Summary: A benzimidazoyl-substituted tetraline that selectively binds and inhibits CALCIUM CHANNELS, T-TYPE.

Top Publications

  1. Nebe B, Holzhausen C, Rychly J, Urbaszek W. Impaired mechanisms of leukocyte adhesion in vitro by the calcium channel antagonist mibefradil. Cardiovasc Drugs Ther. 2002;16:183-93 pubmed
    ..We studied the influence of the calcium antagonists mibefradil (T-type channel blocker), amlodipine and verapamil (both L-type channel blockers) on mechanisms related to ..
  2. Brenker C, Goodwin N, Weyand I, Kashikar N, Naruse M, Krähling M, et al. The CatSper channel: a polymodal chemosensor in human sperm. EMBO J. 2012;31:1654-65 pubmed publisher
    ..We propose that the CatSper channel complex serves as a polymodal sensor for multiple chemical cues that assist sperm during their voyage across the female genital tract. ..
  3. Hotta A, Okada N, Suzuki H. Mibefradil-sensitive component involved in the plateau potential in submucosal interstitial cells of the murine proximal colon. Biochem Biophys Res Commun. 2007;353:170-6 pubmed
    ..0mM [K(+)](o). The rise rate of plateau potentials was significantly reduced by the application of 3 microM mibefradil or 100 microM Ni(2+) but not by 0.3 microM nifedipine...
  4. Fareh S, Benardeau A, Nattel S. Differential efficacy of L- and T-type calcium channel blockers in preventing tachycardia-induced atrial remodeling in dogs. Cardiovasc Res. 2001;49:762-70 pubmed
    ..This study was designed to evaluate the relative efficacies of selective T-type (mibefradil) and L-type (diltiazem) Ca(2+)-channel blockers in preventing tachycardia-induced atrial remodeling...
  5. Nebe B, Kunz F, Peters A, Rychly J, Noack T, Beck R. Induction of apoptosis by the calcium antagonist mibefradil correlates with depolarization of the membrane potential and decreased integrin expression in human lens epithelial cells. Graefes Arch Clin Exp Ophthalmol. 2004;242:597-604 pubmed
    ..Our approach using the T-calcium channel antagonist mibefradil is based on the hypothesis that this drug inhibits the signaling pathways mediated by cell adhesion...
  6. Krahenbuhl S, Menafoglio A, Giostra E, Gallino A. Serious interaction between mibefradil and tacrolimus. Transplantation. 1998;66:1113-5 pubmed
    ..We report a serious kinetic interaction between tacrolimus and mibefradil, a potent cytochrome P450 inhibitor...
  7. Welker H, Wiltshire H, Bullingham R. Clinical pharmacokinetics of mibefradil. Clin Pharmacokinet. 1998;35:405-23 pubmed
    b>Mibefradil, a tetralol derivative, is a new long-acting calcium antagonist used for the treatment of patients with hypertension and chronic stable angina pectoris...
  8. Beck R, Nebe B, Guthoff R, Rychly J. Inhibition of lens epithelial cell adhesion by the calcium antagonist Mibefradil correlates with impaired integrin distribution and organization of the cytoskeleton. Graefes Arch Clin Exp Ophthalmol. 2001;239:452-8 pubmed
    ..b>Mibefradil, a T-type calcium-channel blocker, was used to examine the influence on adhesion-mediating mechanisms in human ..
  9. Chung O, Hinder M, Sharma A, Bonner G, Middeke M, Platon J, et al. Comparison of the efficacy and safety of losartan (50-100 mg) with the T-type calcium channel blocker mibefradil (50-100 mg) in mild to moderate hypertension. Fundam Clin Pharmacol. 2000;14:31-41 pubmed
    The objective of this study was to compare the antihypertensive efficacy and safety of losartan and mibefradil. 324 outpatients (57 +/- 9...

More Information


  1. Boddy G, Willis A, Galante G, Daniel E. Sodium-, chloride-, and mibefradil-sensitive calcium channels in intestinal pacing in wild-type and W/WV mice. Can J Physiol Pharmacol. 2006;84:589-99 pubmed
    ..circular (CM) and longitudinal (LM) muscle from wild-type and W/WV mice, we found that sodium-, chloride-, and mibefradil-sensitive ion channel currents are required for normal pacing to occur...
  2. Beltrame J, Turner S, Leslie S, Solomon P, Freedman S, Horowitz J. The angiographic and clinical benefits of mibefradil in the coronary slow flow phenomenon. J Am Coll Cardiol. 2004;44:57-62 pubmed
    The aim of the study was to assess the angiographic and clinical benefits of the calcium T-channel blocker, mibefradil, in the coronary slow flow phenomenon (CSFP)...
  3. Jensen L, Salomonsson M, Jensen B, Holstein Rathlou N. Depolarization-induced calcium influx in rat mesenteric small arterioles is mediated exclusively via mibefradil-sensitive calcium channels. Br J Pharmacol. 2004;142:709-18 pubmed
    ..The data suggest that the Ca(2+) response was caused by the activation of voltage-dependent Ca(2+) channels. 4. Mibefradil use dependently inhibited the Ca(2+) response to 75 mm K(+) by 29+/-2% (100 nm), 73+/-7% (1 microm) or 89+/-7% (..
  4. Ma G, Allen T, Cooper M, Cao Z. Calcium channel blockers, either amlodipine or mibefradil, ameliorate renal injury in experimental diabetes. Kidney Int. 2004;66:1090-8 pubmed
    ..Amlodipine, a CCB which blocks the L channel, and mibefradil, a CCB blocking the T as well as the L channels, were given to diabetic rats for six months...
  5. Viana F, van den Bosch L, Missiaen L, Vandenberghe W, Droogmans G, Nilius B, et al. Mibefradil (Ro 40-5967) blocks multiple types of voltage-gated calcium channels in cultured rat spinal motoneurones. Cell Calcium. 1997;22:299-311 pubmed
    The actions of the novel calcium (Ca2+) channel antagonist mibefradil (Ro 40-5967), a selective T-type channel blocker in myocardium, were investigated in embryonic rat spinal motoneurones maintained in culture...
  6. Cribbs L, Lee J, Yang J, Satin J, Zhang Y, Daud A, et al. Cloning and characterization of alpha1H from human heart, a member of the T-type Ca2+ channel gene family. Circ Res. 1998;83:103-9 pubmed
    ..The alpha1H channel is sensitive to mibefradil, a nondihydropyridine Ca2+ channel blocker, with an IC50 of 1...
  7. Pellizzer A, Kamen P, Esler M, Lim S, Krum H. Comparative effects of mibefradil and nifedipine gastrointestinal transport system on autonomic function in patients with mild to moderate essential hypertension. J Hypertens. 2001;19:279-85 pubmed
    ..group study compared the effect of nifedipine gastrointestinal transport system (GITS) (L-type CCB) versus mibefradil (T-type CCB) on ANS function in patients with mild-moderate essential hypertension...
  8. McNulty M, Kyle J, Lipkind G, Hanck D. An inner pore residue (Asn406) in the Nav1.5 channel controls slow inactivation and enhances mibefradil block to T-type Ca2+ channel levels. Mol Pharmacol. 2006;70:1514-23 pubmed
    b>Mibefradil is a tetralol derivative once marketed to treat hyper-tension. Its primary target is the T-type Ca(2+) channel (IC(50), approximately 0.1-0...
  9. Mullins M, Horowitz B, Linden D, Smith G, Norton R, Stump J. Life-threatening interaction of mibefradil and beta-blockers with dihydropyridine calcium channel blockers. JAMA. 1998;280:157-8 pubmed
    b>Mibefradil is a T-type and L-type calcium channel blocker (CCB) released in the United States in 1997 for management of hypertension and chronic stable angina...
  10. Yoo H, Zheng H, Nam J, Nguyen Y, Kang T, Earm Y, et al. Facilitation of Ca2+-activated K+ channels (IKCa1) by mibefradil in B lymphocytes. Pflugers Arch. 2008;456:549-60 pubmed publisher
    ..b>Mibefradil, a blocker of T-type Ca2+ channels, has been reported to affect the proliferation of immune cells...
  11. Shin J, Martinez Salgado C, Heppenstall P, Lewin G. A T-type calcium channel required for normal function of a mammalian mechanoreceptor. Nat Neurosci. 2003;6:724-30 pubmed
    ..This is the first evidence that a calcium channel is required for normal function of a vertebrate mechanoreceptor. ..
  12. Strege P, Bernard C, Ou Y, Gibbons S, Farrugia G. Effect of mibefradil on sodium and calcium currents. Am J Physiol Gastrointest Liver Physiol. 2005;289:G249-53 pubmed
    ..b>Mibefradil has a higher affinity for T-type over L-type Ca2+ channels, and the drug has been used in the gastrointestinal ..
  13. Riley J, Wilton L, Shakir S. A post-marketing observational study to assess the safety of mibefradil in the community in England. Int J Clin Pharmacol Ther. 2002;40:241-8 pubmed
    To conduct a post-marketing observational cohort study to assess the safety of mibefradil in the community, using Prescription-Event Monitoring (PEM)...
  14. Li Y, Liu S, Lu F, Zhang T, Chen H, Wu S, et al. A role of functional T-type Ca2+ channel in hepatocellular carcinoma cell proliferation. Oncol Rep. 2009;22:1229-35 pubmed
    ..SNU449, PLC/PRF5, Hep3B and LO2 cell lines were subjected to growth assay in the presence of Mibefradil, a T-type Ca2+ channel blocker, only the proliferation of SNU449 cell which had functional T-type Ca2+ channel ..
  15. Villame J, Massicotte J, Jasmin G, Dumont L. Effects of mibefradil, a T- and L-type calcium channel blocker, on cardiac remodeling in the UM-X7.1 cardiomyopathic hamster. Cardiovasc Drugs Ther. 2001;15:41-8 pubmed
    ..We tested the hypothesis that chronic exposure to mibefradil, a selective T-type calcium channel blocker, improves the deleterious cardiac remodeling observed in this ..
  16. Young R, Zhang P. Inhibition of in vitro contractions of human myometrium by mibefradil, a T-type calcium channel blocker: support for a model using excitation-contraction coupling, and autocrine and paracrine signaling mechanisms. J Soc Gynecol Investig. 2005;12:e7-12 pubmed
    ..Tissue was then exposed to the T-type calcium channel blocker mibefradil (1 microM), the L-type calcium channel blocker nifedipine (5 nM), or the cyclooxygenase (COX) inhibitor ..
  17. Lindqvist M, Kahan T, Melcher A, Ekholm M, Hjemdahl P. Long-term calcium antagonist treatment of human hypertension with mibefradil or amlodipine increases sympathetic nerve activity. J Hypertens. 2007;25:169-75 pubmed
    ..the effects of long-term treatment with amlodipine, a long-acting dihydropyridine-type calcium antagonist, and mibefradil, a phenylalkylamine-type calcium antagonist, on sympathetic nerve activity...
  18. McNulty M, Hanck D. State-dependent mibefradil block of Na+ channels. Mol Pharmacol. 2004;66:1652-61 pubmed
    b>Mibefradil is a T-type Ca2+ channel antagonist with reported cross-reactivity with other classes of ion channels, including K+, Cl-, and Na+ channels...
  19. Kosmidis K, Karalis V, Argyrakis P, Macheras P. Michaelis-Menten kinetics under spatially constrained conditions: application to mibefradil pharmacokinetics. Biophys J. 2004;87:1498-506 pubmed
    ..of the enzymatic reaction under heterogeneous conditions to interpret the unusual nonlinear pharmacokinetics of mibefradil. Firstly, a detailed model based on the kinetic differential equations is proposed to study the enzymatic ..
  20. Keir S, Friedman H, Reardon D, Bigner D, Gray L. Mibefradil, a novel therapy for glioblastoma multiforme: cell cycle synchronization and interlaced therapy in a murine model. J Neurooncol. 2013;111:97-102 pubmed publisher
    ..We also present data that MGMT expressing GBM tumors, which are temozolomide resistant, may be rendered more sensitive by this strategy. ..
  21. Michels G, Matthes J, Handrock R, Kuchinke U, Groner F, Cribbs L, et al. Single-channel pharmacology of mibefradil in human native T-type and recombinant Ca(v)3.2 calcium channels. Mol Pharmacol. 2002;61:682-94 pubmed
    ..Type I channels are therefore classified as T-type channels. They were strongly inhibited by 10 microM mibefradil. Mibefradil block was caused by changes in two gating parameters: a pronounced reduction in fraction of active ..
  22. Bertolesi G, Shi C, Elbaum L, Jollimore C, Rozenberg G, Barnes S, et al. The Ca(2+) channel antagonists mibefradil and pimozide inhibit cell growth via different cytotoxic mechanisms. Mol Pharmacol. 2002;62:210-9 pubmed
    ..Ca(2+) channels (T-channels) are more sensitive to the antiproliferative effects of the drugs pimozide and mibefradil than cells without significant T-channel expression...
  23. Strünker T, Goodwin N, Brenker C, Kashikar N, Weyand I, Seifert R, et al. The CatSper channel mediates progesterone-induced Ca2+ influx in human sperm. Nature. 2011;471:382-6 pubmed publisher
    ..signals evoked by alkaline pH and progesterone are inhibited by the Ca(v) channel blockers NNC 55-0396 and mibefradil. Patch-clamp recordings from sperm reveal an alkaline-activated current carried by mono- and divalent ions that ..
  24. Leuranguer V, Mangoni M, Nargeot J, Richard S. Inhibition of T-type and L-type calcium channels by mibefradil: physiologic and pharmacologic bases of cardiovascular effects. J Cardiovasc Pharmacol. 2001;37:649-61 pubmed
    ..In contrast, mibefradil was reported to be more selective for T-type channels...
  25. Chevalier M, Lory P, Mironneau C, Macrez N, Quignard J. T-type CaV3.3 calcium channels produce spontaneous low-threshold action potentials and intracellular calcium oscillations. Eur J Neurosci. 2006;23:2321-9 pubmed
    ..3 channel activity given that they were recorded from a potential range of -55 to -70 mV, blocked by nickel and mibefradil, as well as by low external Ca2+ concentration...
  26. Lee T, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, et al. Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78:11-20 pubmed
    We compared detailed efficacy of efonidipine and nifedipine, dihydropyridine analogues, and mibefradil using recombinant T- and L-type Ca2+ channels expressed separately in mammalian cells...
  27. Yoshimura Y, Inaba M, Yamada K, Kurotani T, Begum T, Reza F, et al. Involvement of T-type Ca2+ channels in the potentiation of synaptic and visual responses during the critical period in rat visual cortex. Eur J Neurosci. 2008;28:730-43 pubmed publisher
    ..In visual cortical slices, LTP was blocked by mibefradil, kurtoxin and R-(-)-efonidipine, T-type VGCC blockers, but not by SNX-482, an R-type VGCC blocker, indicating ..
  28. Moosmang S, Haider N, Brüderl B, Welling A, Hofmann F. Antihypertensive effects of the putative T-type calcium channel antagonist mibefradil are mediated by the L-type calcium channel Cav1.2. Circ Res. 2006;98:105-10 pubmed
    ..T-type Ca2+ channels in resistance arteries has been proposed to explain the effect of the antihypertensive drug mibefradil. In the present study, we used a third generation, time- and tissue-specific conditional knockout model of the L-..
  29. Todorovic S, Meyenburg A, Jevtovic Todorovic V. Mechanical and thermal antinociception in rats following systemic administration of mibefradil, a T-type calcium channel blocker. Brain Res. 2002;951:336-40 pubmed
    ..We studied the antinociceptive potential of systemically administered mibefradil, a peripherally acting antihypertensive agent and preferential T-type Ca(2+) channel blocker...
  30. Bancila M, Copin J, Daali Y, Schatlo B, Gasche Y, Bijlenga P. Two structurally different T-type Ca 2+ channel inhibitors, mibefradil and pimozide, protect CA1 neurons from delayed death after global ischemia in rats. Fundam Clin Pharmacol. 2011;25:469-78 pubmed publisher
    ..The aim of this work was to study the neuroprotective potential of mibefradil and pimozide, both T-type Ca(2+) channel inhibitors, in an in vivo rat model of global ischemia...
  31. Li J, Schiffrin E. Effect of short-term treatment of SHR with the novel calcium channel antagonist mibefradil on function of small arteries. Am J Hypertens. 1997;10:94-100 pubmed
    ..specific antihypertensive treatment, SHR and WKY were treated for 4 weeks with the novel calcium channel blocker mibefradil. Blood pressure rise was significantly reduced by mibefradil treatment in SHR to 165 +/- 1 mm Hg compared to a ..
  32. Dogrul A, Gardell L, Ossipov M, Tulunay F, Lai J, Porreca F. Reversal of experimental neuropathic pain by T-type calcium channel blockers. Pain. 2003;105:159-68 pubmed
    ..b>Mibefradil or ethosuximide was administered either intraperitoneally, intrathecally (i.th...
  33. Asokan K, Sarkar S, Mishra S, Raviprakash V. Effects of mibefradil on uterine contractility. Eur J Pharmacol. 2002;455:65-71 pubmed
    b>Mibefradil, a benzimidazolyl tetralol derivative, is a new Ca(2+) channel antagonist which is structurally distinct from other Ca(2+) channel antagonists such as nifedipine, verapamil and diltiazem...
  34. Glaser S, Steinbach M, Opitz C, Wruck U, Kleber F. Torsades de pointes caused by Mibefradil. Eur J Heart Fail. 2001;3:627-30 pubmed
    We report a case of symptomatic Torsades de pointes due to QTc prolongation by Mibefradil, which potentially explains unexpected deaths related to this drug...
  35. Barton M, Eberle E, Shannon H. The antihyperalgesic effects of the T-type calcium channel blockers ethosuximide, trimethadione, and mibefradil. Eur J Pharmacol. 2005;521:79-85 pubmed
    ..the analgesic effects of the low voltage-activated T-type Ca2+ channel blockers ethosuximide, trimethadione, and mibefradil in persistent and acute nociceptive tests...
  36. Lee J, Kim J, Kim C, Min C. Inhibitory actions of mibefradil on steroidogenesis in mouse Leydig cells: involvement of Ca(2+) entry via the T-type Ca(2+) channel. Asian J Androl. 2010;12:807-13 pubmed publisher
    ..The effects of mibefradil (a putative T-type Ca(2+) channel blocker) on steroidogenesis were assessed using reverse transcription (RT)-..
  37. Monteil A, Chemin J, Bourinet E, Mennessier G, Lory P, Nargeot J. Molecular and functional properties of the human alpha(1G) subunit that forms T-type calcium channels. J Biol Chem. 2000;275:6090-100 pubmed
    ..This alpha(1G)-related current was inhibited by mibefradil (IC(50) = 2 microM) and weakly blocked by Ni(2+) ions (IC(50) = 148 microM) and amiloride (IC(50) > 1 mM)...
  38. Sekiguchi N, Kato M, Takada M, Watanabe H, Higashida A, Sakai S, et al. In vivo approach for the evaluation of mechanism-based inhibition of cytochrome P450 3A in rats. Xenobiotica. 2008;38:368-81 pubmed
    ..2. Midazolam (MDZ), mainly metabolized by cytochrome P450 3A in rats, and mibefradil, which showed the most intense time-dependent inhibition among the inhibitors tested, were selected as the probe ..
  39. Meissner A, Noack T. Proliferation of human lens epithelial cells (HLE-B3) is inhibited by blocking of voltage-gated calcium channels. Pflugers Arch. 2008;457:47-59 pubmed publisher
    ..are substantially present in human lens epithelial cell (hLEC), and total calcium currents are inhibited by mibefradil. Here, the hypothesis was tested if calcium influx via Ca(v) channels regulates proliferation in epithelial ..
  40. Kito Y, Ward S, Sanders K. Pacemaker potentials generated by interstitial cells of Cajal in the murine intestine. Am J Physiol Cell Physiol. 2005;288:C710-20 pubmed
    ..Pacemaker potentials and slow waves were not blocked by nifedipine (3 microM). In the presence of nifedipine, mibefradil, a voltage-dependent Ca(2+) channel blocker, reduced the amplitude, frequency, and rate of rise of upstroke ..
  41. Amobi N, Guillebaud J, Smith C. Comparative effects of T-type and L-type Ca(2+)-antagonists against noradrenaline-induced contractions of human vas deferens. BJU Int. 2010;106:578-85 pubmed publisher
    To investigate the effects of the relatively selective T-type Ca(2+)-antagonists, mibefradil and flunarizine, and the L-type Ca(2+)-antagonist, nifedipine, on the contractions of longitudinal and circular muscles of human vas deferens, to ..
  42. Hansen P, Poulsen C, Walter S, Marcussen N, Cribbs L, Skøtt O, et al. Functional importance of L- and P/Q-type voltage-gated calcium channels in human renal vasculature. Hypertension. 2011;58:464-70 pubmed publisher
    ..2×10(-8) mol/L. The T-type antagonist mibefradil inhibited the potassium-induced constriction with large variations between patients...
  43. Mandi G, Sarkar S, Mishra S, Raviprakash V. Effects of calcium channel blocker, mibefradil, and potassium channel opener, pinacidil, on the contractile response of mid-pregnant goat myometrium. Indian J Exp Biol. 2005;43:795-801 pubmed
    The present study was undertaken to investigate the in vitro influence of mibefradil, a calcium channel blocker, and pinacidil, a potassium channel opener, on pregnant goat myometrial spontaneous rhythmic contractility and contractions ..
  44. Heitmann J, Grote L, Knaack L, Kohler U, Hinder M, Peter J. Cardiovascular effects of mibefradil in hypertensive patients with obstructive sleep apnea. Eur J Clin Pharmacol. 1998;54:691-6 pubmed
    ..The objective of this study was to investigate the effects of the new T-selective calcium channel blocker mibefradil on invasively measured blood pressure (BP) and heart rate in hypertensive patients with OSA...
  45. Lacourciere Y, Poirier L, Lefebvre J, Archambault F, Dalle Ave S, Ward C, et al. The antihypertensive efficacy of the novel calcium antagonist mibefradil in comparison with nifedipine GITS in moderate to severe hypertensives with ambulatory hypertension. Am J Hypertens. 1997;10:189-96 pubmed
    b>Mibefradil is a novel calcium antagonist that blocks selectively the T-type calcium channels...
  46. Yue J, Liu L, Liu Z, Shu B, Zhang Y. Upregulation of T-type Ca2+ channels in primary sensory neurons in spinal nerve injury. Spine (Phila Pa 1976). 2013;38:463-70 pubmed publisher
    ..The effect of intrathecal administration of mibefradil in nerve-ligated rats was examined by painful behavior testing and current clamp...
  47. Osborne Pellegrin M, Labat C, Mercier N, Challande P, Lacolley P. Changes in aortic stiffness related to elastic fiber network anomalies in the Brown Norway rat during maturation and aging. Am J Physiol Heart Circ Physiol. 2010;299:H144-52 pubmed publisher
    ..Thereafter, age-related AA stiffness increased less in BN than in LE, likely due to the numerous IEL ruptures. We conclude that, in the BN rat, the lower E/C and the presence of IEL ruptures have opposing effects on arterial stiffness...
  48. Bonaccorsi L, Forti G, Baldi E. Low-voltage-activated calcium channels are not involved in capacitation and biological response to progesterone in human sperm. Int J Androl. 2001;24:341-51 pubmed
    ..responsiveness to P and capacitation, by employing three different pharmacological antagonists of VOCCT, namely mibefradil (Ro 5967), pimozide and amiloride...
  49. Chen Y, Tsaur M, Wang S, Wang T, Hung Y, Lin C, et al. Chronic intrathecal infusion of mibefradil, ethosuximide and nickel attenuates nerve ligation-induced pain in rats. Br J Anaesth. 2015;115:105-11 pubmed publisher
    ..After surgery, saline, mibefradil, ethosuximide or NiCl2 were given intrathecally for seven days...
  50. Levic S, Dulon D. The temporal characteristics of Ca2+ entry through L-type and T-type Ca2+ channels shape exocytosis efficiency in chick auditory hair cells during development. J Neurophysiol. 2012;108:3116-23 pubmed publisher
    ..10-12) use two types of Ca(2+) currents to control exocytosis: low-voltage-activating, rapidly inactivating (mibefradil sensitive) T-type Ca(2+) currents and high-voltage-activating, noninactivating (nifedipine sensitive) L-type ..
  51. Pool P. Neurohormonal activation in the treatment of congestive heart failure: basis for new treatments?. Cardiology. 1998;90:1-7 pubmed
  52. Chen C, Shen J, Chung N, Min M, Cheng S, Liu I. Retrieval of context-associated memory is dependent on the Ca(v)3.2 T-type calcium channel. PLoS ONE. 2012;7:e29384 pubmed publisher
    ..2 T-type Ca²? channel in the hippocampus. Wild-type mice infused with mibefradil, a T-type channel blocker, exhibited similar behaviors as homozygous knockouts...
  53. Grasic Kuhar C, Budihna M, Pleskovic R. Mibefradil is more effective than verapamil for restoring post-ischemic function of isolated hearts of guinea pigs with acute renal failure. Eur J Pharmacol. 2004;488:137-46 pubmed
    ..Two specific Ca(2+) channel antagonists, mibefradil (0.1 and 1 microM) and verapamil (0...
  54. Schwartz J. The evaluation of pharmacologic therapy in humans: a brief summary of the drug evaluation process and guidelines for clinical trials as they related to women. J Gend Specif Med. 2001;4:13-7 pubmed
    ..The prudent clinician will remember that every time a therapy is initiated for an individual patient, especially a female patient, it is a clinical trial and the outcome is uncertain. ..
  55. Himmel H, Stengel W, Ravens U. Selectivity of blocking of low- versus high-voltage activated calcium currents by the dihydropyridine derivatives Bay E5759 and Bay A4339 in neuroblastoma--glioma NG 108-15 cells. Pharmacol Res. 2001;44:113-6 pubmed
    ..Nisoldipine and mibefradil served as reference compounds...
  56. Lijnen P, Petrov V. Proliferation of human peripheral blood mononuclear cells during calcium entry blockade. Role of protein kinase C. Methods Find Exp Clin Pharmacol. 1999;21:253-9 pubmed
    ..PBMC) was investigated during calcium entry blockade with nifedipine (an L-type calcium channel blocker) and mibefradil (an L- and T-type calcium channel blocker with a higher selectivity for T-type channels)...
  57. Skov K, Fenger Grøn J, Mulvany M. Effects of an angiotensin-converting enzyme inhibitor, a calcium antagonist, and an endothelin receptor antagonist on renal afferent arteriolar structure. Hypertension. 1996;28:464-71 pubmed
    ..SHR with an ACE inhibitor (cilazapril, 5 to 10 mg/kg per day, high; 1 mg/kg per day, low), a calcium antagonist (mibefradil, 20 to 30 mg/kg per day), and an endothelin receptor antagonist (bosentan, 100 mg/kg per day) from age 4 to 20 ..
  58. Woo H, Lee Y, Roh E, Seo S, Song C, Chung H, et al. Synthesis and biological evaluation of 4-piperidinecarboxylate and 4-piperidinecyanide derivatives for T-type calcium channel blockers. Bioorg Med Chem Lett. 2011;21:5910-5 pubmed publisher
    ..85-71.99, hERG channel IC(50)=1.57 ± 0.14-4.98 ± 0.36 ?M). Selected compound 31a was evaluated on SNL model of neuropathic pain and showed inhibitory effect on mechanical allodynia. ..
  59. Xia Q, Reinecke A, Dorenkamp M, Storz C, Bitterling H, Penz S, et al. Comparison of cardioprotective effects of mibefradil and ramipril in stroke-prone spontaneously hypertensive rats. Acta Pharmacol Sin. 2004;25:763-8 pubmed
    To elucidate the cardioprotective effects of T-type calcium channel blocker mibefradil and compare with that of the angiotensin-converting enzyme inhibitor ramipril in a stroke-prone spontaneously hypertensive rats (SHR-SP) model of ..
  60. Ozturk H, Ozturk H, Duran H, Uzunlar A. Mibefradil, a T-type Ca2+ channel blocker, protects against mesenteric ischemia-reperfusion-induced oxidative injury and histologic alterations in intestinal mucosa in rats. Dig Dis Sci. 2006;51:1454-60 pubmed
    The purpose of the present study was to investigate whether mibefradil can reduce oxidative stress and histologic damage in the rat small bowel subjected to mesenteric ischemia and reperfusion injury...
  61. Doddareddy M, Choo H, Cho Y, Rhim H, Koh H, Lee J, et al. 3D pharmacophore based virtual screening of T-type calcium channel blockers. Bioorg Med Chem. 2007;15:1091-105 pubmed
    ..10 microM, eight times as potent as the known selective T-type calcium channel blocker, mibefradil. Search for similar compounds yielded several hits with micro-molar IC(50) values and high T-type calcium ..
  62. Park J, Choi J, Lee E, Lee J, Rhim H, Seo S, et al. Lead discovery and optimization of T-type calcium channel blockers. Bioorg Med Chem. 2007;15:1409-19 pubmed
    ..Among the library with 5 features, alkaneamide derivatives (7b, 9j, 11b, 11g, 11h) with 4-arylsubstituted piperazine showed better IC(50) values than Mibefradil.
  63. Lowie B, Wang X, White E, Huizinga J. On the origin of rhythmic calcium transients in the ICC-MP of the mouse small intestine. Am J Physiol Gastrointest Liver Physiol. 2011;301:G835-45 pubmed publisher
    ..With the use of calcium imaging, study of the effect of T-type calcium channel blocker mibefradil revealed that T-type channels did not play a major role in generating the calcium transients...
  64. Lee D, Goodman S, Dean D, Lenis J, Ma P, Gervais P, et al. Randomized comparison of T-type versus L-type calcium-channel blockade on exercise duration in stable angina: results of the Posicor Reduction of Ischemia During Exercise (PRIDE) trial. Am Heart J. 2002;144:60-7 pubmed
    b>Mibefradil is a T-type calcium-channel antagonist and arterial vasodilator with negative chronotropic effects...
  65. Fei H, Zhao B, Zhao S, Wang Q. Requirements of calcium fluxes and ERK kinase activation for glucose- and interleukin-1beta-induced beta-cell apoptosis. Mol Cell Biochem. 2008;315:75-84 pubmed publisher
    ..Finally, islet release of IL-1beta in response to high glucose could be abrogated by nimodipine, mibefradil, or PD98059...
  66. Yan D, Xiao C, Ma F, Wang L, Luo Y, Liu J, et al. Excitatory effects of low-level lead exposure on action potential firing of pyramidal neurons in CA1 region of rat hippocampal slices. J Neurosci Res. 2008;86:3665-73 pubmed publisher
    ..These excitatory effects of 5 microM lead were blocked by mibefradil, a selective blocker of T-type voltage-dependent calcium channels (VDCC), but not by verapamil and omega-..
  67. Taylor J, Huang L, Keyser B, Zhuang H, Clarkson C, Li M. Role of high-voltage-activated calcium channels in glucose-regulated beta-cell calcium homeostasis and insulin release. Am J Physiol Endocrinol Metab. 2005;289:E900-8 pubmed
    ..Using whole cell patch clamp, we found that N- and L-type channel currents increase gradually subsequent to lower intracellular calcium perfusion, suggesting that these channels may be regulated by glucose-induced changes in calcium. ..
  68. Tzivoni D, Gilula Z, Klutstein M, Reisin L, Botvin S, Kobrin I. The effect of mibefradil on ischemic episodes with and without increase in heart rate. Cardiovasc Drugs Ther. 2000;14:503-9 pubmed
    ..The purpose of this study was to assess the mechanism of action of mibefradil, a new T-channel calcium blocker that is a vasodilator with negative chronotropic properties...
  69. Hayashi K, Wakino S, Ozawa Y, Homma K, Kanda T, Okubo K, et al. Role of protein kinase C in Ca channel blocker-induced renal arteriolar dilation in spontaneously hypertensive rats--studies in the isolated perfused hydronephrotic kidney. Keio J Med. 2005;54:102-8 pubmed
    ..was used to visualize directly the renal microvascular effects of L-/T-type Ca channel blockers (nifedipine and mibefradil, respectively)...