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Chemical Compound Review

Efaroxan     2-(2-ethyl-3H-benzofuran-2- yl)-4,5-dihydro...

Synonyms: Efaroxano, Efaroxanum, CHEMBL57895, SureCN127096, BSPBio_003306, ...
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Disease relevance of Efaroxan


High impact information on Efaroxan

  • Administration of 100 micromol/l phentolamine was somewhat more effective than 100 micromol/l efaroxan to inhibit KATP channel activity in intact cultured beta-cells (reduction by 96 vs. 83%) [6].
  • In support of this, we now show that efaroxan can induce functional changes in the secretory pathway of pancreatic beta-cells that are independent of KATP channel blockade [7].
  • This response has been attributed to efaroxan-mediated blockade of KATP channels, with the subsequent gating of voltage-sensitive calcium channels [7].
  • Desensitization of the imidazoline receptor following exposure to high concentrations of efaroxan, however, was found to result in an increase in SUR1 protein expression and, as a consequence, an upregulation of K(ATP) channel density [8].
  • KATP channels were blocked by efaroxan (IC50 8.8 micromol/l, Hill slope -1.1) and by KU14R (IC50 31.9 micromol/l, Hill slope -1.5) [9].

Chemical compound and disease context of Efaroxan


Biological context of Efaroxan

  • Central administration of efaroxan on day 9 and day 23 of treatment produced a greater increase in blood pressure than did 2-MI with all three antihypertensive agents [13].
  • 4. Comparison of the effects of S-21663 to that of efaroxan, another imidazoline compound shown to act on insulin release in a glucose-dependent way via binding sites distinct from the imidazoline I1 and I2 sites, suggested that S-21663 acts through a novel site which displays a remarkably stable expression along the cell culture [14].
  • Culture with 100 microM BTS 67 582 or 100 microM tolbutamide did not affect basal insulin secretion, cellular insulin content, or cell viability and exerted no influence on the secretory responsiveness to 200 microM of the imidazoline, efaroxan [15].
  • Topically and intracisternally administered naphazoline was examined for its ability to alter intraocular pressure (IOP) of rabbits in the absence and presence of receptor antagonists (rauwolscine, efaroxan) and a G(i/o)ribosylating agent PTX [16].
  • Furthermore, the efaroxan-induced insulin release or vasoconstriction was not affected by the blockade of alpha 2- and alpha 1-adrenoceptors [17].

Anatomical context of Efaroxan

  • Interleukin (IL)-1beta-treated rat islets of Langerhans were exposed in vitro either to the imidazoline compound, Efaroxan, or to the selective inducible nitric oxide synthase (iNOS) inhibitor, 1400W, in a medium containing a high concentration of glucose (16.7 mmol/L) [2].
  • We found high affinities for unlabeled p-iodoclonidine (subnanomolar), clonidine (0.2 nM), and efaroxan (11 nM), but idazoxan did not compete significantly for the p-[125I]iodoclonidine binding in these membranes [18].
  • Metabolic inhibition of intact B-cells by 250muM NaCN, most likely by a decrease of the ATP/ADP ratio, significantly diminished the K(ATP) channel-blocking effect of a low concentration of alinidine (10muM), whereas efaroxan proved to be susceptible even at a highly effective concentration (100muM) [19].
  • Sensitive and specific methods for the determination of efaroxan and idazoxan in blood plasma have been developed based on solvent extraction, chromatographic separation and quantification by selected-ion monitoring using a quadruple mass-selective detector [20].
  • These effects were dose-dependent, and were significantly reversed by efaroxan (an I1-imidazoline and alpha2-adrenergic blocker) administered via the vertebral artery [21].

Associations of Efaroxan with other chemical compounds

  • Essential role of the imidazoline moiety in the insulinotropic effect but not the KATP channel-blocking effect of imidazolines; a comparison of the effects of efaroxan and its imidazole analogue, KU14R [9].
  • The action of moxonidine on ERK activation was blocked by the I1-receptor antagonist efaroxan and by D609, an inhibitor of phosphatidylcholine-selective phospholipase C (PC-PLC), previously implicated as the initial event in I1-receptor signaling [22].
  • Antagonism of the stimulatory effects of efaroxan and glibenclamide in rat pancreatic islets by the imidazoline, RX801080 [23].
  • The antagonism between K(ATP) channel-blocking insulinotropic imidazolines - phentolamine, alinidine, idazoxan and efaroxan - and K(ATP) channel openers, diazoxide and nucleoside diphosphates, was studied in mouse pancreatic islets and B-cells [19].
  • SK&F 86466 and efaroxan both antagonized moxonidine-induced inhibition of SP-elicited behavior in all mouse lines [24].

Gene context of Efaroxan


Analytical, diagnostic and therapeutic context of Efaroxan


  1. Relative importance of medullary brain nuclei for the sympatho-inhibitory actions of rilmenidine in the anaesthetized rabbit. Head, G.A., Burke, S.L. J. Hypertens. (1998) [Pubmed]
  2. Interleukin (IL)-1beta toxicity to islet beta cells: Efaroxan exerts a complete protection. Papaccio, G., Graziano, A., Valiante, S., D'Aquino, R., Travali, S., Nicoletti, F. J. Cell. Physiol. (2005) [Pubmed]
  3. Relative importance of central imidazoline receptors for the antihypertensive effects of moxonidine and rilmenidine. Chan, C.K., Head, G.A. J. Hypertens. (1996) [Pubmed]
  4. Efaroxan, an alpha-2 antagonist, in the treatment of progressive supranuclear palsy. Rascol, O., Sieradzan, K., Peyro-Saint-Paul, H., Thalamas, C., Brefel-Courbon, C., Senard, J.M., Ladure, P., Montastruc, J.L., Lees, A. Mov. Disord. (1998) [Pubmed]
  5. Identification of the central imidazoline receptor subtype involved in modulation of halothane-epinephrine arrhythmias in rats. Kagawa, K., Hayashi, Y., Itoh, I., Iwasaki, M., Takada, K., Kamibayashi, T., Yamatodani, A., Mashimo, T. Anesth. Analg. (2005) [Pubmed]
  6. Glucose dependence of imidazoline-induced insulin secretion: different characteristics of two ATP-Sensitive K+ channel-blocking compounds. Bleck, C., Wienbergen, A., Rustenbeck, I. Diabetes (2004) [Pubmed]
  7. Characterization of a KATP channel-independent pathway involved in potentiation of insulin secretion by efaroxan. Chan, S.L., Mourtada, M., Morgan, N.G. Diabetes (2001) [Pubmed]
  8. ATP-sensitive potassium channels and efaroxan-induced insulin release in the electrofusion-derived BRIN-BD11 beta-cell line. Chapman, J.C., McClenaghan, N.H., Cosgrove, K.E., Hashmi, M.N., Shepherd, R.M., Giesberts, A.N., White, S.J., Ammälä, C., Flatt, P.R., Dunne, M.J. Diabetes (1999) [Pubmed]
  9. Essential role of the imidazoline moiety in the insulinotropic effect but not the KATP channel-blocking effect of imidazolines; a comparison of the effects of efaroxan and its imidazole analogue, KU14R. Bleck, C., Wienbergen, A., Rustenbeck, I. Diabetologia (2005) [Pubmed]
  10. Role of imidazoline receptors in the cardiovascular actions of moxonidine, rilmenidine and clonidine in conscious rabbits. Chan, C.K., Sannajust, F., Head, G.A. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  11. Antiarrhythmic effect of the selective I1-imidazoline receptor modulator moxonidine on ouabain-induced cardiac arrhythmia in guinea pigs. Mest, H.J., Thomsen, P., Raap, A. Ann. N. Y. Acad. Sci. (1995) [Pubmed]
  12. Potential role of imidazoline (I1) receptors in modulating aqueous humor dynamics. Campbell, W.R., Potter, D.E. Journal of ocular pharmacology. (1994) [Pubmed]
  13. Importance of imidazoline-preferring receptors in the cardiovascular actions of chronically administered moxonidine, rilmenidine and clonidine in conscious rabbits. Parkin, M.L., Godwin, S.J., Head, G.A. J. Hypertens. (2003) [Pubmed]
  14. Stimulation of insulin release from the MIN6 cell line by a new imidazoline compound, S-21663: evidence for the existence of a novel imidazoline site in beta cells. Le Brigand, L., Virsolvy, A., Peyrollier, K., Manechez, D., Godfroid, J.J., Guardiola-Lemaître, B., Bataille, D. Br. J. Pharmacol. (1997) [Pubmed]
  15. Induced desensitization of the insulinotropic effects of antidiabetic drugs, BTS 67 582 and tolbutamide. McClenaghan, N.H., Ball, A.J., Flatt, P.R. Br. J. Pharmacol. (2000) [Pubmed]
  16. Naphazoline-induced suppression of aqueous humor pressure and flow: involvement of central and peripheral alpha(2)/I(1) receptors. Ogidigben, M.J., Chu, T.C., Potter, D.E. Exp. Eye Res. (2001) [Pubmed]
  17. Effects of imidazolines and derivatives on insulin secretion and vascular resistance in perfused rat pancreas. Berdeu, D., Gross, R., Ribes, G., Loubatières-Mariani, M.M., Bertrand, G. Eur. J. Pharmacol. (1994) [Pubmed]
  18. Evidence for the existence of imidazoline-specific binding sites in synaptosomal plasma membranes of the bovine brainstem. Heemskerk, F.M., Dontenwill, M., Greney, H., Vonthron, C., Bousquet, P. J. Neurochem. (1998) [Pubmed]
  19. Antagonism of the insulinotropic action of first generation imidazolines by openers of K(ATP) channels. Wienbergen, A., Bleck, C., Lackmann, T.G., Rustenbeck, I. Biochem. Pharmacol. (2007) [Pubmed]
  20. Determination of underivatised efaroxan and idazoxan in blood plasma by capillary gas chromatography with mass-selective detection. Nichols, J.D., Hyde, N.A., Sugden, K. The Analyst. (1989) [Pubmed]
  21. I1-imidazoline receptors and cholinergic outflow to the airways. Haxhiu, M.A., Dreshaj, I.A., McFadden, C.B., Erokwu, B.O., Ernsberger, P. J. Auton. Nerv. Syst. (1998) [Pubmed]
  22. The I1-imidazoline receptor in PC12 pheochromocytoma cells activates protein kinases C, extracellular signal-regulated kinase (ERK) and c-jun N-terminal kinase (JNK). Edwards, L., Fishman, D., Horowitz, P., Bourbon, N., Kester, M., Ernsberger, P. J. Neurochem. (2001) [Pubmed]
  23. Antagonism of the stimulatory effects of efaroxan and glibenclamide in rat pancreatic islets by the imidazoline, RX801080. Brown, C.A., Chan, S.L., Stillings, M.R., Smith, S.A., Morgan, N.G. Br. J. Pharmacol. (1993) [Pubmed]
  24. Moxonidine, a selective alpha2-adrenergic and imidazoline receptor agonist, produces spinal antinociception in mice. Fairbanks, C.A., Wilcox, G.L. J. Pharmacol. Exp. Ther. (1999) [Pubmed]
  25. The I(1)-imidazoline receptor in PC12 pheochromocytoma cells reverses NGF-induced ERK activation and induces MKP-2 phosphatase. Edwards, L., Ernsberger, P. Brain Res. (2003) [Pubmed]
  26. Identification of the monomeric G-protein, Rhes, as an efaroxan-regulated protein in the pancreatic beta-cell. Chan, S.L., Monks, L.K., Gao, H., Deaville, P., Morgan, N.G. Br. J. Pharmacol. (2002) [Pubmed]
  27. Involvement of phosphatidylcholine-selective phospholipase C in activation of mitogen-activated protein kinase pathways in imidazoline receptor antisera-selected protein. Li, F., Wu, N., Su, R.B., Zheng, J.Q., Xu, B., Lu, X.Q., Cong, B., Li, J. J. Cell. Biochem. (2006) [Pubmed]
  28. Augmentation of moxonidine-induced increase in ANP release by atrial hypertrophy. Cao, C., Kang, C.W., Kim, S.Z., Kim, S.H. Am. J. Physiol. Heart Circ. Physiol. (2004) [Pubmed]
  29. [3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor. Wainscott, D.B., Sasso, D.A., Kursar, J.D., Baez, M., Lucaites, V.L., Nelson, D.L. Naunyn Schmiedebergs Arch. Pharmacol. (1998) [Pubmed]
  30. Affinity isolation of imidazoline binding proteins from rat brain using 5-amino-efaroxan as a ligand. Monks, L.K., Cosgrove, K.E., Dunne, M.J., Ramsden, C.A., Morgan, N.G., Chan, S.L. FEBS Lett. (1999) [Pubmed]
  31. Stimulatory effect of harmane and other beta-carbolines on locus coeruleus neurons in anaesthetized rats. Ruiz-Durántez, E., Ruiz-Ortega JA, n.u.l.l., Pineda, J., Ugedo, L. Neurosci. Lett. (2001) [Pubmed]
  32. Selective antihypertensive action of moxonidine is mediated mainly by I1-imidazoline receptors in the rostral ventrolateral medulla. Haxhiu, M.A., Dreshaj, I., Schäfer, S.G., Ernsberger, P. J. Cardiovasc. Pharmacol. (1994) [Pubmed]
  33. Sensitivity improvement of circular dichroism detection in HPLC by using a low-pass electronic noise filter: Application to the enantiomeric determination purity of a basic drug. Lorin, M., Delepee, R., Maurizot, J.C., Ribet, J.P., Morin, P. Chirality (2007) [Pubmed]
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