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Chemical Compound Review

Aptiganel     1-(3-ethylphenyl)-1-methyl-2- naphthalen-1...

Synonyms: Lopac-C-4238, CHEMBL92484, SureCN151144, SureCN151145, ACMC-20mwh1, ...
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Disease relevance of Aptiganel


High impact information on Aptiganel

  • In human volunteers, dose-limiting effects of aptiganel are blood pressure increases and central nervous system (CNS) excitation or depression [6].
  • Clinical experience suggests that although some NMDA antagonists are poorly tolerated at putative neuroprotective doses (e.g., selfotel), potentially neuroprotective plasma concentrations can be achieved in humans with others (e.g., aptiganel), though tolerable adverse effects are frequently observed [7].
  • Although recent studies with selfotel and eliprodil have been discontinued because of insufficient evidence for a satisfactory risk/benefit ratio, encouraging experience with aptiganel, magnesium, and glycine antagonists has prompted continued clinical trials with these agents [7].
  • Aptiganel inhibits c-Jun expression, attenuates neuronal necrosis, and improves outcome [8].
  • Immediate-early gene expression in ovine brain after hypothermic circulatory arrest: effects of aptiganel [9].

Chemical compound and disease context of Aptiganel


Associations of Aptiganel with other chemical compounds


Analytical, diagnostic and therapeutic context of Aptiganel

  • CONCLUSIONS: A 4.5-mg intravenous bolus of aptiganel HCl followed by infusion of 0.75 mg/h for 12 hours is a tolerable dose that can produce plasma drug concentrations shown to be neuroprotective in animal models [6].
  • The non-competitive antagonist, aptiganel, is currently in Phase III clinical trials and its therapeutic efficacy and index should be defined in 1997 and 1998 [12].


  1. Clinical experience with excitatory amino acid antagonist drugs. Muir, K.W., Lees, K.R. Stroke (1995) [Pubmed]
  2. Synthesis and pharmacological evaluation of N-(2,5-disubstituted phenyl)-N'-(3-substituted phenyl)-N'-methylguanidines as N-methyl-D-aspartate receptor ion-channel blockers. Hu, L.Y., Guo, J., Magar, S.S., Fischer, J.B., Burke-Howie, K.J., Durant, G.J. J. Med. Chem. (1997) [Pubmed]
  3. Protective effects of aptiganel HCl (Cerestat) following controlled cortical impact injury in the rat. Kroppenstedt, S.N., Schneider, G.H., Thomale, U.W., Unterberg, A.W. J. Neurotrauma (1998) [Pubmed]
  4. Effects of prolonged infusions of the NMDA antagonist aptiganel hydrochloride (CNS 1102) in normal volunteers. Muir, K.W., Grosset, D.G., Lees, K.R. Clinical neuropharmacology. (1997) [Pubmed]
  5. Neuroprotective properties of aptiganel HCL (Cerestat) following controlled cortical impact injury. Kroppenstedt, S.N., Schneider, G.H., Thomale, U.W., Unterberg, A.W. Acta Neurochir. Suppl. (1998) [Pubmed]
  6. Safety and tolerability study of aptiganel hydrochloride in patients with an acute ischemic stroke. Dyker, A.G., Edwards, K.R., Fayad, P.B., Hormes, J.T., Lees, K.R. Stroke (1999) [Pubmed]
  7. Cerestat and other NMDA antagonists in ischemic stroke. Lees, K.R. Neurology (1997) [Pubmed]
  8. Differential immediate-early gene expression in ovine brain after cardiopulmonary bypass and hypothermic circulatory arrest. Bokesch, P.M., Seirafi, P.A., Warner, K.G., Marchand, J.E., Kream, R.M., Trapp, B. Anesthesiology (1998) [Pubmed]
  9. Immediate-early gene expression in ovine brain after hypothermic circulatory arrest: effects of aptiganel. Bokesch, P.M., Halpin, D.P., Ranger, W.R., Drummond-Webb, J.J., Marchand, J.E., Bronson, R.T., Warner, K.G., Kream, R.M. Ann. Thorac. Surg. (1997) [Pubmed]
  10. Why did NMDA receptor antagonists fail clinical trials for stroke and traumatic brain injury? Ikonomidou, C., Turski, L. Lancet neurology. (2002) [Pubmed]
  11. Development of the NMDA ion-channel blocker, aptiganel hydrochloride, as a neuroprotective agent for acute CNS injury. McBurney, R.N. Int. Rev. Neurobiol. (1997) [Pubmed]
  12. N-methyl-D-aspartate antagonists for stroke and head trauma. Wood, P.L., Hawkinson, J.E. Expert opinion on investigational drugs. (1997) [Pubmed]
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