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Chemical Compound Review

Ro 40-5967     [(1S,2S)-2-[2-[3-(1H- benzoimidazol-2...

Synonyms: Mibefradil HCl, Cerate 50, Posicor (TN), SureCN120810, CS-1189, ...
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Disease relevance of Mibefradil

 

High impact information on Mibefradil

 

Chemical compound and disease context of Mibefradil

 

Biological context of Mibefradil

  • Ro 40-5967 inhibited reversibly the T- and L-type currents with IC50 values of 2.7 and 18.6 microM, respectively [11].
  • 6. In conclusion Ro 40-5967 led to a significant elevation of the plasma concentration-time curve (AUC) of digoxin [12].
  • Ro 40-5967 defines an additional and possibly unique antagonist binding site on the L-type voltage-gated Ca2+ channel [13].
  • It was found that at a physiological membrane potential (-80 mV) Ro 40-5967 was also less potent than verapamil in inhibiting this current, and that negative inotropy and Ca2+ channel blockade were correlated [14].
  • The protective effect of Ro 40-5967 could be partially explained by the decrease of arterial pressure and heart rate induced by Ro 40-5967 [9].
 

Anatomical context of Mibefradil

 

Associations of Mibefradil with other chemical compounds

  • The IC50 values at a holding potential of -80 or -40 mV were 4.9 and 1.4 microM for Ro 40-5967 and 250 and 15.5 microM for verapamil [19].
  • 3. Ro 40-5967 led to an increase of mean maximum digoxin plasma concentrations (Cmax) and AUC [12].
  • Though activation of adhesion molecule expression utilizes PKC and/or calmodulin as second-messenger pathways the investigated calcium channel blockers verapamil (R- and S-enantiomers), diltiazem and Ro 40-5967 failed to inhibit adhesion molecule expression [20].
  • For this purpose, two kidney-one clip (2K-1C) hypertensive rats, 6 weeks after renal artery clipping, were either untreated or treated for 5 weeks with equihypotensive doses of enalapril (3 mg/kg/day) and Ro 40-5967 (30 mg/kg/day) [10].
  • The effects of Ro 40-5967, a chemically novel Ca2+ channel antagonist, were examined on K(+)- and norepinephrine (NE)-stimulated intracellular free Ca2+ concentrations in dog coronary artery vascular muscle cells (VMC) [21].
 

Gene context of Mibefradil

  • Surprisingly, higher concentrations of verapamil (> 12.5 micrograms/ml) or Ro 40-5967 (5 micrograms/ml) significantly enhanced IL-1-induced expression of ELAM-1 [20].
  • These data suggest that there is an important direct PKC inhibitory action of Ro 40-5967 that would at least partially explain relaxation of ET-induced contractions [22].
  • Actions of the novel Ca2+ antagonist, Ro 40-5967, which displays unusual efficacy against endothelin (ET)-induced contractions, were studied in isolated vascular muscle cells (VMCs) using the fluorescent protein kinase C (PKC) indicator, BODIPY 12 alpha-phorbol ester 13 beta-acetate (PBA-BODIPY) [22].
  • Interaction of Ro 40-5967 and verapamil with the stably expressed alpha 1-subunit of the cardiac L-type calcium channel [19].
  • Plasma haptoglobin decreased by 67% after 3.5 h in 2 subjects who received 80 mg Ro 40-5967 in one arm (treatment schedule thereupon discontinued) [23].

References

  1. Hemodynamic and humoral effects of the novel calcium antagonist Ro 40-5967 in patients with hypertension. Schmitt, R., Kleinbloesem, C.H., Belz, G.G., Schroeter, V., Feifel, U., Pozenel, H., Kirch, W., Halabi, A., Woittiez, A.J., Welker, H.A. Clin. Pharmacol. Ther. (1992) [Pubmed]
  2. The novel calcium antagonist Ro 40-5967 limits myocardial infarct size in the dog. Vander Heide, R.S., Schwartz, L.M., Reimer, K.A. Cardiovasc. Res. (1994) [Pubmed]
  3. Ro 40-5967, a novel calcium channel antagonist, protects against ventricular fibrillation. Billman, G.E. Eur. J. Pharmacol. (1992) [Pubmed]
  4. Effects of the new calcium antagonist mibefradil (Ro 40-5967) on exercise duration in patients with chronic stable angina pectoris: a multicenter, placebo-controlled study. Ro 40-5967 International Study Group. Bakx, A.L., van der Wall, E.E., Braun, S., Emanuelsson, H., Bruschke, A.V., Kobrin, I. Am. Heart J. (1995) [Pubmed]
  5. Selective inhibition of T-type Ca2+ channels by Ro 40-5967. Mishra, S.K., Hermsmeyer, K. Circ. Res. (1994) [Pubmed]
  6. Assessment of left ventricular end-systolic pressure-volume relations with an impedance catheter and transient inferior vena cava occlusion: use of this system in the evaluation of the cardiotonic effects of dobutamine, milrinone, Posicor and epinephrine. McKay, R.G., Miller, M.J., Ferguson, J.J., Momomura, S., Sahagian, P., Grossman, W., Pasternak, R.C. J. Am. Coll. Cardiol. (1986) [Pubmed]
  7. Voltage-dependent blockade of diverse types of voltage-gated Ca2+ channels expressed in Xenopus oocytes by the Ca2+ channel antagonist mibefradil (Ro 40-5967). Bezprozvanny, I., Tsien, R.W. Mol. Pharmacol. (1995) [Pubmed]
  8. Effects of calcium channel blockade on the aortic intima in spontaneously hypertensive rats. Gray, G.A., Clozel, M., Clozel, J.P., Baumgartner, H.R. Hypertension (1993) [Pubmed]
  9. Effects of Ro 40-5967, a novel calcium antagonist, on myocardial function during ischemia induced by lowering coronary perfusion pressure in dogs: comparison with verapamil. Clozel, J.P., Banken, L., Osterrieder, W. J. Cardiovasc. Pharmacol. (1989) [Pubmed]
  10. Effects of Ro 40-5967, a new calcium antagonist, and enalapril on cardiac remodeling in renal hypertensive rats. Véniant, M., Clozel, J.P., Heudes, D., Banken, L., Ménard, J. J. Cardiovasc. Pharmacol. (1993) [Pubmed]
  11. The Ca(++)-channel blocker Ro 40-5967 blocks differently T-type and L-type Ca++ channels. Mehrke, G., Zong, X.G., Flockerzi, V., Hofmann, F. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  12. The interaction of the calcium antagonist RO 40-5967 with digoxin. Siepmann, M., Kleinbloesem, C., Kirch, W. British journal of clinical pharmacology. (1995) [Pubmed]
  13. The binding interactions of Ro 40-5967 at the L-type Ca2+ channel in cardiac tissue. Rutledge, A., Triggle, D.J. Eur. J. Pharmacol. (1995) [Pubmed]
  14. Potential-dependent inhibition of cardiac Ca2+ inward currents by Ro 40-5967 and verapamil: relation to negative inotropy. Fang, L.M., Osterrieder, W. Eur. J. Pharmacol. (1991) [Pubmed]
  15. Mibefradil (Ro 40-5967) blocks multiple types of voltage-gated calcium channels in cultured rat spinal motoneurones. Viana, F., Van den Bosch, L., Missiaen, L., Vandenberghe, W., Droogmans, G., Nilius, B., Robberecht, W. Cell Calcium (1997) [Pubmed]
  16. Mibefradil (Ro 40-5967) inhibits several Ca2+ and K+ currents in human fusion-competent myoblasts. Liu, J.H., Bijlenga, P., Occhiodoro, T., Fischer-Lougheed, J., Bader, C.R., Bernheim, L. Br. J. Pharmacol. (1999) [Pubmed]
  17. Resting state block and use independence of rat vascular muscle Ca++ channels by Ro 40-5967. Mishra, S.K., Hermsmeyer, K. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  18. Ca2+ channel actions of the non-dihydropyridine Ca2+ channel antagonist Ro 40-5967 in vascular muscle cells cultured from dog coronary and saphenous arteries. Bian, K., Hermsmeyer, K. Naunyn Schmiedebergs Arch. Pharmacol. (1993) [Pubmed]
  19. Interaction of Ro 40-5967 and verapamil with the stably expressed alpha 1-subunit of the cardiac L-type calcium channel. Lacinová, L., Welling, A., Bosse, E., Ruth, P., Flockerzi, V., Hofmann, F. J. Pharmacol. Exp. Ther. (1995) [Pubmed]
  20. Modulation of adhesion molecule expression on endothelial cells by verapamil and other Ca++ channel blockers. Hailer, N.P., Blaheta, R.A., Harder, S., Scholz, M., Encke, A., Markus, B.H. Immunobiology (1994) [Pubmed]
  21. Inhibition of signal Ca2+ in dog coronary arterial vascular muscle cells by Ro 40-5967. Mishra, S.K., Hermsmeyer, K. J. Cardiovasc. Pharmacol. (1994) [Pubmed]
  22. Protein kinase C mechanism enhances vascular muscle relaxation by the Ca2+ antagonist, Ro 40-5967. Hermsmeyer, K., Miyagawa, K. J. Vasc. Res. (1996) [Pubmed]
  23. Hemolysis on intravenous administration of a new calcium antagonist. Kleinbloesem, C.H., Siepmann, M., Kirch, W. J. Cardiovasc. Pharmacol. (1995) [Pubmed]
 
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