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Chemical Compound Review

Flupirtine     ethyl N-[2-amino-6-[(4...

Synonyms: Flupirtino, Flupirtinum, Lopac-F-8927, SureCN25009, CHEMBL255044, ...
 
 
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Disease relevance of Flupirtine

 

Psychiatry related information on Flupirtine

 

High impact information on Flupirtine

  • Flupirtine also prevents the death of CLN3- and CLN2-deficient postmitotic hNT neurons at the mitochondrial level [1].
  • Flupirtine blocks apoptosis in batten patient lymphoblasts and in human postmitotic CLN3- and CLN2-deficient neurons [1].
  • The selective potential of flupirtine to reduce apoptosis without influencing uninduced apoptosis may qualify this compound as a potential drug in the therapy of HIV-1 infected patients [2].
  • In the present study we demonstrate that flupirtine, an already clinically used, centrally acting, non-opiate analgesic agent, protects rat cortical neurons against HIV-gp120 induced apoptotic cell death [2].
  • The anti-apoptotic effect of flupirtine was restricted to CD3+ lymphocytes and in particular to CD4+ cells [2].
 

Chemical compound and disease context of Flupirtine

 

Biological context of Flupirtine

 

Anatomical context of Flupirtine

 

Associations of Flupirtine with other chemical compounds

 

Gene context of Flupirtine

  • Furthermore, addition of 10 or 100 microM: flupirtine before incubation with TNF-alpha led to an approximately threefold increase of Bcl-2 expression [22].
  • Our data demonstrate that flupirtine up-regulates the expression of Bcl-2 protein in OLN cells; this Bcl-2 induction is associated with a reduced rate of TNF-alpha-induced cell death [22].
  • In contrast, the oncogene proteins for TIAR and ICH-1t, were lower in flupirtine-treated cells than in control cells [16].
  • By contrast, retigabine and flupirtine (each at 10 microM) were less effective in counteracting NMDA- or OGD-induced toxicity in the CA1 region [21].
  • Based on these in vitro data and on the favorable pharmacokinetic profile of the drug, we strongly suggest that flupirtine may prove useful for treatment of patients with prion disease [5].
 

Analytical, diagnostic and therapeutic context of Flupirtine

  • The results indicate that flupirtine produces analgesia by spinal inhibition of nociceptive impulse transmission from afferent nerve fibres to neurones sending their axons to the brain and, in addition, by supraspinal inhibition of nociceptive impulse transmission to the thalamus [23].
  • Microinjection of flupirtine (1.7 micrograms/rat) made in the PAG did not reduce, but increased the spontaneous and C fibre-evoked activity in ascending axons [24].
  • Flupirtine administered 20 min before ischaemia reduced the depression of the b-wave during occlusion and accelerated recovery during reperfusion [25].
  • Quantitation of flupirtine and its active acetylated metabolite by reversed-phase high-performance liquid chromatography using fluorometric detection [26].
  • Pentazocine and flupirtine effects on spontaneous and evoked EEG activity [27].

References

  1. Flupirtine blocks apoptosis in batten patient lymphoblasts and in human postmitotic CLN3- and CLN2-deficient neurons. Dhar, S., Bitting, R.L., Rylova, S.N., Jansen, P.J., Lockhart, E., Koeberl, D.D., Amalfitano, A., Boustany, R.M. Ann. Neurol. (2002) [Pubmed]
  2. Flupirtine protects both neuronal cells and lymphocytes against induced apoptosis in vitro: implications for treatment of AIDS patients. Müller, W.E., Dobmeyer, J.M., Dobmeyer, T.S., Pergande, G., Perovic, S., Leuck, J., Rossol, R. Cell Death Differ. (1997) [Pubmed]
  3. Protection of rabbit retina from ischemic injury by flupirtine. Osborne, N.N., Schwarz, M., Pergande, G. Invest. Ophthalmol. Vis. Sci. (1996) [Pubmed]
  4. Protection of flupirtine on beta-amyloid-induced apoptosis in neuronal cells in vitro: prevention of amyloid-induced glutathione depletion. Müller, W.E., Romero, F.J., Perovic, S., Pergande, G., Pialoglou, P. J. Neurochem. (1997) [Pubmed]
  5. Effect of flupirtine on Bcl-2 and glutathione level in neuronal cells treated in vitro with the prion protein fragment (PrP106-126). Perovic, S., Schröder, H.C., Pergande, G., Ushijima, H., Müller, W.E. Exp. Neurol. (1997) [Pubmed]
  6. Evaluation of the abuse potential of the novel analgesic flupirtine maleate. Preston, K.L., Funderburk, F.R., Liebson, I.A., Bigelow, G.E. Drug and alcohol dependence. (1991) [Pubmed]
  7. Novel approaches in diagnosis and therapy of Creutzfeldt-Jakob disease. Müller, W.E., Laplanche, J.L., Ushijima, H., Schröder, H.C. Mech. Ageing Dev. (2000) [Pubmed]
  8. Antiparkinsonian effect of flupirtine in monoamine-depleted rats. Schwarz, M., Nolden-Koch, M., Purr, J., Pergande, G., Block, F. Journal of neural transmission (Vienna, Austria : 1996) (1996) [Pubmed]
  9. Possible involvement of noradrenergic descending pain-modulating pathways in the mode of antinociceptive action of flupirtine, a novel non-opioid analgesic. Nickel, B., Engel, J., Szelenyi, I. Agents Actions (1988) [Pubmed]
  10. Comparative physical dependence studies in rats with flupirtine and opiate receptor stimulating analgesics. Nickel, B., Aledter, A. Postgraduate medical journal. (1987) [Pubmed]
  11. Influence of flupirtine on a G-protein coupled inwardly rectifying potassium current in hippocampal neurones. Jakob, R., Krieglstein, J. Br. J. Pharmacol. (1997) [Pubmed]
  12. Antidystonic effects of K(v)7 (KCNQ) channel openers in the dt(sz) mutant, an animal model of primary paroxysmal dystonia. Richter, A., Sander, S.E., Rundfeldt, C. Br. J. Pharmacol. (2006) [Pubmed]
  13. Clinical trial of flupirtine maleate in patients with migraine. Million, R., Finlay, B.R., Whittington, J.R. Current medical research and opinion. (1984) [Pubmed]
  14. Pharmacological intervention in age-associated brain disorders by Flupirtine: Alzheimer's and prion diseases. Perovic, S., Böhm, M., Meesters, E., Meinhardt, A., Pergande, G., Müller, W.E. Mech. Ageing Dev. (1998) [Pubmed]
  15. KCNQ/M-currents contribute to the resting membrane potential in rat visceral sensory neurons. Wladyka, C.L., Kunze, D.L. J. Physiol. (Lond.) (2006) [Pubmed]
  16. Induction of apoptosis in cultured human retinal pigment epithelial cells is counteracted by flupirtine. Osborne, N.N., Cazevieille, C., Pergande, G., Wood, J.P. Invest. Ophthalmol. Vis. Sci. (1997) [Pubmed]
  17. Protection of mitochondrial integrity from oxidative stress by the triaminopyridine derivative flupirtine. Schlüter, T., Struy, H., Schönfeld, P. FEBS Lett. (2000) [Pubmed]
  18. Flupirtine. A review of its pharmacological properties, and therapeutic efficacy in pain states. Friedel, H.A., Fitton, A. Drugs (1993) [Pubmed]
  19. Effect of the triaminopyridine flupirtine on calcium uptake, membrane potential and ATP synthesis in rat heart mitochondria. Zimmer, G., Balakirev, M., Zwicker, K., Hofmann, M., Woodcock, B.G., Pergande, G. Br. J. Pharmacol. (1998) [Pubmed]
  20. Melatonin counteracts ischemia-induced apoptosis in human retinal pigment epithelial cells. Osborne, N.N., Nash, M.S., Wood, J.P. Invest. Ophthalmol. Vis. Sci. (1998) [Pubmed]
  21. Retigabine and flupirtine exert neuroprotective actions in organotypic hippocampal cultures. Boscia, F., Annunziato, L., Taglialatela, M. Neuropharmacology (2006) [Pubmed]
  22. Association of increased bcl-2 expression with rescue from tumor necrosis factor-alpha-induced cell death in the oligodendrocyte cell line OLN-93. Burgmaier, G., Schönrock, L.M., Kuhlmann, T., Richter-Landsberg, C., Brück, W. J. Neurochem. (2000) [Pubmed]
  23. Flupirtine depresses nociceptive activity evoked in rat thalamus. Bleyer, H., Carlsson, K.H., Erkel, H.J., Jurna, I. Eur. J. Pharmacol. (1988) [Pubmed]
  24. Depression by flupirtine, a novel analgesic agent, of motor and sensory responses of the nociceptive system in the rat spinal cord. Carlsson, K.H., Jurna, I. Eur. J. Pharmacol. (1987) [Pubmed]
  25. Flupirtine protects against ischaemic retinal dysfunction in rats. Block, F., Pergande, G., Schwarz, M. Neuroreport (1994) [Pubmed]
  26. Quantitation of flupirtine and its active acetylated metabolite by reversed-phase high-performance liquid chromatography using fluorometric detection. Narang, P.K., Tourville, J.F., Chatterji, D.C., Gallelli, J.F. J. Chromatogr. (1984) [Pubmed]
  27. Pentazocine and flupirtine effects on spontaneous and evoked EEG activity. Bromm, B., Ganzel, R., Herrmann, W.M., Meier, W., Scharein, E. Neuropsychobiology (1986) [Pubmed]
 
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