Effects of inhibitors of protein kinase C and Na +/H + exchange on α1‐adrenoceptor‐mediated inotropic responses in the rat left ventricular papillary muscle

Effects of inhibitors of protein kinase C and Na +/H + exchange on α1‐adrenoceptor‐mediated inotropic responses in the rat left ventricular papillary muscle
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蛋白激酶 C 抑制剂和 Na +/H + 交换对大鼠左心室乳头肌 α1 肾上腺素受体介导的正性肌力反应的影响

DOI:
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发表时间:
1990
影响因子:
7.3
通讯作者:
C. Inagaki
C. Inagaki
中科院分区:
医学2区
文献类型:
--
作者:
H. Otani;H. Otani;Toshiko Uriu;M. Hara;M. Inoue;K. Omori;E. Cragoe;C. Inagaki

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刺激大鼠左心室乳头肌的1 α1-肾上腺素能受体产生三相变力反应:最初的短暂正性变力效应(PIE),随后是短暂负性变力效应(NIE)和持续PIE。2蛋白激酶C抑制剂staurosporine在30 ~ 100 nm范围内对持续性PIE有抑制作用,对一过性PIE和NIE无明显影响。3 H-7,1-(5-异喹啉磺酰基)-2-甲基哌嗪是一种特异性低于星形孢菌素的蛋白激酶C抑制剂,在100 μm浓度下可抑制瞬时NIE和持续PIE,但不影响瞬时PIE。4钠/氢交换抑制剂阿米洛利在0.1 ~ 1 mM浓度范围内抑制持续性PIE,在更高浓度下也抑制短暂性NIE。5阿米洛利类似物5-(N-甲基-N-异丁基)阿米洛利(MIBA)仅抑制持续性PIE,IC 50为0.3 μm,比阿米洛利低约两个数量级。6通过蛋白激酶C激活的Na+/H+交换的受体相关刺激可能是α1-肾上腺素受体介导的持续PIE的机制。
1 α1‐Adrenoceptor stimulation of rat left ventricular papillary muscle produced a triphasic inotropic response: an initial transient positive inotropic effect (PIE) followed by a transient negative inotropic effect (NIE) and a sustained PIE. 2 The protein kinase C inhibitor, staurosporine, at concentrations ranging from 30 nm to 100 nm inhibited the sustained PIE, but had no significant effect on the transient PIE and NIE. 3 H‐7, 1‐(5‐isoquinoline sulphonyl)‐2‐methylpiperazine, a less specific inhibitor of protein kinase C than staurosporine, at a concentration of 100 μm inhibited both the transient NIE and the sustained PIE without affecting the transient PIE. 4 Amiloride, an inhibitor of Na+/H+ exchange, at concentrations ranging from 0.1 mm to 1 mm inhibited the sustained PIE and, at higher concentrations, also inhibited the transient NIE. 5 An amiloride analogue, 5‐(N‐methyl‐N‐isobutyl)amiloride (MIBA), inhibited only the sustained PIE with an IC50 of 0.3 μm which is approximately two orders of magnitude lower than amiloride. 6 The receptor‐linked stimulation of Na+/H+ exchange through protein kinase C activation may be a mechanism for α1‐adrenoceptor‐mediated sustained PIE.
卡巴胆碱对兔虹膜括约肌平滑肌肌醇三磷酸积累、肌球蛋白轻链磷酸化及收缩影响的相关研究
DOI: --
发表时间: 1986
期刊: The Journal of pharmacology and experimental therapeutics
影响因子: --
作者:
Howe,PH;Akhtar,RA;Naderi,S;Abdel-Latif,AA
通讯作者: Abdel-Latif,AA
Na /H 交换调节血管紧张素 II 刺激的血管平滑肌细胞中二酰甘油积累的证据。
DOI: --
发表时间: 1988
期刊: The Journal of biological chemistry
影响因子: --
作者:
Griendling,KK;Berk,BC;Alexander,RW
通讯作者: Alexander,RW