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Chemical Compound Review

Gacyclidine     1-[(1R,2S)-2-methyl-1- thiophen-2-yl...

Synonyms: GK-11, PubChem24062, GK11, SureCN397836, CHEMBL1742478, ...
 
 
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Disease relevance of Gacyclidine

 

High impact information on Gacyclidine

 

Biological context of Gacyclidine

 

Anatomical context of Gacyclidine

 

Associations of Gacyclidine with other chemical compounds

  • The aim of this study was to analyze the optimal time-window for neuroprotection by a novel NMDA antagonist, Gacyclidine, after experimental spinal cord injury, in terms of its functional, histopathological and electrophysiological effects [10].
  • The pharmacological characterization and mode of action of numerous drugs was presented, including IL-1ra, ARL-17477, zVAD-fmk, L-790984, CEP-1347, gacyclidine, NBI-30775, AWD-131-138, flumazenil, ondansetron, LY-367385, MPEP, and NBI-34060 [11].
 

Gene context of Gacyclidine

  • Globally, the current lack of any other NMDA receptor antagonist suitable for human use reinforces the therapeutic value of gacyclidine as a central nervous system protective agent for the treatment of OP poisoning [12].
  • Gacyclidine enantiomers and PCP were monitored using the fragment ions at m/z 206 and 200, respectively [13].
 

Analytical, diagnostic and therapeutic context of Gacyclidine

  • As Gacyclidine is already in clinical trials, the present findings suggest the premise that it is a promising agent for limiting the initial neuronal damage induced by CNS trauma leading to better functional recovery [14].
  • This simple and rapid assay (total run time < 10 min) was validated for a pilot pharmacokinetic study in healthy rats after intravenous injection of a bolus dose of gacyclidine (2.5 mg kg-1) [15].
  • The novel non-competitive N-methyl-D-aspartate antagonist gacyclidine blocks the glutamate-induced release of hydroxyl radicals in the striatum under conditions in which dizocilpine does not. A microdialysis study in rats [16].
  • This review summarizes the therapeutic value of gacyclidine as a complement to the available emergency treatment against severe organophosphate poisoning [12].
  • However, only gacyclidine is able to ensure complete management of nerve agent poisoning for rapid normalization of EEG activity, clinical recovery and neuroprotection [12].

References

  1. Acute soman poisoning in primates neither pretreated nor receiving immediate therapy: value of gacyclidine (GK-11) in delayed medical support. Lallement, G., Clarençon, D., Galonnier, M., Baubichon, D., Burckhart, M.F., Peoc'h, M. Arch. Toxicol. (1999) [Pubmed]
  2. Gacyclidine: a new neuroprotective agent acting at the N-methyl-D-aspartate receptor. Hirbec, H., Gaviria, M., Vignon, J. CNS drug reviews. (2001) [Pubmed]
  3. Characterization of 'non-N-methyl-D-Aspartate' binding sites for gacyclidine enantiomers in the rat cerebellar and telencephalic structures. Hirbec, H., Kamenka, J.M., Privat, A., Vignon, J. J. Neurochem. (2001) [Pubmed]
  4. Neuroprotective effects of gacyclidine after experimental photochemical spinal cord lesion in adult rats: dose-window and time-window effects. Gaviria, M., Privat, A., d'Arbigny, P., Kamenka, J.M., Haton, H., Ohanna, F. J. Neurotrauma (2000) [Pubmed]
  5. Interaction of gacyclidine enantiomers with 'non-NMDA' binding sites in the rat central nervous system. Hirbec, H., Kamenka, J.M., Privat, A., Vignon, J. Brain Res. (2001) [Pubmed]
  6. Distribution of gacyclidine enantiomers after experimental spinal cord injury in rats: possible involvement of an active transport system. Hoizey, G., Kaltenbach, M.L., Dukic, S., Lamiable, D., Lallemand, A., Millart, H., D'Arbigny, P., Vistelle, R. Journal of pharmaceutical sciences. (2001) [Pubmed]
  7. Distribution of gacyclidine enantiomers in spinal cord extracellular fluid. Hoizey, G., Kaltenbach, M.L., Dukic, S., Lamiable, D., Lallemand, A., D'Arbigny, P., Millart, H., Vistelle, R. Pharm. Res. (2000) [Pubmed]
  8. Binding properties of [3H]gacyclidine (cis(pip/me)-1-[1-(2-thienyl)-2-methylcyclohexyl]piperidine) enantiomers in the rat central nervous system. Hirbec, H., Teilhac, J., Kamenka, J., Privat, A., Vignon, J. Brain Res. (2000) [Pubmed]
  9. Binding properties of [3H]gacyclidine in the rat central nervous system. Hirbec, H., Privat, A., Vignon, J. Eur. J. Pharmacol. (2000) [Pubmed]
  10. Neuroprotective effects of a novel NMDA antagonist, Gacyclidine, after experimental contusive spinal cord injury in adult rats. Gaviria, M., Privat, A., d'Arbigny, P., Kamenka, J., Haton, H., Ohanna, F. Brain Res. (2000) [Pubmed]
  11. FENS 2000--Federation of European Neuroscience Societies. 24-28 June 2000, Brighton, UK. Hannan, A. IDrugs : the investigational drugs journal. (2000) [Pubmed]
  12. Review of the value of gacyclidine (GK-11) as adjuvant medication to conventional treatments of organophosphate poisoning: primate experiments mimicking various scenarios of military or terrorist attack by soman. Lallement, G., Baubichon, D., Clarençon, D., Galonnier, M., Peoc'h, M., Carpentier, P. Neurotoxicology (1999) [Pubmed]
  13. Determination of gacyclidine enantiomers in human plasma by gas chromatography-mass spectrometry using selected-ion monitoring. Hoizey, G., Vistelle, R., Lamiable, D., Millart, H., Gourdier, B., d'Arbigny, P. J. Chromatogr. B Biomed. Sci. Appl. (1997) [Pubmed]
  14. Efficacy of a new neuroprotective agent, gacyclidine, in a model of rat spinal cord injury. Feldblum, S., Arnaud, S., Simon, M., Rabin, O., D'Arbigny, P. J. Neurotrauma (2000) [Pubmed]
  15. Sensitive gas chromatographic-mass spectrometric method for the determination of gacyclidine in rat plasma and spinal cord dialyzates. Hoizey, G., Lamiable, D., Dukic, S., Millart, H., d'Arbigny, P., Vistelle, R. The Analyst. (1999) [Pubmed]
  16. The novel non-competitive N-methyl-D-aspartate antagonist gacyclidine blocks the glutamate-induced release of hydroxyl radicals in the striatum under conditions in which dizocilpine does not. A microdialysis study in rats. Laplanche, L., Kamenka, J.M., Barbanel, G. Neurosci. Lett. (2000) [Pubmed]
 
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