Description
1-EBIO is an activator of Ca2+-sensitive K+ channels (EC50 = 490 μM in T84 human carcinoma cells).This action is sensitive to the neurotoxin charybdotoxin (Ki = 3.5 nM). In mouse colonic epithelia, 1-EBIO also activates cAMP-sensitive K+ channels, a response this is inhibited by 293B.In this type of epithelium, but not mouse nasal epithelia, 1-EBIO activates both types of channels, resulting in large Cl- secretory currents.It also activates the human intermediate conductance Ca2+-activated K+ channel (EC50 = 74 μM).1-EBIO is currently used to study the role of these types of K+ channels in diverse physiological functions.
Biological Activity
Activator of epithelial K Ca channels, stimulates a large and sustained trans-epithelial Cl - secretory response across T84 monolayers. Induces hyperpolarization to the same magnitude as ACh in aortic value endothelial cells.
References
[1] ADEAGBO A S O. 1-Ethyl-2-benzimidazolinone stimulates endothelial KCa channels and nitric oxide formation in rat mesenteric vessels[J]. European journal of pharmacology, 1999, 379 2: Pages 151-159. DOI:
10.1016/s0014-2999(99)00489-6[2] J. E. ORFILA. Increasing small conductance Ca2+-activated potassium channel activity reverses ischemia-induced impairment of long-term potentiation[J]. European Journal of Neuroscience, 2014, 40 8: 3179-3188. DOI:
10.1111/ejn.12683[3] DUANE ALLEN. SK2 channels are neuroprotective for ischemia-induced neuronal cell death.[J]. Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism, 2011: 2302-2312. DOI:
10.1038/jcbfm.2011.90[4] MARTIN MÜLLER. Ca2+ activated K channels-new tools to induce cardiac commitment from pluripotent stem cells in mice and men.[J]. Stem Cell Reviews and Reports, 2012: 720-740. DOI:
10.1007/s12015-011-9324-9[5] ALEX J FAY. SK channels mediate NADPH oxidase-independent reactive oxygen species production and apoptosis in granulocytes.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2006: 17548-17553. DOI:
10.1073/pnas.0607914103
