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吡唑化合物pyr3干预对压力负荷诱导的大鼠左心室肥厚的影响 被引量:3
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作者 田小芍 陈明 刘春霞 《中国循环杂志》 CSCD 北大核心 2013年第3期226-229,共4页
目的:探讨瞬时受体电位通道C亚族3亚型(TRPC3)的选择性阻滞剂吡唑化合物Ethyl-1-(4-f2,3,3一trichloroacrylamide)phenyl)-5-(trifluoromethyl)-1H—pyrazole-4-carboxylate(pyr3)的体内干预对压力负荷大鼠左心室肥厚(LvH... 目的:探讨瞬时受体电位通道C亚族3亚型(TRPC3)的选择性阻滞剂吡唑化合物Ethyl-1-(4-f2,3,3一trichloroacrylamide)phenyl)-5-(trifluoromethyl)-1H—pyrazole-4-carboxylate(pyr3)的体内干预对压力负荷大鼠左心室肥厚(LvH)程度的影响。方法:采用腹主动脉缩窄手术建立左心压力负荷模型。30只200—240g雄性SD大鼠随机分为五组(n=6):假手术对照组、手术对照组、假手术后全程给药组、手术后后期给药组,手术后全程给药组。6周后,计算各组大鼠左心室质量指数、左心室心肌细胞横径,逆转录多聚酶连反应(RT—PCR)、免疫组织化学和蛋白免疫印迹检测TRPC3和钙调神经磷酸酶A13信使核糖核酸(mRNA)和蛋白的表达水平。结果:与假手术对照组相比,手术对照组左心室肥厚相关指标(左心室质量指数和左心室心肌细胞横径)及TRPC3、钙调神经磷酸酶AB蛋白和mRNA的表达显著升高;假手术后全程给药组左心室肥厚相关指标无显著变化,而TRPC3和钙调神经磷酸酶AB蛋白及mRNA的表达量显著升高,差异均有统计学意义(P均〈0.05)。与手术对照组比较,手术后全程给药组左心室肥厚相关指标、TRPC3及钙调神经磷酸酶A13蛋白和mRNA表达均明显降低(P均〈0.05);手术后后期给药组左心室肥厚相关指标及钙调神经磷酸酶AB蛋白和mRNA的表达下降,差异均有统计学意义(P均〈0.05),而TRPC3的蛋白和mRNA表达未见显著降低。结论:pyr3体内干预能够一定程度上阻止压力负荷导致的大鼠左心室肥厚,降低压力负荷大鼠左心室TRPC3和钙调神经磷酸酶AB表达的上调。 展开更多
关键词 Ethyl-1-(4-(2 3 3-trichloroacrylamide)phenyl)-5-(trifluoromethyl)-1H—pyrazole-4-carboxylate 压力负荷 左心室肥厚 瞬时受体电位通道C亚族3亚型 钙调神经磷酸酶Aβ
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A Selective TRPC3 Inhibitor Pyr3 Attenuates Myocardial Ischemia/Reperfusion Injury in Mice 被引量:3
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作者 Min LU Xiao-xia FANG +6 位作者 Dan-dan SHI Rui LIU Yan DING Qiu-fang ZHANG Han-qin WANG Jun-ming TANG Xi-ju HE 《Current Medical Science》 SCIE CAS 2020年第6期1107-1113,共7页
An emerging body of evidence indicates that transient receptor potential TRP channels act as important mediators for a wide variety of physiological functions and are potential targets for drug discovery.Our previous ... An emerging body of evidence indicates that transient receptor potential TRP channels act as important mediators for a wide variety of physiological functions and are potential targets for drug discovery.Our previous study has identified transient receptor potential channel 3(TRPC3)and TRPC6 as cation channels through which most of the damaging calcium enters,aggravates pathological changes in vivo and increases ischemia/reperfusion(I/R)injury in mice.This study aimed to verify the effects of TRPC3 inhibitor Pyr3 on myocardial I/R injury in mice.C57BL/6J wild-type male mice(8 to 12 weeks old)were anesthetized with 3.3%chloral hydrate.A murine I(30 min)/R(24 h)injury model was established by temporary occlusion of the left anterior descending(LAD)coronary artery.Pyr3 was administered at concentrations of 0,2.5,5,or 10 mg/kg via the right jugular vein 5 min before reperfusion.We observed that the selective TRPC3 inhibitor,10 mg/kg Pyr3,significantly decreased the infarct size of left ventricle,and reduced the myocardial cell apoptosis rate and inflammatory response in mice.In a conclusion,TRPC3 can function as a candidate target for I/R injury prevention,and Pyr3 may directly bind to TRPC3 channel protein,inhibit TRPC3 channel activity,and improve TRPC3-related myocardial I/R injury.Pyr3 may be used for clarification of TRPC3 functions and for treatments of TRPC3-mediated diseases. 展开更多
关键词 ischemia/reperfusion injury TRPC3 pyr3 APOPTOSIS
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兔肺静脉肌袖心肌细胞TRPC3离子流的特性
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作者 林勇 黄卫斌 +2 位作者 张蓉芳 曾松 刘泰槰 《中国心脏起搏与心电生理杂志》 2013年第4期334-337,共4页
目的采用TRPC3通道特异性阻断剂证实兔肺静脉肌袖细胞(PVC)与左房心肌细胞(LAC)上存在TRPC3通道,并进行比较,探讨TRPC3通道在由PVC起源的心律失常中可能的作用。方法酶解法分离PVC和LAC,采用全细胞膜片钳制技术,分别记录总背景电流(I BG... 目的采用TRPC3通道特异性阻断剂证实兔肺静脉肌袖细胞(PVC)与左房心肌细胞(LAC)上存在TRPC3通道,并进行比较,探讨TRPC3通道在由PVC起源的心律失常中可能的作用。方法酶解法分离PVC和LAC,采用全细胞膜片钳制技术,分别记录总背景电流(I BG)。用TRPC3通道特异性阻断剂吡唑类复合2-氨基-3甲基-5-氰基吡啶(Pyr3)确定该离子流中存在I TRPC3。结果研究发现,加入Pyr3灌流后LAC和PVC I BG电流密度均减少,被抑制的离子流部分即为I TRPC3,且PVC I TRPC3电流密度比LAC明显减小(-0.122 5±0.084 8 pA/pF vs-0.330 1±0.086 3 pA/pF,-60 mV,n=10,P<0.05;0.254 8±0.089 8 pA/pF vs 0.670 4±0.124 7 pA/pF,+60 mV,n=10,P<0.05)。结论 PVC和LAC存在TRPC3通道,且两者I TRPC3电流密度的差异与PVC动作电位时程较长有关。 展开更多
关键词 电生理学 兔心脏 肺静脉肌袖心肌细胞 膜片钳制 瞬时感受器阳离子通道 吡唑类复合2-氨基-3甲基-5-氰基吡啶
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Syntheses and Crystal Structure of [Cu(pyr)_3]·Hg_2I_6
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作者 宋俊玲 曾卉一 +3 位作者 杨冰苹 董振超 郭国聪 黄锦顺 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 北大核心 2003年第1期29-32,共4页
A new compound containing discrete cationic and anionic complexes, [Cu(pyr)3]Hg2I6 (C30H24CuHg2I6N6), where pyr = 2,2-bipyridine, was prepared by the reaction of CuBr with pyr and HgI2 in a mixed solvent of acetone, m... A new compound containing discrete cationic and anionic complexes, [Cu(pyr)3]Hg2I6 (C30H24CuHg2I6N6), where pyr = 2,2-bipyridine, was prepared by the reaction of CuBr with pyr and HgI2 in a mixed solvent of acetone, methanol and acetonitrile. Single-crystal X-ray diffraction analysis indicates that it crystallizes in an orthorhombic system, Pna21 (No. 33), a = 33.1595(7), b = 9.4605(1), c = 13.0899(2) ? V = 4106.4(1) 3, Mr = 1694.67, Dc = 2.741 g/cm3, Z = 4, F(000) = 3012, m(MoKa) = 12.511 mm-1, R = 0.0736, wR = 0.1360 (I > 2(I)) and S = 1.218. The structure consists of discrete [Hg2I6]2- anions and [Cu(bipyridine)3]2+ cations. The double tetrahedral [Hg2I6]2- unit is formed by sharing one tetrahedral edge and possesses approximate D2h symmetry. The mononuclear Cu2+ ion is coordinated by six N atoms from three pyr molecules to form a slightly disordered octahedral geometry. 展开更多
关键词 [Cu(pyr)3].Hg2I6 铜配合物 合成 晶体结构 X射线衍射 吡啶
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