{"title":"气道平滑肌兴奋-收缩耦合机制:药物设计的新靶点。","authors":"I W Rodger","doi":"","DOIUrl":null,"url":null,"abstract":"<p><p>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.</p>","PeriodicalId":11271,"journal":{"name":"Drug design and delivery","volume":"5 3","pages":"169-93"},"PeriodicalIF":0.0000,"publicationDate":"1990-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Excitation-contraction coupling mechanisms in airway smooth muscle: new targets in drug design.\",\"authors\":\"I W Rodger\",\"doi\":\"\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>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.</p>\",\"PeriodicalId\":11271,\"journal\":{\"name\":\"Drug design and delivery\",\"volume\":\"5 3\",\"pages\":\"169-93\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1990-03-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Drug design and delivery\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Drug design and delivery","FirstCategoryId":"1085","ListUrlMain":"","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Excitation-contraction coupling mechanisms in airway smooth muscle: new targets in drug design.
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.