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Chemical Compound Review

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

Synonyms: CHEMBL554054, SureCN871689, CNS-1102, SureCN7414862, C4238_SIGMA, ...
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Disease relevance of Aptiganel

  • The present study evaluated the neuroprotective efficacy of three noncompetitive NMDA receptor antagonists: Gacyclidine (GK-11), a new compound, Dizocilpine (MK-801), and Cerestat (CNS-1102) in a rat spinal cord contusion model [1].
  • Recent studies have demonstrated a neuroprotective effect of the noncompetitive N-methyl-D-aspartate receptor antagonist aptiganel HCl (Cerestat) in focal cerebral ischemia [2].

Psychiatry related information on Aptiganel

  • Conversely, cerestat (0.3, 1, and 3 mg/kg, sc) injected at 10 and 120 min postocclusion significantly reduced the ischemic volume at the dose of 1 mg/kg, and, at the same dose, significantly attenuated behavioural deficits in the body proprioception and in the forelimb flexion tests [3].

High impact information on Aptiganel

  • Cerestat and other NMDA antagonists in ischemic stroke [4].
  • This study investigated the ability of NBQX, an AMPA receptor antagonist, and cerestat, a NMDA receptor antagonist, to counteract neurological deficits and morphological damage induced by permanent occlusion of the left middle cerebral artery (MCAO model) in the rat [3].
  • Effects of cerestat and NBQX on functional and morphological outcomes in rat focal cerebral ischemia [3].
  • Cerestat reduced contusion volume from 77.3 +/- 5.8 mm3 to 66.8 +/- 3.9 mm3 (p < 0.05) [5].

Biological context of Aptiganel


Associations of Aptiganel with other chemical compounds

  • 2. Memantine and cerestat produced complete inhibition of ACh-induced inward currents with affinities similar to that reported for native NMDA receptors [6].


  1. 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]
  2. 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]
  3. Effects of cerestat and NBQX on functional and morphological outcomes in rat focal cerebral ischemia. Pitsikas, N., Brambilla, A., Besozzi, C., Bonali, P., Fodritto, F., Grippa, N., Scandroglio, A., Borsini, F. Pharmacol. Biochem. Behav. (2001) [Pubmed]
  4. Cerestat and other NMDA antagonists in ischemic stroke. Lees, K.R. Neurology (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. Inhibition of human alpha 7 nicotinic acetylcholine receptors by open channel blockers of N-methyl-D-aspartate receptors. Maskell, P.D., Speder, P., Newberry, N.R., Bermudez, I. Br. J. Pharmacol. (2003) [Pubmed]
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