心切掉 ,不染色梗死心肌称质量 ,计算梗死心肌占全心脏面积或质量的百分率。结果兔血清GPT、GOT升高 ,高剂量组LDH、α HBD水平降低。结论复方丹参浓缩片具有较好的抑制家兔心肌梗死作用和改善心肌酶谱的作用     

巴曲酶对急性心肌缺血犬冠脉节段阻力和流量的影响

犬冠状动脉定量狭窄造成急性心肌缺血,观察巴曲酶(batroxobin)对冠脉循环及血流动力学的影响。结果显示,batroxobin可剂量依赖性地增加缺血心脏冠脉血流量,2BU·kg^-1(0.1BU·kg^-1·min^-1)iv后40min,缺血犬冠脉流量比盐水对照组增加12%,此时小冠脉阻力由4.1±0.5降至3.2±0.5mmHg·min·ml^-1,而大冠脉阻力无明显变化;给药后120min,上述作用仍然持续,且冠脉总阻力降低13%,左室压上升及下降最大速率与盐水对照组相比分别增大14%和16%。结果表明,batroXobin在冠脉低灌流状态下仍可降低小冠脉阻力,增加冠脉流量,这可能是其改善缺血犬冠状循环及心脏功能的机理之一。     

槲皮素磷酸酯钾对实验性心肌梗塞的影响

iv10～20mg/kg(木解)皮素磷酸酯钾使兔急性心肌梗塞范围明显缩小,ST段明显降低,并能对抗冠脉结扎后引起的血清CPK含量增加及心律失常,这些作用与普萘洛尔相似。但iv40mg/kg后作用不明显。     

EFFECT OF LIGNOCAINE ON CORONARY BLOOD FLOW, SYSTOLIC MYOCARDIAL FUNCTION AND MYOCARDIAL HIGH ENERGY PHOSPHATE STORES IN SWINE

1. To investigate the effect of lignocaine upon coronary blood flow, myocardial systolic wall function and high energy phosphate stores, lignocaine was administered as a rapid intravenous injection to 14 open chest anaesthetized swine. 2. Before and after injection, measurements were made of coronary blood flow by electromagnetic flow probe, per cent wall thickening by ultrasonic crystals, adenosine triphosphate (ATP) and creatine phosphate (CP) content by myocardial biopsy, and arterial pressure by central aortic catheter. The animals were divided into two groups based on whether or not they received a continuous low-dose infusion of lignocaine prior to the study. Group I received the continuous low-dose infusion of lignocaine and group II did not. 3. With a 2 mg/kg lignocaine injection, peak diastolic coronary flow rose significantly in groups I and II by 27 +/- 7 and 29 +/- 7% respectively. This was followed by a significant decline in per cent wall thickening in groups I and II of -11 +/- 2 and -19 +/- 6% respectively. In group I myocardial CP content decreased after lignocaine injection by 58 +/- 6% and ATP tended to rise even though systolic and diastolic pressure did not change significantly. In group II neither CP nor ATP changed significantly, but systolic and diastolic blood pressure decreased significantly. 4. Repeat lignocaine injections were given over a wider dosage range (0.5-4.0 mg/kg) to determine dose-response for lignocaine versus coronary blood flow. Coronary blood flow increased and per cent wall thickening decreased as doses of lignocaine were increased. 5. It was concluded that rapid intravenous lignocaine injection appeared to cause a dose-dependent coronary dilatation and systolic dysfunction. Pre-treatment with low-dose continuous infusion of lignocaine appeared to result in a decrease in CP and a rise in ATP when compared with no pre-treatment--despite a similar effect on myocardial function and coronary blood flow.     

葛根素对急性心肌缺血狗区域性心肌血流与心脏血流动力学的作用

麻醉开胸狗ⅳ葛根素(puerarin)可减慢心率(HR)、降低主动脉压(MAP),用同位素标记微球法测得的缺血区侧枝冠脉血流量并不减少。从狗的右室旁路制备的心脏血流动力学实验发现葛根素明显减低张力一时间指数(TTI)与左室压力升高速度(LV dp/dt)。当MAP调整到给药前的水平时,TTI与LV dp/dt恢复,进入缺血区的侧技血流增加,非缺血区的冠脉血流量(CBF)亦增加。葛根素减低冠脉血管阻力(CVR)的作用比减低全身血管阻力(SVR)的作用更显著。葛根素不影响心肌收缩力,但增加局部心肌缺血时的侧枝血流并减少与心肌氧消耗有关的血流动力学参数。这些结果提示葛根素有益于治疗心肌缺血。     

硝基甘油对狗缺血区冠脉循环的作用

用实验性犬冠脉狭窄模型,冠脉内恒流灌注硝基甘油0.5μg/kg.min^-1,使冠脉血流量(CBF)增加、远端小动脉压(DCP)、冠脉血管总阻力(R_T)、小冠脉血管阻力(R_S)及冠状静脉低切血粘(η_b)减少;而主动脉压和心率无明显变化。恒流灌注硝基甘油1μg/kg.min^-1时,在开始5min内冠脉循环的变化同上,并伴大冠脉血管阻力(R_L)减少,10 min后出现CBF减少和R_T,R_{L及ηb增加。结果提示,硝基甘油有缓解和加重心肌缺血的双重作用,其作用可能与剂量张扩张远端小动脉压的程度有关。}     

THE EFFECT OF VASOPRESSIN ON HEPATIC ARTERY FLOW IN THE RAT

The effects of vasopressin infusion on hepatic artery flow was studied in rats. Hepatic artery ligation followed by the infusion of vasopressin (0.08 microU/g body weight per min) decreases portal venous flow and liver blood flow. Vasopressin infusion results in an increase in hepatic artery flow and liver blood flow both of which are abolished by subsequent hepatic artery ligation. The increase in hepatic artery flow and the decrease in portal venous flow following the infusion of vasopressin is discussed in relation to the management of patients presenting with bleeding oesophageal varices.     

亚硒酸钠对实验性冠脉痉挛诱发心肌细胞动作电位变化的影响

在豚鼠实验性冠状动脉痉挛动物模型上,用浮置微电极技术,观察心肌细胞AP的改变以及亚硒酸钠对此改变的影响。静脉注射垂体后叶素(0.3 U/kg)后,APH降低28%,APD_(50)与APD_(50)分别缩短17%与15%。静注亚硒酸钠,AP未见明显变化。但在亚硒酸钠注射的基础上再给予同剂量的垂体后叶素,则上述各项指标减少程度均较单独注射垂体后叶素为轻。结果提示亚硒酸钠对实验性冠脉痉挛所诱发的AP改变有一定对抗作用。     

亚硒酸钠对实验性冠脉痉挛诱发心肌细胞动作电位变化的影响

在豚鼠实验性冠状动脉痉挛动物模型上,用浮置微电极技术,观察心肌细胞AP的改变以及亚硒酸钠对此改变的影响。静脉注射垂体后叶素(0.3 U/kg)后,APH降低28%,APD₅₀与APD₅₀分别缩短17%与15%。静注亚硒酸钠,AP未见明显变化。但在亚硒酸钠注射的基础上再给予同剂量的垂体后叶素,则上述各项指标减少程度均较单独注射垂体后叶素为轻。结果提示亚硒酸钠对实验性冠脉痉挛所诱发的AP改变有一定对抗作用。     

尼群的平对麻醉犬冠脉流量、心肌耗氧量、二氧化碳产生率的影响

尼群的平20μg/kg iv显著降低麻醉犬血压的过程,冠状窦流量明显增加。持续3h,冠状窦氧含量增加,氧摄取率、心肌耗氧量、二氧化碳产生率降低,持续了3h以上,说明该剂适用于高血压伴心肌缺血。     

间尼索地平与尼索地平对清醒兔血流动力学和局部血流量的影响

应用放射性生物微球技术观察间尼索地平(m-Nis)和尼索地平(Nis)对清醒兔血流动力学和局部血流量的影响。m-Nis 1μg/kg·min~(-1)×10min iv显著增加清醒兔CO、CI、SV和LVSW;等剂量Nis增加CO及CI不显著;两药对清醒兔MABP、HR和脑、心、肾、脾等局部血流量影响相似,对这些器官的血流分布及心输出量分布无明显影响。