The pharmacology of mechanogated membrane ion channels.

作者: Owen P Hamill , Don W. Mcbride

DOI:

关键词: MechanotransductionTetrodotoxinPharmacologyIon channelReceptorChannel blockerAcetylcholine receptorAmilorideStretch-activated ion channelChemistry

摘要: In this article, the actions, mechanisms and applications of various ions drugs that interact with MG channels have been discussed. At present, no compound has found displays high specificity affinity exhibited by tetrodotoxin or alpha-bungarotoxin proved so useful in functional structural characterization voltage-gated Na+ channel acetylcholine receptor channel, respectively. Nevertheless, three different classes compounds discovered since Paintal's review clearly block channels. These compounds, represented amiloride, gentamicin gadolinium, act mainly on SA cation which appears to be shared many nonsensory some mechanosensory cells. Each class can distinguished voltage concentration dependence most likely involves blocking action. general, blocker pharmacology indicates a variety "receptor sites" The recognition acceptance such receptors should provide added impetus for continued screening more potent drugs, venoms toxins. case activators, little is understood amphipathic amphiphilic stimulate channels, although bilayer protein evoked. Even less role new K+ their modulation fatty acids plays physiological perhaps pathological processes. However, given general tend reduce excitability nerve muscle, plausible roles include acid regulation vascular tone control neuronal network excitability. both cases, detailed understanding required regarding stimuli modulate these through receptors. It may turn out and/or development cell-type specific agents activate will possess therapeutic potential. any case, observation chemically blocked activated wide range requires revision long-standing conclusion Paintal mechanotransduction process low susceptibility chemical influence.

参考文章(0)