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[钙拮抗剂的实验药理学]

[Experimental pharmacology of calcium antagonists].

作者信息

Godfraind T

机构信息

Laboratoire de Pharmacologie, Université Catholique de Louvain, Bruxelles, Belgique.

出版信息

Therapie. 1993 Nov-Dec;48 Spec No:637-49.

PMID:8091349
Abstract

Calcium antagonists (calcium channel blockers) constitute a chemically heterogeneous group of drugs which block voltage-operated calcium channels of L-type. They specifically interact with the alpha 1 subunit of the calcium channel. Their mechanism of action has been demonstrated using pharmacological, electrophysiological and radiochemical techniques. Their therapeutic effects are not only related to their hemodynamic action but also to their remodeling effect in hypertrophic heart and arteries, to their anti-ischaemic action and to the preservation of vascular integrity during several pathologies. Drugs belonging to the second generation of calcium antagonists show various pharmacological profiles responsible for their tissue selectivity. The latter is a rational basis for novel therapeutic indications including atherosclerosis and cardiac failure.

摘要

钙拮抗剂(钙通道阻滞剂)是一类化学结构各异的药物,可阻断L型电压门控钙通道。它们特异性地与钙通道的α1亚基相互作用。其作用机制已通过药理学、电生理学和放射化学技术得以证实。它们的治疗作用不仅与其血流动力学作用有关,还与其对肥厚心脏和动脉的重塑作用、抗缺血作用以及在多种病理状态下对血管完整性的保护作用有关。属于第二代钙拮抗剂的药物具有多种药理学特性,这决定了它们的组织选择性。后者是包括动脉粥样硬化和心力衰竭在内的新治疗适应症的合理依据。

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