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Chemical Compound Review

Prosynap     (2S)-1-[4-(benzothiazol-2-yl- methyl-amino)...

Synonyms: Lubeluzole, Prosynap (TN), CHEMBL281724, SureCN159725, JK-8792, ...
 
 
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Disease relevance of R 87926

 

Psychiatry related information on R 87926

 

High impact information on R 87926

  • BACKGROUND AND PURPOSE: We aimed to assess the safety and efficacy of lubeluzole in patients with a clinical diagnosis of acute (< 6 hours) ischemic stroke in the carotid artery territory [6].
  • In contrast to lubeluzole, DCLHb hemodilution prolonged T50 by 68% with no significant effect on Volmax [7].
  • Neuroprotection of lubeluzole is mediated through the signal transduction pathways of nitric oxide [2].
  • We also review NO-based therapeutic strategies for stroke treatment, not only those directly linked with the NO pathway such as NO donors and NOS inhibitors but also those partially related like statins, aspirin or lubeluzole [8].
  • Six fetuses were treated with lubeluzole (0.33 mg/kg estimated body weight) before induction of global cerebral ischemia (-90, -60, and -30 min), while the remainder (n = 7) received solvent [9].
 

Chemical compound and disease context of R 87926

  • In conclusion, the long-term neuroprotective property of lubeluzole against glutamate toxicity in hippocampal cultures is reflected by the fact of interference with the glutamateactivated nitric oxide synthase pathway [10].
  • Treatment of C6 glioma cells with lubeluzole did not affect lipopolysaccharide/gamma interferon induced guanosine 3',5'-cyclic monophosphate levels, suggesting that lubeluzole does not inhibit the glial nitric oxide synthase pathway [10].
  • Here we show that lubeluzole administered i.p. decreases by 25% the high (50 mM) K+-evoked accumulation of Tau in striatal microdialysates of healthy rats and by 34% in rats with thioacetamide-induced hepatic failure, where the increased extracellular accumulation of Tau signifies ongoing hepatic encephalopathy [11].
 

Biological context of R 87926

  • However, because the observation period lasted only 3 d, a possible effect of lubeluzole on pathophysiological mechanisms inducing delayed neuronal cell death cannot be fully excluded [9].
  • Lubeluzole and the (R)-enantiomer also blocked the high-voltage-activated calcium channel current (iHVA), with IC50 values of 2.6 and 3.5 microM, respectively, and accelerated the apparent inactivation of iHVA [12].
  • 8. The results suggest that lubeluzole and its R-isomer caused cytoprotection against veratridine cell damage, by blocking the veratridine stimulated Na+ and Ca2+ entry, as well as the [Ca2+]i oscillations [13].
  • Safety and pharmacokinetics of the neuroprotective drug lubeluzole in patients with ischemic stroke [14].
  • Effects of the antihypoxic and neuroprotective drug, lubeluzole, on repolarization phase of canine heart assessed by monophasic action potential recording [15].
 

Anatomical context of R 87926

 

Associations of R 87926 with other chemical compounds

  • 1. The effects of lubeluzole (a neuroprotective benzothiazole derivative) and its (-) enantiomer R91154 on whole-cell currents through Ca2+ channels, with 10 mM Ba2+ as charge carrier (IBa), have been studied in bovine and mouse voltage-clamped adrenal chromaffin cells [16].
  • Experiments with extracellular application of 3 microM lubeluzole (pK(a) = 7.6) at different values of extracellular pH suggest that the protonated form of lubeluzole contributes to the block of iLVA and iHVA from the extracellular side [4].
  • Effects of the neuroprotectant lubeluzole on the cytotoxic actions of veratridine, barium, ouabain and 6-hydroxydopamine in chromaffin cells [13].
  • Here we report about the effects of lubeluzole and its R-isomer on glutamate-induced neuronal cell death in mixed hippocampal cultures [18].
  • Blockade of the peri-infarct taurine response suggests that lubeluzole also may have reduced cellular osmotic stress in the peri-infarct zone [19].
 

Gene context of R 87926

  • Lubeluzole also was able to prevent the initial stages of cellular membrane inversion labeled with annexin-V binding, an early and sensitive indicator of PCD [5].
  • Combination Therapy Stroke Trial: recombinant tissue-type plasminogen activator with/without lubeluzole [20].
  • Surprisingly, neither the drug lubeluzole which was has been shown to prevent the GABAergic disinhibition observed after photothrombotic lesioning of rat neocortex, nor the prevention of spreading depressions by the NMDA-receptor antagonist MK-801 during lesion induction significantly affected the frequency of epileptiform discharges [21].
 

Analytical, diagnostic and therapeutic context of R 87926

References

  1. Protection with lubeluzole against delayed ischemic brain damage in rats. A quantitative histopathologic study. Haseldonckx, M., Van Reempts, J., Van de Ven, M., Wouters, L., Borgers, M. Stroke (1997) [Pubmed]
  2. Neuroprotection of lubeluzole is mediated through the signal transduction pathways of nitric oxide. Maiese, K., TenBroeke, M., Kue, I. J. Neurochem. (1997) [Pubmed]
  3. Lubeluzole following traumatic brain injury in the rat. Kroppenstedt, S.N., Stroop, R., Kern, M., Thomale, U.W., Schneider, G.H., Unterberg, A.W. J. Neurotrauma (1999) [Pubmed]
  4. Site of action of lubeluzole on voltage-sensitive Ca(2+) channels in isolated dorsal root ganglion cells of the rat: influence of pH. Marrannes, R., De Prins, E. J. Pharmacol. Exp. Ther. (2000) [Pubmed]
  5. Critical temporal modulation of neuronal programmed cell injury. Maiese, K., Vincent, A.M. Cell. Mol. Neurobiol. (2000) [Pubmed]
  6. Lubeluzole in acute ischemic stroke. A double-blind, placebo-controlled phase II trial. Lubeluzole International Study Group. Diener, H.C., Hacke, W., Hennerici, M., Rådberg, J., Hantson, L., De Keyser, J. Stroke (1996) [Pubmed]
  7. Combined neuroprotection and reperfusion therapy for stroke. Effect of lubeluzole and diaspirin cross-linked hemoglobin in experimental focal ischemia. Aronowski, J., Strong, R., Grotta, J.C. Stroke (1996) [Pubmed]
  8. Role of nitric oxide after brain ischaemia. Moro, M.A., Cárdenas, A., Hurtado, O., Leza, J.C., Lizasoain, I. Cell Calcium (2004) [Pubmed]
  9. Lubeluzole pretreatment does not provide neuroprotection against transient global cerebral ischemia in fetal sheep near term. Garnier, Y., Löbbert, T., Jensen, A., Berger, R. Pediatr. Res. (2002) [Pubmed]
  10. Lubeluzole, a novel long-term neuroprotectant, inhibits the glutamate-activated nitric oxide synthase pathway. Lesage, A.S., Peeters, L., Leysen, J.E. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  11. Lubeluzole attenuates K(+)-evoked extracellular accumulation of taurine in the striatum of healthy rats and rats with hepatic failure. Zielińska, M., Hilgier, W., Borkowska, H.D., Oja, S.S., Saransaari, P., Albrecht, J. Brain Res. (2001) [Pubmed]
  12. Influence of lubeluzole on voltage-sensitive Ca++ channels in isolated rat neurons. Marrannes, R., De Prins, E., Clincke, G. J. Pharmacol. Exp. Ther. (1998) [Pubmed]
  13. Effects of the neuroprotectant lubeluzole on the cytotoxic actions of veratridine, barium, ouabain and 6-hydroxydopamine in chromaffin cells. Cano-Abad, M.F., López, M.G., Hernández-Guijo, J.M., Zapater, P., Gandía, L., Sánchez-García, P., García, A.G. Br. J. Pharmacol. (1998) [Pubmed]
  14. Safety and pharmacokinetics of the neuroprotective drug lubeluzole in patients with ischemic stroke. De Keyser, J., Van de Velde, V., Schellens, R.L., Hantson, L., Tritsmans, L., Gheuens, J., Van Peer, A., Woestenborghs, R., Franke, C.L., van Gorp, J. Clinical therapeutics. (1997) [Pubmed]
  15. Effects of the antihypoxic and neuroprotective drug, lubeluzole, on repolarization phase of canine heart assessed by monophasic action potential recording. Sugiyama, A., Ni, C., Arita, J., Eto, K., Xue, Y.X., Hashimoto, K. Toxicol. Appl. Pharmacol. (1996) [Pubmed]
  16. Differential effects of the neuroprotectant lubeluzole on bovine and mouse chromaffin cell calcium channel subtypes. Hernández-Guijo, J.M., Gandía, L., de Pascual, R., García, A.G. Br. J. Pharmacol. (1997) [Pubmed]
  17. Treatment of experimental focal ischemia in rats with lubeluzole. Aronowski, J., Strong, R., Grotta, J.C. Neuropharmacology (1996) [Pubmed]
  18. Lubeluzole protects hippocampal neurons from excitotoxicity in vitro and reduces brain damage caused by ischemia. Culmsee, C., Junker, V., Wolz, P., Semkova, I., Krieglstein, J. Eur. J. Pharmacol. (1998) [Pubmed]
  19. Lubeluzole blocks increases in extracellular glutamate and taurine in the peri-infarct zone in rats. Scheller, D.K., De Ryck, M., Kolb, J., Szathmary, S., van Reempts, J., Clincke, G., Tegtmeier, F. Eur. J. Pharmacol. (1997) [Pubmed]
  20. Combination Therapy Stroke Trial: recombinant tissue-type plasminogen activator with/without lubeluzole. Grotta, J. Cerebrovasc. Dis. (2001) [Pubmed]
  21. Epileptiform discharges to extracellular stimuli in rat neocortical slices after photothrombotic infarction. Buchkremer-Ratzmann, I., August, M., Hagemann, G., Witte, O.W. J. Neurol. Sci. (1998) [Pubmed]
  22. Diffusion-weighted MRI of infarct growth in a rat photochemical stroke model: effect of lubeluzole. De Ryck, M., Verhoye, M., Van der Linden, A.M. Neuropharmacology (2000) [Pubmed]
 
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