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钙通道拮抗剂PN 200 - 110的血管床及血管收缩剂依赖性选择性

Vascular bed and vasoconstrictor-dependent selectivity of the calcium channel antagonist, PN 200-110.

作者信息

Bijak A, Pasternac A, McPherson G A, Bevan J A

出版信息

Eur J Pharmacol. 1986 Dec 16;132(2-3):313-7. doi: 10.1016/0014-2999(86)90623-0.

DOI:10.1016/0014-2999(86)90623-0
PMID:2949990
Abstract

The potency of the dihydropyridine calcium channel blocker, PN 200-110 was assessed in vitro against contractions induced by potassium (20-55 mM) and histamine (1-300 microM) in rabbit thoracic aorta, coronary, basilar, renal and central ear arteries. PN 200-110 was particularly effective against potassium responses in the coronary and basilar arteries (IC50 30 and 50 pM) and of little effect against histamine responses in the renal artery and thoracic aorta (IC50 greater than 1 microM). These results suggest that PN 200-110 has some preferential actions dependent on both the vascular bed and also the constrictor used.

摘要

在体外评估了二氢吡啶类钙通道阻滞剂PN 200 - 110对兔胸主动脉、冠状动脉、基底动脉、肾动脉和中耳动脉中由钾(20 - 55 mM)和组胺(1 - 300 microM)诱导的收缩的作用。PN 200 - 110对冠状动脉和基底动脉中的钾反应特别有效(IC50分别为30和50 pM),而对肾动脉和胸主动脉中的组胺反应几乎没有作用(IC50大于1 microM)。这些结果表明,PN 200 - 110具有一些依赖于血管床和所用收缩剂的优先作用。

相似文献

1
Vascular bed and vasoconstrictor-dependent selectivity of the calcium channel antagonist, PN 200-110.钙通道拮抗剂PN 200 - 110的血管床及血管收缩剂依赖性选择性
Eur J Pharmacol. 1986 Dec 16;132(2-3):313-7. doi: 10.1016/0014-2999(86)90623-0.
2
In vitro effects of calcium antagonists PN 200-110, nifedipine, and nimodipine on human and canine cerebral arteries.钙拮抗剂PN 200 - 110、硝苯地平和尼莫地平对人和犬脑动脉的体外作用。
J Cereb Blood Flow Metab. 1983 Sep;3(3):354-61. doi: 10.1038/jcbfm.1983.51.
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Cardioprotection by the calcium antagonist PN 200-110 in the absence and presence of cardiodepression.在存在和不存在心脏抑制的情况下,钙拮抗剂PN 200 - 110的心脏保护作用。
Br J Pharmacol. 1985 Sep;86(1):181-9. doi: 10.1111/j.1476-5381.1985.tb09448.x.
4
Separation of the coronary vasodilator from the cardiac effects of PN 200-110, a new dihydropyridine calcium antagonist, in the dog heart.新型二氢吡啶类钙拮抗剂PN 200 - 110在犬心脏中冠状动脉扩张作用与心脏效应的分离
J Cardiovasc Pharmacol. 1985 Jan-Feb;7(1):190-6. doi: 10.1097/00005344-198501000-00030.
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Prolonged depolarization increases the pharmacological effect of dihydropyridines and their binding affinity for calcium channels of vascular smooth muscle.延长去极化会增加二氢吡啶类药物的药理作用及其对血管平滑肌钙通道的结合亲和力。
J Pharmacol Exp Ther. 1987 Nov;243(2):711-5.
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Stereoselectivity at the calcium channel: different profiles of hemodynamic activity of the enantiomers of the dihydropyridine derivative PN 200-110.钙通道的立体选择性:二氢吡啶衍生物PN 200 - 110对映体的不同血流动力学活性特征。
J Cardiovasc Pharmacol. 1986 Mar-Apr;8(2):221-6. doi: 10.1097/00005344-198603000-00001.
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Effects of calcium entry blockers on calcium-dependent contractions of rat portal vein.钙通道阻滞剂对大鼠门静脉钙依赖性收缩的影响。
Br J Pharmacol. 1987 Sep;92(1):203-11. doi: 10.1111/j.1476-5381.1987.tb11313.x.
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Cerebrovascular selectivity and vasospasmolytic action of the novel calcium antagonist (+/-)-(E)-1-(3-fluoro-6, 11-dihydrodibenz[b,e]oxepin-11-yl)-4-(3-phenyl-2-propenyl)-piperazine dimaleate in isolated cerebral arteries of the rabbit and dog.新型钙拮抗剂(±)-(E)-1-(3-氟-6,11-二氢二苯并[b,e]氧杂卓-11-基)-4-(3-苯基-2-丙烯基)-哌嗪二马来酸盐在兔和犬离体脑动脉中的脑血管选择性及血管痉挛解作用
Arzneimittelforschung. 1997 Apr;47(4):339-46.
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Central and peripheral cardiovascular effects of the enantiomers of the calcium antagonist PN 200-110.钙拮抗剂PN 200 - 110对映体的中枢和外周心血管效应
Eur J Pharmacol. 1988 May 20;150(1-2):43-50. doi: 10.1016/0014-2999(88)90748-0.
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PN 200-110, a new calcium antagonist: electrophysiological, inotropic, and chronotropic effects on guinea pig myocardial tissue and effects on contraction and calcium uptake of rabbit aorta.PN 200 - 110,一种新型钙拮抗剂:对豚鼠心肌组织的电生理、变力性和变时性作用以及对兔主动脉收缩和钙摄取的影响。
J Cardiovasc Pharmacol. 1984 May-Jun;6(3):399-406.

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