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新型二氢吡啶CGP 28392对人血小板钙内流的增强作用。

Enhancement of calcium influx in human platelets by CGP 28392, a novel dihydropyridine.

作者信息

Erne P, Bürgisser E, Bühler F R, Dubach B, Kühnis H, Meier M, Rogg H

出版信息

Biochem Biophys Res Commun. 1984 Feb 14;118(3):842-7. doi: 10.1016/0006-291x(84)91471-2.

DOI:10.1016/0006-291x(84)91471-2
PMID:6322768
Abstract

CGP 28392, a novel compound structurally related to the dihydropyridine Ca2+-entry blockers, causes a dose-dependent increase in intracellular free Ca2+ in human platelets, as measured with the Quin-2 Ca2+ indicator, with a semimaximal effective concentration of 2.2 X 10(-7) M. This effect occurs in a concentration range in which CGP 28392 competes for specific [3H]nitrendipine binding in guinea pig heart membranes. It can be inhibited by nitrendipine. The data presented furnish direct evidence of the Ca2+-entry-stimulating properties of CGP 28392 and indicate the presence of dihydropyridine-susceptible structures in human platelets.

摘要

CGP 28392是一种在结构上与二氢吡啶类钙内流阻滞剂相关的新型化合物,在用喹啉-2钙指示剂测定时,它会使人类血小板内的游离钙浓度呈剂量依赖性增加,其半数有效浓度为2.2×10⁻⁷M。这种效应发生在CGP 28392与豚鼠心脏膜片中特异性[³H]尼群地平结合发生竞争的浓度范围内。它可被尼群地平抑制。所呈现的数据为CGP 28392的钙内流刺激特性提供了直接证据,并表明人类血小板中存在对二氢吡啶敏感的结构。

相似文献

1
Enhancement of calcium influx in human platelets by CGP 28392, a novel dihydropyridine.新型二氢吡啶CGP 28392对人血小板钙内流的增强作用。
Biochem Biophys Res Commun. 1984 Feb 14;118(3):842-7. doi: 10.1016/0006-291x(84)91471-2.
2
The influence of CGP 28392, a 1,4-dihydropyridine, on human platelet calcium and cyclic AMP metabolism.
Eur J Pharmacol. 1985 Jul 31;113(3):383-93. doi: 10.1016/0014-2999(85)90086-x.
3
In vitro comparative studies of the calcium-entry activators YC-170, CGP 28392, and BAY K 8644.钙离子内流激活剂 YC-170、CGP 28392 和 BAY K 8644 的体外比较研究。
J Cardiovasc Pharmacol. 1985;7 Suppl 6:S31-7. doi: 10.1097/00005344-198500076-00006.
4
Inotropic effect, binding properties, and calcium flux effects of the calcium channel agonist CGP 28392 in intact cultured embryonic chick ventricular cells.钙通道激动剂CGP 28392在完整培养的胚胎鸡心室细胞中的变力效应、结合特性及钙通量效应
Circ Res. 1985 May;56(5):676-82. doi: 10.1161/01.res.56.5.676.
5
Effects of the calcium-channel agonist CGP 28392 on insulin secretion from isolated rat islets of Langerhans.钙通道激动剂CGP 28392对离体大鼠胰岛胰岛素分泌的影响。
Biochem J. 1985 Nov 1;231(3):629-34. doi: 10.1042/bj2310629.
6
Activation of the voltage-dependent Ca2+ channel in rat heart cells by dihydropyridine derivatives.二氢吡啶衍生物对大鼠心脏细胞中电压依赖性钙通道的激活作用。
Biochem Biophys Res Commun. 1984 Nov 30;125(1):405-12. doi: 10.1016/s0006-291x(84)80382-4.
7
High-affinity antibodies to the 1,4-dihydropyridine Ca2+-channel blockers.针对1,4 - 二氢吡啶类钙离子通道阻滞剂的高亲和力抗体。
Proc Natl Acad Sci U S A. 1986 May;83(9):2792-6. doi: 10.1073/pnas.83.9.2792.
8
Differentiation of receptor sites for [3H]nitrendipine in chick hearts and physiological relation to the slow Ca2+ channel and to excitation-contraction coupling.鸡心脏中[3H]尼群地平受体位点的分化及其与慢钙通道和兴奋-收缩偶联的生理关系。
Eur J Biochem. 1984 Mar 15;139(3):673-81. doi: 10.1111/j.1432-1033.1984.tb08056.x.
9
Specific binding of a calcium channel activator, [3H]BAY k 8644, to membranes from cardiac muscle and brain.
Biochem Biophys Res Commun. 1984 May 31;121(1):317-23. doi: 10.1016/0006-291x(84)90725-3.
10
Effects of temperature and allosteric modulators on [3H] nitrendipine binding: methods for detecting potential Ca2+ channel blockers.温度和变构调节剂对[3H]尼群地平结合的影响:检测潜在钙通道阻滞剂的方法
J Recept Res. 1984;4(1-6):557-69. doi: 10.3109/10799898409042573.

引用本文的文献

1
Stimulation of insulin release by an organic calcium agonist.有机钙激动剂对胰岛素释放的刺激作用。
Diabetologia. 1985 Mar;28(3):153-6. doi: 10.1007/BF00273863.
2
Biphasic inotropic effects of a Ca2+ channel activator CGP28392 in rat myocardium: possible relation to intracellular Ca2+ release.Ca2+通道激活剂CGP28392对大鼠心肌的双相变力作用:与细胞内Ca2+释放的可能关系。
Br J Pharmacol. 1987 Nov;92(3):499-504. doi: 10.1111/j.1476-5381.1987.tb11349.x.
3
Effects of calcium channel antagonists and facilitators on beating of primary cultures of embryonic chick heart cells.
钙通道拮抗剂和促进剂对鸡胚心脏细胞原代培养物搏动的影响。
Br J Pharmacol. 1988 Nov;95(3):771-6. doi: 10.1111/j.1476-5381.1988.tb11703.x.
4
Effects of the calcium-channel agonist CGP 28392 on insulin secretion from isolated rat islets of Langerhans.钙通道激动剂CGP 28392对离体大鼠胰岛胰岛素分泌的影响。
Biochem J. 1985 Nov 1;231(3):629-34. doi: 10.1042/bj2310629.
5
The behavioral effects of the calcium agonist Bay K 8644 in the mouse: antagonism by the calcium antagonist nifedipine.钙激动剂Bay K 8644对小鼠的行为影响:钙拮抗剂硝苯地平的拮抗作用。
Naunyn Schmiedebergs Arch Pharmacol. 1985 Feb;328(4):373-7. doi: 10.1007/BF00692903.
6
The dihydropyridine derivative, Bay K 8644, enhances insulin secretion by isolated pancreatic islets.二氢吡啶衍生物Bay K 8644可增强分离的胰岛分泌胰岛素的能力。
Naunyn Schmiedebergs Arch Pharmacol. 1985 Jan;328(3):351-3. doi: 10.1007/BF00515566.
7
Ca-agonists: a new class of inotropic drugs.钙激动剂:一类新型的正性肌力药物。
Basic Res Cardiol. 1989;84 Suppl 1:105-16. doi: 10.1007/BF02650350.
8
Paradoxical reversion of the inhibitory effects of dihydropyridine enantiomers on the calcium current in frog heart by CGP 28861.CGP 28861对二氢吡啶对映体抑制蛙心钙电流作用的反常逆转
Br J Pharmacol. 1989 Feb;96(2):253-5. doi: 10.1111/j.1476-5381.1989.tb11808.x.
9
Different insulin-secretory responses to calcium-channel blockers in islets of lean and obese (ob/ob) mice.瘦小鼠和肥胖(ob/ob)小鼠胰岛对钙通道阻滞剂的胰岛素分泌反应不同。
Biochem J. 1988 Jan 15;249(2):401-7. doi: 10.1042/bj2490401.
10
Oxytocin and cAMP stimulate monovalent cation movements through a Ca2+-sensitive, amiloride-insensitive channel in the apical membrane of toad urinary bladder.催产素和环磷酸腺苷通过蟾蜍膀胱顶端膜中对钙离子敏感、对氨氯吡脒不敏感的通道刺激单价阳离子运动。
Proc Natl Acad Sci U S A. 1987 Jan;84(1):313-7. doi: 10.1073/pnas.84.1.313.