氨氯吡咪类似物在体外可引起犬冠状动脉内皮依赖性舒张：钠/钙交换的可能作用。
Amiloride analogues cause endothelium-dependent relaxation in the canine coronary artery in vitro: possible role of Na+/Ca2+ exchange.
作者信息
Cocks T M, Little P J, Angus J A, Cragoe E J
机构信息
Baker Medical Research Institute, Victoria, Australia.
出版信息
Br J Pharmacol. 1988 Sep;95(1):67-76. doi: 10.1111/j.1476-5381.1988.tb16549.x.
Abstract
- A number of amiloride analogues were used to test the proposal that Na+/Ca2+ exchange may play a role in the secretion of endothelium-derived relaxing factor (EDRF). The analogues used were those substituted on either the 5-amino group or the terminal guanidino nitrogen atom. The former block both Na+/Ca2+ and Na+/H+ exchange whilst the latter block the Na+ channel and the Na+/Ca2+ exchange. 2. Both series of compounds caused relaxation in isolated rings of dog coronary artery (EC50 values, 1-10 microM) presumably due to release of EDRF since removal of endothelium greatly attenuated the response. 3. Amiloride (1-100 microM) had little effect on either endothelium-intact or denuded arteries. 4. The guanidino substituted analogues also appeared to block selectively the relaxation response to acetylcholine in the coronary artery, independently of their EDRF-releasing activity. 5. It is proposed that endothelial cells have an active Na+/Ca2+ exchange operating in the forward mode to extrude Ca2+. This mechanism may be important in the control of EDRF release.
摘要
- 用多种氨氯地平类似物来检验关于Na⁺/Ca²⁺交换可能在内皮衍生舒张因子（EDRF）分泌中起作用的假说。所用类似物是在5-氨基或末端胍基氮原子上被取代的那些。前者阻断Na⁺/Ca²⁺和Na⁺/H⁺交换，而后者阻断Na⁺通道和Na⁺/Ca²⁺交换。2. 这两类化合物都能使犬冠状动脉离体环舒张（半数有效浓度值，1 - 10微摩尔），推测是由于EDRF的释放，因为去除内皮会大大减弱这种反应。3. 氨氯地平（1 - 100微摩尔）对内皮完整或去内皮的动脉几乎没有影响。4. 胍基取代类似物似乎还能选择性地阻断冠状动脉对乙酰胆碱的舒张反应，这与其释放EDRF的活性无关。5. 有人提出内皮细胞有一个以正向模式运作以排出Ca²⁺的活跃Na⁺/Ca²⁺交换。这种机制可能在控制EDRF释放中很重要。
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本文引用的文献
1
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Annu Rev Physiol. 1982;44:435-49. doi: 10.1146/annurev.ph.44.030182.002251.
2
Endothelium-dependent relaxation of coronary arteries by noradrenaline and serotonin.去甲肾上腺素和血清素对冠状动脉的内皮依赖性舒张作用。
Nature. 1983;305(5935):627-30. doi: 10.1038/305627a0.
3
Glycine-directed peptide amidation: presence in rat brain of two enzymes that convert p-Glu-His-Pro-Gly-OH into p-Glu-His-Pro-NH2 (thyrotropin-releasing hormone).甘氨酸导向的肽酰胺化作用：大鼠脑中存在两种将对-谷氨酸-组氨酸-脯氨酸-甘氨酸-OH 转化为对-谷氨酸-组氨酸-脯氨酸-NH2（促甲状腺激素释放激素）的酶。
Proc Natl Acad Sci U S A. 1984 May;81(10):3228-32. doi: 10.1073/pnas.81.10.3228.
4
5
6
Comparison of angiotensin converting enzyme inhibitors captopril and MK421-diacid in guinea pig atria.豚鼠心房中血管紧张素转换酶抑制剂卡托普利和MK421-二酸的比较。
Eur J Pharmacol. 1982 Jul 16;81(3):487-92. doi: 10.1016/0014-2999(82)90114-5.
7
Mechanisms of transmembrane calcium movement in cultured chick embryo ventricular cells.培养的鸡胚心室细胞中跨膜钙转运的机制。
J Physiol. 1982 Apr;325:243-60. doi: 10.1113/jphysiol.1982.sp014148.
8
Refractory period fluid stimulation of right atria: a method for studying presynaptic receptors in cardiac autonomic transmission.
J Pharmacol Methods. 1981 Aug;6(1):51-64. doi: 10.1016/0160-5402(81)90084-x.
9
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Biochemistry. 1984 Sep 11;23(19):4481-8. doi: 10.1021/bi00314a038.
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