Rodger I W
Department of Physiology & Pharmacology, Royal College, University of Strathclyde, Glasgow, Scotland.
Drug Des Deliv. 1990 Mar;5(3):169-93.
Homeostatic regulation of Ca2+ levels within airway smooth muscle cells, and the consequences of changes in intracellular Ca2+ levels are reviewed, and a number of mechanisms are identified as targets for drug action. In the prophylaxis of asthma--by preventing the induction of contraction--the opportunities relate to receptor antagonism, the inhibition of Ca2+ influx, the inhibition of intracellular Ca2+ release, calmodulin antagonism, and the antagonism of contractile proteins. In the symptomatic relief of asthma--by reversal of established contractile responses--the opportunities relate to the inhibition of Ca2+ influx, the inhibition of inositol trisphosphate metabolism, the inhibition of protein kinase C, and the augmentation of Ca2+ removal mechanisms.
本文综述了气道平滑肌细胞内钙离子水平的稳态调节以及细胞内钙离子水平变化的后果，并确定了一些作为药物作用靶点的机制。在哮喘预防方面——通过防止收缩的诱导——机会涉及受体拮抗、钙离子内流的抑制、细胞内钙离子释放的抑制、钙调蛋白拮抗以及收缩蛋白的拮抗。在哮喘症状缓解方面——通过逆转已建立的收缩反应——机会涉及钙离子内流的抑制、肌醇三磷酸代谢的抑制、蛋白激酶C的抑制以及钙离子清除机制的增强。
