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Chemical Compound Review

bepridil     N-benzyl-N-[3-(2- methylpropoxy)-2...

Synonyms: Bepadin, Vascor, CHEMBL1008, Bepadin (TN), Bepridil (INN), ...
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Disease relevance of bepridil

  • Verapamil and bepridil failed to block the [Ca]i rise induced by anoxia and were equally ineffective on anoxic gene expression [1].
  • This study suggests that bepridil, 400 mg daily, is effective for the treatment of exercise-induced myocardial ischemia and angina pectoris [2].
  • CONCLUSION: Bepridil plasma concentrations needed in vitro to modulate MDR could be achieved in this study with tolerable toxicity; however, despite most tumors being MDR1/Pgp-positive, no response was obtained that could be attributed to the drug combination [3].
  • PURPOSE: To achieve an adequate plasma concentration of bepridil, a calcium channel blocker, which reverts multidrug resistance (MDR) in vitro, when administered in combination with vinblastine in patients with advanced colorectal cancer, a tumor characterized by high MDR1 gene expression [3].
  • In two patients with intranodal reciprocal rhythm, the injection of bepridil terminated the tachycardia which could not be reinitiated later [4].

High impact information on bepridil


Chemical compound and disease context of bepridil


Biological context of bepridil

  • Moreover, platelet aggregation induced by various physiologic agonists was inhibited by DCB or bepridil, while platelet agglutination by ristocetin was not [7].
  • Identification of binding sites for bepridil and trifluoperazine on cardiac troponin C [14].
  • Treatment of confluent osteoblast cultures for 14 days with low levels of bepridil (3.0 microM) or KB-R7943 (1.0 microM and 0.1 microM) resulted in a significantly diminished capacity of these cells to mineralize bone matrix, without significantly altering cell morphology, viability, or cell differentiation [15].
  • In group 2, heart rate (HR) and contractility initially increased (8% and 10%, respectively, P less than 0.05 vs C), secondary to the greater fall in afterload, followed by a significant reduction at 5 and 10 min after bepridil (9% and 10%, respectively), accompanied by a 36% increase in LV enddiastolic pressure (P less than 0.05 vs C) [16].
  • Cardiac output, measured immediately after bepridil, was unaltered, although in group 2 stroke volume index increased (14%) and systemic resistance decreased (16%), both P less than 0.05 vs C [16].

Anatomical context of bepridil


Associations of bepridil with other chemical compounds


Gene context of bepridil

  • The antiarrhythmic KCNQ1 channel blocker bepridil inhibited KCNQ4 with an IC(50) value of 9.4 microM, whereas clofilium was without significant effect at 100 microM [24].
  • Micromolar bepridil inhibited tail currents carried by KCNQ1/KCNE1 channels in a concentration-dependent manner (IC50 = 5.3 +/- 0.7 microM at -40 mV from 1000 milliseconds test pulse) [25].
  • The effect of bepridil on DNR and VCR accumulation and chemosensitivity in the XG cells was in accordance with the XG expression of mdr1/Pgp [18].
  • It is shown that bepridil blocks both cellular calcium entry as measured by Mn2+ quenching of fura-2 fluorescence and activation of the Na+/H(+)-exchanger following expression of the Ha-ras oncogene [26].
  • 10 mumol/l bepridil inhibit oscillations of PD and protect +ras cells against actin stress fiber depolymerization [26].

Analytical, diagnostic and therapeutic context of bepridil


  1. Elevation of cytosolic calcium precedes anoxic gene expression in maize suspension-cultured cells. Subbaiah, C.C., Bush, D.S., Sachs, M.M. Plant Cell (1994) [Pubmed]
  2. Effect of bepridil in patients with chronic stable angina: results of a multicenter trial. Hill, J.A., O'Brien, J.T., Alpert, J.S., Gore, J.M., Zusman, R.M., Christensen, D., Boucher, C.A., Vetrovec, G., Borer, J.S., Friedman, C. Circulation (1985) [Pubmed]
  3. Clinical and pharmacologic study of multidrug resistance reversal with vinblastine and bepridil. Linn, S.C., van Kalken, C.K., van Tellingen, O., van der Valk, P., van Groeningen, C.J., Kuiper, C.M., Pinedo, H.M., Giaccone, G. J. Clin. Oncol. (1994) [Pubmed]
  4. Electrophysiological profile of bepridil, a new anti-anginal drug with calcium blocking properties. Flammang, D., Waynberger, M., Jansen, F.H., Paillet, R., Coumel, P. Eur. Heart J. (1983) [Pubmed]
  5. Bepridil and cetiedil. Vasodilators which inhibit Ca2+-dependent calmodulin interactions with erythrocyte membranes. Agre, P., Virshup, D., Bennett, V. J. Clin. Invest. (1984) [Pubmed]
  6. Involvement of Na+/Ca2+ exchanger in inside-out signaling through the platelet integrin IIbbeta3. Shiraga, M., Tomiyama, Y., Honda, S., Suzuki, H., Kosugi, S., Tadokoro, S., Kanakura, Y., Tanoue, K., Kurata, Y., Matsuzawa, Y. Blood (1998) [Pubmed]
  7. Affinity modulation of the platelet integrin alpha IIb beta 3 by alpha-chymotrypsin: a possible role for Na+/Ca2+ exchanger. Shiraga, M., Tomiyama, Y., Honda, S., Kashiwagi, H., Kosugi, S., Handa, M., Ikeda, Y., Kanakura, Y., Kurata, Y., Matsuzawa, Y. Blood (1996) [Pubmed]
  8. Axotomy-induced axonal degeneration is mediated by calcium influx through ion-specific channels. George, E.B., Glass, J.D., Griffin, J.W. J. Neurosci. (1995) [Pubmed]
  9. Na(+)-Ca2+ exchanger mediates Ca2+ influx during anoxia in mammalian central nervous system white matter. Stys, P.K., Waxman, S.G., Ransom, B.R. Ann. Neurol. (1991) [Pubmed]
  10. The effects of calcium entry blockade on the vulnerability of infarcted canine myocardium toward ventricular fibrillation. Lynch, J.J., Montgomery, D.G., Lucchesi, B.R. J. Pharmacol. Exp. Ther. (1986) [Pubmed]
  11. Comparative effects of nisoldipine, nifedipine and bepridil on experimental pulmonary hypertension. Archer, S.L., Yankovich, R.D., Chesler, E., Weir, E.K. J. Pharmacol. Exp. Ther. (1985) [Pubmed]
  12. Broad sensitivity of rodent arrhythmia models to class I, II, III, and IV antiarrhythmic agents. Brooks, R.R., Miller, K.E., Carpenter, J.F., Jones, S.M. Proc. Soc. Exp. Biol. Med. (1989) [Pubmed]
  13. Comparative antiarrhythmic and electrophysiological effects of drugs known to inhibit calmodulin (TFP, W7 and bepridil). Barron, E., Marshall, R.J., Martorana, M., Winslow, E. Br. J. Pharmacol. (1986) [Pubmed]
  14. Identification of binding sites for bepridil and trifluoperazine on cardiac troponin C. Kleerekoper, Q., Liu, W., Choi, D., Putkey, J.A. J. Biol. Chem. (1998) [Pubmed]
  15. Inhibition of Na+/Ca2+ exchange with KB-R7943 or bepridil diminished mineral deposition by osteoblasts. Stains, J.P., Gay, C.V. J. Bone Miner. Res. (2001) [Pubmed]
  16. Dose related coronary and systemic haemodynamic effects of intravenous bepridil in patients with coronary artery disease. Remme, W.J., van Hoogenhuyze, D.C., Krauss, X.H., Hofman, A., Storm, C.J., Kruyssen, H.A. Eur. Heart J. (1987) [Pubmed]
  17. Protective effects of the calmodulin antagonist bepridil on ischaemia induced in the rat myocardium. Shikano, K., Kusagawa, M., Itoh, H., Hidaka, H. Cardiovasc. Res. (1986) [Pubmed]
  18. Correlation between functional and molecular analysis of mdr1 P-glycoprotein in human solid-tumor xenografts. Broxterman, H.J., Feller, N., Kuiper, C.M., Boven, E., Versantvoort, C.H., Teerlink, T., Pinedo, H.M., Lankelma, J. Int. J. Cancer (1995) [Pubmed]
  19. Bepridil and cetiedil reversibly inhibit thyroid hormone stimulation in vitro of human red cell Ca2+-ATPase activity. Dube, M.P., Davis, F.B., Davis, P.J., Blas, S.D. Mol. Endocrinol. (1987) [Pubmed]
  20. Myocardial protection with calcium-channel blockers during ischaemia and reperfusion by PTCA. Chouairi, S., Carrie, D., Puel, J. Eur. Heart J. (1995) [Pubmed]
  21. Digoxin and bepridil: pharmacokinetic and pharmacodynamic interactions. Belz, G.G., Wistuba, S., Matthews, J.H. Clin. Pharmacol. Ther. (1986) [Pubmed]
  22. HERG and KvLQT1/IsK, the cardiac K+ channels involved in long QT syndromes, are targets for calcium channel blockers. Chouabe, C., Drici, M.D., Romey, G., Barhanin, J., Lazdunski, M. Mol. Pharmacol. (1998) [Pubmed]
  23. Effect of ion channel inhibitors on the cytopathogenicity of Entamoeba histolytica. Ravdin, J.I., Sperelakis, N., Guerrant, R.L. J. Infect. Dis. (1982) [Pubmed]
  24. KCNQ4 channels expressed in mammalian cells: functional characteristics and pharmacology. Søgaard, R., Ljungstrøm, T., Pedersen, K.A., Olesen, S.P., Jensen, B.S. Am. J. Physiol., Cell Physiol. (2001) [Pubmed]
  25. Bepridil block of recombinant human cardiac IKs current shows a time-dependent unblock. Yumoto, Y., Horie, M., Kubota, T., Ninomiya, T., Kobori, A., Takenaka, K., Takano, M., Niwano, S., Izumi, T. J. Cardiovasc. Pharmacol. (2004) [Pubmed]
  26. Activation of Na+/H(+)-exchanger by transforming Ha-ras requires stimulated cellular calcium influx and is associated with rearrangement of the actin cytoskeleton. Ritter, M., Wöll, E., Haller, T., Dartsch, P.C., Zwierzina, H., Lang, F. Eur. J. Cell Biol. (1997) [Pubmed]
  27. Binding of a calcium sensitizer, bepridil, to cardiac troponin C. A fluorescence stopped-flow kinetic, circular dichroism, and proton nuclear magnetic resonance study. MacLachlan, L.K., Reid, D.G., Mitchell, R.C., Salter, C.J., Smith, S.J. J. Biol. Chem. (1990) [Pubmed]
  28. Bepridil, an antiarrhythmic drug, opens mitochondrial KATP channels, blocks sarcolemmal KATP channels, and confers cardioprotection. Sato, T., Costa, A.D., Saito, T., Ogura, T., Ishida, H., Garlid, K.D., Nakaya, H. J. Pharmacol. Exp. Ther. (2006) [Pubmed]
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