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Chemical Compound Review

Sibelium     1-[bis(4- fluorophenyl)methyl]-4- cinnamyl...

Synonyms: Flufenal, Fluvert, Narzine, Zinasen, Flunarizin, ...
 
 
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Disease relevance of Sibelium

 

Psychiatry related information on Sibelium

 

High impact information on Sibelium

 

Chemical compound and disease context of Sibelium

 

Biological context of Sibelium

 

Anatomical context of Sibelium

 

Associations of Sibelium with other chemical compounds

 

Gene context of Sibelium

  • Flunarizine also inhibits KCNQ1/KCNE1 channel current with an IC50 of 0.76 microM [30].
  • Serum prolactin is increased during chronic flunarizine treatment of patients suffering from migraine [31].
  • The effect of flunarizine on hERG potassium current is concentration and time dependent, and displays voltage dependence over the voltage range between -40 and 0 mV [30].
  • Concomitant with an increase in viability, treatment with flunarizine resulted in a marked dissociation of Nrf2/Keap1 and subsequent intranuclear translocation of Nrf2, which was mediated by PI3K-Akt signaling [18].
  • A paradoxical increase of growth hormone to thyrotropin releasing hormone observed before therapy was blunted after flunarizine treatment [32].
 

Analytical, diagnostic and therapeutic context of Sibelium

  • Flunarizine protects neurons from death after axotomy or NGF deprivation [10].
  • In cell culture, flunarizine at 30 to 40 microM also prevented neuronal death in nerve growth factor-dependent embryonic sensory and sympathetic neurons after the abrupt withdrawal of neurotrophic support [10].
  • 12 subjects, 8 women and 4 men, presented with extrapyramidal motor signs and psychic depression after treatment with flunarizine for between 3 weeks and 15 months [2].
  • Using 113Sn-labeled microspheres, 25 micron in diameter, we measured blood flow to primary tumors and regional lymph node metastases in conscious SMT-2A mammary adenocarcinoma-bearing syngeneic rats following a single i.v. bolus injection of the calcium entry blocker, flunarizine [22].
  • After reperfusion the dogs received the calcium entry blocker, flunarizine, 6 micrograms/kg infused over a ten minute period [33].

References

  1. Flunarizine in alternating hemiplegia in childhood. Casaer, P., Azou, M. Lancet (1984) [Pubmed]
  2. Parkinsonism, tardive dyskinesia, akathisia, and depression induced by flunarizine. Chouza, C., Scaramelli, A., Caamaño, J.L., De Medina, O., Aljanati, R., Romero, S. Lancet (1986) [Pubmed]
  3. Flunarizine: a once-daily therapy for urinary incontinence. Palmer, J.H., Worth, P.H., Exton-Smith, A.N. Lancet (1981) [Pubmed]
  4. Flunarizine allows differentiation between mechanisms of arrhythmias in the intact heart. Vos, M.A., Gorgels, A.P., Leunissen, J.D., Wellens, H.J. Circulation (1990) [Pubmed]
  5. Flunarizine as maintenance treatment of a patient with bipolar disorder. Lindelius, R., Nilsson, C.G. The American journal of psychiatry. (1992) [Pubmed]
  6. Photochemical stroke model: flunarizine prevents sensorimotor deficits after neocortical infarcts in rats. De Ryck, M., Van Reempts, J., Borgers, M., Wauquier, A., Janssen, P.A. Stroke (1989) [Pubmed]
  7. Cyclandelate versus flunarizine. A double-blind study in a selected group of patients with dementia. Albizzati, M.G., Bassi, S., Calloni, E., Sbacchi, M., Piolti, R., Frattola, L. Drugs (1987) [Pubmed]
  8. Influence of flunarizine, nicardipine and nimodipine on the anticonvulsant activity of different antiepileptic drugs in mice. Czuczwar, S.J., Gasior, M., Janusz, W., Kleinrok, Z. Neuropharmacology (1992) [Pubmed]
  9. Pharmacological protection against hypoxia-induced effects on medium-term memory in a two-way avoidance paradigm. Clincke, G.H., Wauquier, A. Behav. Brain Res. (1984) [Pubmed]
  10. Flunarizine protects neurons from death after axotomy or NGF deprivation. Rich, K.M., Hollowell, J.P. Science (1990) [Pubmed]
  11. Parkinsonism, tardive dyskinesia, akathisia, and depression induced by flunarizine. Meyboom, R.H., Ferrari, M.D., Dieleman, B.P. Lancet (1986) [Pubmed]
  12. Mechanisms of flunarizine-induced vasodilation in the rabbit mesenteric artery. Itoh, T., Satoh, S., Ishimatsu, T., Fujiwara, T., Kanmura, Y. Circ. Res. (1987) [Pubmed]
  13. Specificity of action of Ca++ entry blockers. A comparison of their actions in rat arteries and in human coronary arteries. Godfraind, T., Miller, R.C. Circ. Res. (1983) [Pubmed]
  14. Significance of prostaglandin E2 in acute necrotising pancreatitis in rats. van Ooijen, B., Kort, W.J., Tinga, C.J., Wilson, J.H., Westbroek, D.L. Gut (1989) [Pubmed]
  15. Functional, behavioral, and histological changes induced by transient global cerebral ischemia in rats: effects of cinnarizine and flunarizine. Poignet, H., Beaughard, M., Lecoin, G., Massingham, R. J. Cereb. Blood Flow Metab. (1989) [Pubmed]
  16. [3H]Phenytoin identifies a novel anticonvulsant-binding domain on voltage-dependent sodium channels. Francis, J., Burnham, W.M. Mol. Pharmacol. (1992) [Pubmed]
  17. Topical flunarizine reduces IOP and protects the retina against ischemia-excitotoxicity. Osborne, N.N., Wood, J.P., Cupido, A., Melena, J., Chidlow, G. Invest. Ophthalmol. Vis. Sci. (2002) [Pubmed]
  18. Flunarizine induces Nrf2-mediated transcriptional activation of heme oxygenase-1 in protection of auditory cells from cisplatin. So, H.S., Kim, H.J., Lee, J.H., Lee, J.H., Park, S.Y., Park, C., Kim, Y.H., Kim, J.K., Lee, K.M., Kim, K.S., Chung, S.Y., Jang, W.C., Moon, S.K., Chung, H.T., Park, R.K. Cell Death Differ. (2006) [Pubmed]
  19. Effect of flunarizine and calcium on serotonin uptake in human and rat blood platelets and rat synaptosomes. Jensen, P.N., Smith, D.F., Poulsen, J.H., Møller, H.J., Rosenberg, R. Biol. Psychiatry (1994) [Pubmed]
  20. Flunarizine reduces cerebral infarct size after photochemically induced thrombosis in spontaneously hypertensive rats. Van Reempts, J., Van Deuren, B., Van de Ven, M., Cornelissen, F., Borgers, M. Stroke (1987) [Pubmed]
  21. Hemodynamic and metabolic effects of flunarizine in experimental subarachnoid hemorrhage in dogs. De Ley, G., Eechaute, W., Strijckmans, K., Goethals, P., Lemahieu, I., Van de Velde, E., Weyne, J. Stroke (1993) [Pubmed]
  22. Blood flow to primary tumors and lymph node metastases in SMT-2A tumor-bearing rats following intravenous flunarizine. Kaelin, W.G., Shrivastav, S., Jirtle, R.L. Cancer Res. (1984) [Pubmed]
  23. Third Activity of Bordetella Adenylate Cyclase (AC) Toxin-Hemolysin: MEMBRANE TRANSLOCATION OF AC DOMAIN POLYPEPTIDE PROMOTES CALCIUM INFLUX INTO CD11b+ MONOCYTES INDEPENDENTLY OF THE CATALYTIC AND HEMOLYTIC ACTIVITIES. Fiser, R., Masín, J., Basler, M., Krusek, J., Spuláková, V., Konopásek, I., Sebo, P. J. Biol. Chem. (2007) [Pubmed]
  24. Effects of flunarizine on neurological recovery and spinal cord blood flow in experimental spinal cord ischemia in rabbits. Johnson, S.H., Kraimer, J.M., Graeber, G.M. Stroke (1993) [Pubmed]
  25. Protective effect of flunarizine on blood-brain barrier permeability alterations in acutely hypertensive rats. Nag, S. Stroke (1991) [Pubmed]
  26. Involvement of calcium-activated potassium channels in the regulation of DNA synthesis in cultured Müller glial cells. Kodal, H., Weick, M., Moll, V., Biedermann, B., Reichenbach, A., Bringmann, A. Invest. Ophthalmol. Vis. Sci. (2000) [Pubmed]
  27. Receptors on the neutrophil membrane. I. Flunarizine-adenosine antagonism as detected by 1H-nuclear magnetic resonance relaxation investigations. Di Perri, T., Orrico, A., Laghi Pasini, F., Gaggelli, E., Valensin, G. Biophys. J. (1987) [Pubmed]
  28. Influence of cyclandelate on in vitro red blood cell deformability. Hall, D.W., van den Hoven, W.E. Drugs (1987) [Pubmed]
  29. Flunarizine as a modulator of doxorubicin resistance in human colon-adenocarcinoma cells. Silvestrini, R., Zaffaroni, N., Costa, A., Orlandi, L., Villa, R., Hendriks, H.R. Int. J. Cancer (1993) [Pubmed]
  30. Flunarizine is a highly potent inhibitor of cardiac hERG potassium current. Trepakova, E.S., Dech, S.J., Salata, J.J. J. Cardiovasc. Pharmacol. (2006) [Pubmed]
  31. Nimodipine in migraine: clinical efficacy and endocrinological effects. Formisano, R., Falaschi, P., Cerbo, R., Proietti, A., Catarci, T., D'Urso, R., Roberti, C., Aloise, V., Chiarotti, F., Agnoli, A. Eur. J. Clin. Pharmacol. (1991) [Pubmed]
  32. Possible involvement of dopaminergic mechanisms in the antimigraine action of flunarizine. Piccini, P., Nuti, A., Paoletti, A.M., Napolitano, A., Melis, G.B., Bonuccelli, U. Cephalalgia : an international journal of headache. (1990) [Pubmed]
  33. Failure of flunarizine to improve cerebral blood flow or neurologic recovery in a canine model of complete cerebral ischemia. Newberg, L.A., Steen, P.A., Milde, J.H., Michenfelder, J.D. Stroke (1984) [Pubmed]
 
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