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Chemical Compound Review

EBIO     3-ethyl-1H-benzoimidazol-2-one

Synonyms: Tocris-1041, CHEMBL452887, SureCN612643, AG-D-05595, ACMC-2097q9, ...
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Disease relevance of C13840


Psychiatry related information on C13840

  • Accordingly, this study has investigated the therapeutic potential of 1-EBIO using a range of in vivo seizure models, and assessed the adverse effect liability with the rotarod and locomotor activity paradigms [3].
  • 1-EBIO was found to be effective at reducing seizure incidence in mice following maximal electroshock (ED(50) 36.0 mg/kg) as well as increasing the threshold to electrically- and pentylenetetrazole-induced seizures (TID(10)s 7.3 and 21.5 mg/kg, respectively) [3].

High impact information on C13840

  • The effects of 1-EBIO and apamin are independent of the NADPH oxidase pathway, as demonstrated by using a PLB-985 cell line lacking the gp91phox subunit [4].
  • Consistent with the enhanced ROS production and K(+) efflux mediated by 1-EBIO, we found that this SK opener increased apoptosis of PLB-985 cells [4].
  • We report here that 1-ethyl-2-benzimidazolinone (1-EBIO), an activator of Ca(2+)-activated potassium channels of small conductance (SK) and intermediate conductance (IK), causes production of superoxide and hydrogen peroxide by neutrophils and granulocyte-differentiated PLB-985 cells [4].
  • The elucidation of SK channel function has recently benefited from the discovery of SK channel enhancers, the prototype of which is 1-EBIO [5].
  • After 3 days of treatment with 1-EBIO, mRNA levels of hIK1 were substantially diminished and no channel activity was detected [6].

Biological context of C13840


Anatomical context of C13840

  • OBJECTIVE: To confirm the identity of this channel as iKCA1 in human lung mast cells and to examine the effect of an iKCA1 opener, 1-ethyl-2-benzimidazolinone (1-EBIO), on Ca2+ influx and degranulation after IgE-dependent activation [11].
  • The increased IKCa1 expression levels following exposure to high levels of LSS resulted in enhanced IK(Ca) whole-cell currents and in an increased hyperpolarization of the endothelium in response to ATP and the IK(Ca) opener 1-EBIO [12].
  • 3. In endothelium-intact arteries, smooth muscle relaxation to 1-EBIO was not altered by either of the potassium channel blockers ChTX (100 nM; n=7), or IbTX (100 nM; n=4), or raised extracellular K(+) (25 mM) [13].
  • 4. In freshly isolated mesenteric endothelial cells, 1-EBIO (600 microM) evoked a ChTX-sensitive outward K-current [13].
  • Experiments were conducted to determine whether the Cl- secretagogue, 1-ethyl-2-benzimidazolinone (EBIO), stimulates Cl- transport in the rabbit conjunctival epithelium [14].

Associations of C13840 with other chemical compounds


Gene context of C13840

  • Transient expression of KCNN4 cloned from H441 cells conferred a Ca(2+)- and 1-EBIO-sensitive K(+) conductance on Chinese hamster ovary cells, but this channel was inactive when [Ca(2+)](i) was <0.2 muM [17].
  • To examine this issue, we have used the acute hippocampal slice model of epileptiform activity to investigate the effects of an enhancer of SK channel activity, 1-ethyl-benzimidazolinone (EBIO) [18].
  • Electrophysiological investigations showed that expression of amino acids 1-299 of SK3 (SK3N_299) modified the 1-EBIO pharmacology of endogenous SK3 channels in PC12 cells without affecting the Ca(2+)-sensitvity [19].
  • The K+ channel opener 1-ethyl-2-benzimidazolinone further increased CaCC-mediated Cl- secretion in normal and CF tissues [20].
  • Salbutamol (1-10 microM) inhibited iKCa1 currents following activation with both anti-IgE and the iKCa1 opener 1-EBIO, and was reversed by removing salbutamol or by the addition of the selective beta2-adrenoceptor antagonist and inverse agonist ICI 118551 [21].

Analytical, diagnostic and therapeutic context of C13840


  1. Chlorzoxazone or 1-EBIO increases Na(+) absorption across cystic fibrosis airway epithelial cells. Gao, L., Yankaskas, J.R., Fuller, C.M., Sorscher, E.J., Matalon, S., Forman, H.J., Venglarik, C.J. Am. J. Physiol. Lung Cell Mol. Physiol. (2001) [Pubmed]
  2. Effects of intermediate-conductance Ca2+-activated K+ channel modulators on human prostate cancer cell proliferation. Parihar, A.S., Coghlan, M.J., Gopalakrishnan, M., Shieh, C.C. Eur. J. Pharmacol. (2003) [Pubmed]
  3. In vivo characterisation of the small-conductance K(Ca) (SK) channel activator 1-ethyl-2-benzimidazolinone (1-EBIO) as a potential anticonvulsant. Anderson, N.J., Slough, S., Watson, W.P. Eur. J. Pharmacol. (2006) [Pubmed]
  4. SK channels mediate NADPH oxidase-independent reactive oxygen species production and apoptosis in granulocytes. Fay, A.J., Qian, X., Jan, Y.N., Jan, L.Y. Proc. Natl. Acad. Sci. U.S.A. (2006) [Pubmed]
  5. Specific enhancement of SK channel activity selectively potentiates the afterhyperpolarizing current I(AHP) and modulates the firing properties of hippocampal pyramidal neurons. Pedarzani, P., McCutcheon, J.E., Rogge, G., Jensen, B.S., Christophersen, P., Hougaard, C., Strøbaek, D., Stocker, M. J. Biol. Chem. (2005) [Pubmed]
  6. Unexpected down-regulation of the hIK1 Ca2+-activated K+ channel by its opener 1-ethyl-2-benzimidazolinone in HaCaT keratinocytes. Inverse effects on cell growth and proliferation. Koegel, H., Kaesler, S., Burgstahler, R., Werner, S., Alzheimer, C. J. Biol. Chem. (2003) [Pubmed]
  7. Impaired EDHF-mediated vasodilation and function of endothelial Ca-activated K channels in uremic rats. Köhler, R., Eichler, I., Schönfelder, H., Grgic, I., Heinau, P., Si, H., Hoyer, J. Kidney Int. (2005) [Pubmed]
  8. Ca2+ release-dependent hyperpolarizations modulate the firing pattern of juvenile GABA neurons in mouse substantia nigra pars reticulata in vitro. Yanovsky, Y., Velte, S., Misgeld, U. J. Physiol. (Lond.) (2006) [Pubmed]
  9. Charybdotoxin-sensitive small conductance K(Ca) channel activated by bradykinin and substance P in endothelial cells. Sollini, M., Frieden, M., Bény, J.L. Br. J. Pharmacol. (2002) [Pubmed]
  10. Pharmacological modulation of ion transport across wild-type and DeltaF508 CFTR-expressing human bronchial epithelia. Devor, D.C., Bridges, R.J., Pilewski, J.M. Am. J. Physiol., Cell Physiol. (2000) [Pubmed]
  11. The K+ channel iKCA1 potentiates Ca2+ influx and degranulation in human lung mast cells. Mark Duffy, S., Berger, P., Cruse, G., Yang, W., Bolton, S.J., Bradding, P. J. Allergy Clin. Immunol. (2004) [Pubmed]
  12. Shear stress-induced up-regulation of the intermediate-conductance Ca(2+)-activated K(+) channel in human endothelium. Brakemeier, S., Kersten, A., Eichler, I., Grgic, I., Zakrzewicz, A., Hopp, H., Köhler, R., Hoyer, J. Cardiovasc. Res. (2003) [Pubmed]
  13. Activation of endothelial cell IK(Ca) with 1-ethyl-2-benzimidazolinone evokes smooth muscle hyperpolarization in rat isolated mesenteric artery. Walker, S.D., Dora, K.A., Ings, N.T., Crane, G.J., Garland, C.J. Br. J. Pharmacol. (2001) [Pubmed]
  14. Cl- secretory effects of EBIO in the rabbit conjunctival epithelium. Alvarez, L.J., Zamudio, A.C., Candia, O.A. Am. J. Physiol., Cell Physiol. (2005) [Pubmed]
  15. Further investigation of endothelium-derived hyperpolarizing factor (EDHF) in rat hepatic artery: studies using 1-EBIO and ouabain. Edwards, G., Gardener, M.J., Feletou, M., Brady, G., Vanhoutte, P.M., Weston, A.H. Br. J. Pharmacol. (1999) [Pubmed]
  16. Characterization of a charybdotoxin-sensitive intermediate conductance Ca2+-activated K+ channel in porcine coronary endothelium: relevance to EDHF. Bychkov, R., Burnham, M.P., Richards, G.R., Edwards, G., Weston, A.H., Félétou, M., Vanhoutte, P.M. Br. J. Pharmacol. (2002) [Pubmed]
  17. Expression of intermediate-conductance, Ca2+-activated K+ channel (KCNN4) in H441 human distal airway epithelial cells. Wilson, S.M., Brown, S.G., McTavish, N., McNeill, R.P., Husband, E.M., Inglis, S.K., Olver, R.E., Clunes, M.T. Am. J. Physiol. Lung Cell Mol. Physiol. (2006) [Pubmed]
  18. Activation of SK channels inhibits epileptiform bursting in hippocampal CA3 neurons. Lappin, S.C., Dale, T.J., Brown, J.T., Trezise, D.J., Davies, C.H. Brain Res. (2005) [Pubmed]
  19. Interactions of N-Terminal and C-Terminal Parts of the Small Conductance Ca Activated K(+) Channel, hSK3. Frei, E., Spindler, I., Grissmer, S., Jager, H. Cell. Physiol. Biochem. (2006) [Pubmed]
  20. Modulation of Ca2+-activated Cl- secretion by basolateral K+ channels in human normal and cystic fibrosis airway epithelia. Mall, M., Gonska, T., Thomas, J., Schreiber, R., Seydewitz, H.H., Kuehr, J., Brandis, M., Kunzelmann, K. Pediatr. Res. (2003) [Pubmed]
  21. Beta2-adrenoceptor regulation of the K+ channel iKCa1 in human mast cells. Duffy, S.M., Cruse, G., Lawley, W.J., Bradding, P. FASEB J. (2005) [Pubmed]
  22. 1-EBIO stimulates Cl- secretion by activating a basolateral K+ channel in the mouse jejunum. Hamilton, K.L., Meads, L., Butt, A.G. Pflugers Arch. (1999) [Pubmed]
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