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Chemical Compound Review

Licostinel     6,7-dichloro-5-nitro-1,4...

Synonyms: AC1NUOFE, CAT-213, iCo-008, ACEA-1021, CHEMBL289832, ...
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Disease relevance of Licostinel


Psychiatry related information on Licostinel

  • In the present study the effects of ACEA 1021 (5, 7.5, 8, 10, 15 and 20 mg/kg i.p.) on sniffing stereotypy, locomotor activity, prepulse inhibition of the acoustic startle response, the anti-cataleptic properties and spatial learning were tested [5].

High impact information on Licostinel

  • Licostinel may be a safer and better tolerated neuroprotective agent than many of the previously evaluated NMDA antagonists [1].
  • The purpose of this study was to assess the safety, tolerability, and pharmacokinetics of licostinel in patients with acute stroke [1].
  • For example, using fixed agonist concentrations (10 microM glycine and 100 microM glutamate) IC50 values for ACEA-1021 with four binary combinations were as follows: NMDA receptor (NR)1A/2A, 29 nM; NR1A/2B, 300 nM; NR1A/2C, 120 nM; NR1A/2D, 1500 nM [6].
  • Apparent dissociation constants (Kb values) for ACEA-1021 and ACEA-1031 ranged between 6 and 8 nM for oocyte assays and between 5 and 7 nM for neuronal assays [6].
  • Our results suggest that these additional effects of ACEA 1021 may contribute to its anticonvulsive properties in mice as well as to its neuroprotective properties in animal models of cerebral ischemia [7].

Chemical compound and disease context of Licostinel


Biological context of Licostinel


Anatomical context of Licostinel


Associations of Licostinel with other chemical compounds

  • Our results suggest that the in vivo neuro-protective actions of ACEA-1021 and ACEA-1031 are predominantly due to inhibition at NMDA receptor glycine sites, although additional inhibition at non-NMDA receptors may play an ancillary role [6].
  • The glycine-site modulators, (+)-HA-966, ACEA 1021 and milacemide, and the polyamine/NR2B-selective antagonist, eliprodil, also failed to substitute fully for NPC 17742 in rats and monkeys [14].

Analytical, diagnostic and therapeutic context of Licostinel

  • During MCAO and the first 24 h of reperfusion, rats (n = 10) were administered e55-nitro-6,7-dichloro-2,3-quinoxalinedione (ACEA 1021) i.v. as a bolus infusion of 5 mg/kg followed by 3.5 mg/kg/h (Low-Dose) or 10 mg/kg followed by 7 mg/kg/ h (High-Dose) for 24 h [15].
  • The bolus dose of ACEA-1021 was followed by a continuous intravenous infusion of vehicle or ACEA-1021 at 14 [3].


  1. Dose escalation study of the NMDA glycine-site antagonist licostinel in acute ischemic stroke. Albers, G.W., Clark, W.M., Atkinson, R.P., Madden, K., Data, J.L., Whitehouse, M.J. Stroke (1999) [Pubmed]
  2. In vivo models of cerebral ischemia: effects of parenterally administered NMDA receptor glycine site antagonists. Warner, D.S., Martin, H., Ludwig, P., McAllister, A., Keana, J.F., Weber, E. J. Cereb. Blood Flow Metab. (1995) [Pubmed]
  3. Glycine receptor antagonism. Effects of ACEA-1021 on the minimum alveolar concentration for halothane in the rat. McFarlane, C., Warner, D.S., Nader, A., Dexter, F. Anesthesiology (1995) [Pubmed]
  4. The effect of (R)-HA966 or ACEA 1021 on dexfenfluramine or (S)-MDMA-induced changes in temperature, activity, and neurotoxicity. Russell, B.R., Laverty, R. Pharmacol. Biochem. Behav. (2001) [Pubmed]
  5. ACEA 1021, a glycine site antagonist with minor psychotomimetic and amnestic effects in rats. Kretschmer, B.D., Kratzer, U., Breithecker, K., Koch, M. Eur. J. Pharmacol. (1997) [Pubmed]
  6. In vitro pharmacology of ACEA-1021 and ACEA-1031: systemically active quinoxalinediones with high affinity and selectivity for N-methyl-D-aspartate receptor glycine sites. Woodward, R.M., Huettner, J.E., Guastella, J., Keana, J.F., Weber, E. Mol. Pharmacol. (1995) [Pubmed]
  7. Reevaluation of ACEA 1021 as an antagonist at the strychnine-insensitive glycine site of the N-methyl-D-aspartate receptor. Lingenhöhl, K., Pozza, M.F. Neuropharmacology (1998) [Pubmed]
  8. In vivo neuroprotective effects of ACEA 1021 confirmed by magnetic resonance imaging in ischemic stroke. Petty, M.A., Neumann-Haefelin, C., Kalisch, J., Sarhan, S., Wettstein, J.G., Juretschke, H.P. Eur. J. Pharmacol. (2003) [Pubmed]
  9. Effects of NMDA receptor antagonists on cocaine-conditioned motor activity in rats. Bespalov, A.Y., Dravolina, O.A., Zvartau, E.E., Beardsley, P.M., Balster, R.L. Eur. J. Pharmacol. (2000) [Pubmed]
  10. Neuroprotective effects of NMDA receptor glycine recognition site antagonism: dependence on glycine concentration. Pearlstein, R.D., Beirne, J.P., Massey, G.W., Warner, D.S. J. Neurochem. (1998) [Pubmed]
  11. Synthesis and SAR of novel di- and trisubstituted 1,4-dihydroquinoxaline-2,3-diones related to licostinel (Acea 1021) as NMDA/glycine site antagonists. Zhou, Z.L., Kher, S.M., Cai, S.X., Whittemore, E.R., Espitia, S.A., Hawkinson, J.E., Tran, M., Woodward, R.M., Weber, E., Keana, J.F. Bioorg. Med. Chem. (2003) [Pubmed]
  12. ACEA 1021: flip or flop? Petty, M.A., Weintraub, P.M., Maynard, K.I. CNS drug reviews. (2004) [Pubmed]
  13. Glycine antagonism does not block ischemic spontaneous depolarization in the rat. Takaoka, S., Bart, R.D., Pearlstein, R.D., Warner, D.S. Neuroreport (1997) [Pubmed]
  14. Discriminative stimulus effects of site-selective N-methyl-D-aspartate antagonists in NPC 17742-trained rats and squirrel monkeys. Wiley, J.L., Li, H., Balster, R.L. Psychopharmacology (Berl.) (1997) [Pubmed]
  15. Neuroprotective effect of NMDA receptor glycine recognition site antagonism persists when brain temperature is controlled. Takaoka, S., Bart, R.D., Pearlstein, R., Brinkhous, A., Warner, D.S. J. Cereb. Blood Flow Metab. (1997) [Pubmed]
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