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Chemical Compound Review

CGP-39551     [(E)-4-amino-4- ethoxycarbonyl-2-methyl- but...

Synonyms: Cgp 39551, LS-183922, AC1O4M9I, 127910-32-1, MolPort-003-983-537
 
 
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Disease relevance of Cgp 39551

  • The time course of action of CGP 39551 is exceptionally prolonged: 42 mumol/kg i.p. protects against clonic seizures for 48 h [1].
  • Anticonvulsant activity of two orally active competitive N-methyl-D-aspartate antagonists, CGP 37849 and CGP 39551, against sound-induced seizures in DBA/2 mice and photically induced myoclonus in Papio papio [1].
  • CGP 39551 significantly ameliorated the signs of HPNS, compared with controls, at pressures above 31 ATA and prevented the severe signs from occurring at the higher pressures [2].
  • This result suggests a wider therapeutic range for CGP 39551 and especially for CGP 37849 than for MK-801 in the treatment of epilepsy [3].
  • After CGP 39551 administration, a decreased muscle tension was observed, which rendered evaluation of the influence on catalepsy impossible [4].
 

Psychiatry related information on Cgp 39551

 

High impact information on Cgp 39551

  • The NMDA antagonist CGP 39551 failed to affect reinstatement [7].
  • At the P11 stage, in particular, the fragmented DNA extracted from the cerebellum of CGP 39551-treated pups showed a clear laddering of nucleosomal fragments after agarose-gel electrophoresis [8].
  • The increase in seizure sensitivity of repeatedly withdrawn mice was prevented by treatment with the NMDA receptor antagonist CGP 39551 (20 mg/kg, i.p.) given once daily during the 3-day breaks in diazepam treatment, suggesting a role of glutamatergic transmission in the sensitisation process [9].
  • Also reliable (dose-dependent), although weaker, anxiolytic activity was produced by the uncompetitive NMDA receptor antagonist (+)MK-801 and the competitive antagonist CGP 39551 [10].
  • Assays for different neurochemical parameters, carried out at 80-90 days of age, suggested some alteration of the balance between excitatory and inhibitory circuits in the basal ganglia of CGP 39551-treated rats [5].
 

Chemical compound and disease context of Cgp 39551

 

Biological context of Cgp 39551

  • CGP 39551 showed weaker activity at NMDA receptor recognition sites and both compounds were weak or inactive at 18 other receptor binding sites [14].
  • The decrease in PS and EPSP amplitude produced by CGP 39551 was observed mainly in non-potentiated synaptic populations; potentiated field potentials were only minimally affected by drug treatment [15].
  • Current evoked by NMDA was concentration-dependently blocked by CGP 39551 with an IC50 of 2100 +/- 220 nM [16].
 

Anatomical context of Cgp 39551

  • 3. CGP 37849 and CGP 39551 were inactive as inhibitors of L-[3H]-glutamate uptake into rat brain synaptosomes and had no effect on the release of endogenous glutamate from rat hippocampal slices evoked by electrical field stimulation [14].
  • Histological evaluation of cellular degeneration revealed that the number of somatostatin-immunoreactive (SOM-IR) neurons in both stimulated groups was reduced almost equally, but in the CGP 39551 treated animals pyramidal cell damage was partly protected [17].
  • Adaptive changes in the NMDA receptor complex in rat hippocampus after chronic treatment with CGP 39551 [18].
  • The anticonvulsant and behavioural actions of CGP 37849 and CGP 39551, two novel competitive NMDA receptor antagonists, were examined in fully amygdala kindled rats following systemic administration [19].
  • Effects of the novel NMDA receptor antagonist, CGP 39551, on field potentials and the induction and expression of LTP in the dentate gyrus in vivo [15].
 

Associations of Cgp 39551 with other chemical compounds

 

Gene context of Cgp 39551

  • Five different competitive NMDA receptor antagonists [(1) DL-AP5; (2) DL-AP7; (3) CGP-37847; (4) CGP 39551; (5) (RS)-CPP] have been docked into both NR2A and NR2B subunits [24].
  • CGP 37849 and CGP 39551: novel and potent competitive N-methyl-D-aspartate receptor antagonists with oral activity [14].
  • Anticonvulsant and behavioral effects of two novel competitive N-methyl-D-aspartic acid receptor antagonists, CGP 37849 and CGP 39551, in the kindling model of epilepsy. Comparison with MK-801 and carbamazepine [25].
  • We report here experiments in which the competitive NMDA receptor antagonist CGP 39551 was administered to rat pups from postnatal day 7 (P7) to P18 [26].
  • Other neurochemical markers (glutamatergic, gabaergic, purinergic) and glutamine synthetase were unchanged, while a cholinergic marker was slightly increased in the cerebellum of CGP 39551 treated animals [26].
 

Analytical, diagnostic and therapeutic context of Cgp 39551

  • After oral administration of the drugs, the therapeutic index (TI = ratio of the ED50 values for rotorod performance and anticonvulsant protection) remains relatively constant at 5.9-7.2 for 3 h (CGP 37849) and 4.0-6.1 for 24 h (CGP 39551) [1].
  • Among EEG changes, the pressure induced reduction in delta wave amplitude was prevented by CGP 39551, but the increase in the amplitude of the 7-9 Hz band was not [2].

References

  1. Anticonvulsant activity of two orally active competitive N-methyl-D-aspartate antagonists, CGP 37849 and CGP 39551, against sound-induced seizures in DBA/2 mice and photically induced myoclonus in Papio papio. Chapman, A.G., Graham, J.L., Patel, S., Meldrum, B.S. Epilepsia (1991) [Pubmed]
  2. The orally active NMDA receptor antagonist CGP 39551 ameliorates the high pressure neurological syndrome in Papio anubis. Pearce, P.C., Halsey, M.J., Maclean, C.J., Ward, E.M., Pearson, J., Henley, M., Meldrum, B.S. Brain Res. (1993) [Pubmed]
  3. The effects of NMDA receptor antagonists at anticonvulsive doses on the performance of rats in the water maze task. Ylinen, A., Pitkänen, M., Sirviö, J., Hartikainen, T., Sivenius, J., Koivisto, E., Riekkinen, P.J. Eur. J. Pharmacol. (1995) [Pubmed]
  4. Central effects of CGP 37849 and CGP 39551, competitive NMDA receptor antagonists, in mice. Maj, J., Rogóz, Z., Skuza, G. Polish journal of pharmacology. (1993) [Pubmed]
  5. Long-lasting effects of chronic neonatal blockade of N-methyl-D-aspartate receptor through the competitive antagonist CGP 39551 in rats. Facchinetti, F., Dall'Olio, R., Ciani, E., Sparapani, M., Virgili, M., Contestabile, A. Neuroscience (1994) [Pubmed]
  6. Chronic neonatal blockade of N-methyl-D-aspartate receptor by CGP 39551 increases dopaminergic function in adult rat. Dall'Olio, R., Facchinetti, F., Contestabile, A., Gandolfi, O. Neuroscience (1994) [Pubmed]
  7. Ionotropic and metabotropic glutamate receptor antagonism attenuates cue-induced cocaine seeking. Bäckström, P., Hyytiä, P. Neuropsychopharmacology (2006) [Pubmed]
  8. Blockade of the NMDA receptor increases developmental apoptotic elimination of granule neurons and activates caspases in the rat cerebellum. Monti, B., Contestabile, A. Eur. J. Neurosci. (2000) [Pubmed]
  9. Sensitisation to repeated withdrawal, in mice treated chronically with diazepam, is blocked by an NMDA receptor antagonist. Dunworth, S.J., Stephens, D.N. Psychopharmacology (Berl.) (1998) [Pubmed]
  10. Anxiolytic activity of glycine-B antagonists and partial agonists--no relation to intrinsic activity in the patch clamp. Karcz-Kubicha, M., Jessa, M., Nazar, M., Plaznik, A., Hartmann, S., Parsons, C.G., Danysz, W. Neuropharmacology (1997) [Pubmed]
  11. NMDA receptor antagonists inhibit ethanol-produced locomotor stimulation in NMRI mice. Liljequist, S. Alcohol (1991) [Pubmed]
  12. Excitatory amino acid antagonists and pentylenetetrazol-induced seizures during ontogenesis. IV. Effects of CGP 39551. Velísek, L., Vachová, D., Mares, P. Pharmacol. Biochem. Behav. (1997) [Pubmed]
  13. Some central effects of CGP 37849 and CGP 39551, the competitive NMDA receptor antagonists: potential antiparkinsonian activity. Maj, J., Skuza, G., Rogóz, Z. Journal of neural transmission. Parkinson's disease and dementia section. (1993) [Pubmed]
  14. CGP 37849 and CGP 39551: novel and potent competitive N-methyl-D-aspartate receptor antagonists with oral activity. Fagg, G.E., Olpe, H.R., Pozza, M.F., Baud, J., Steinmann, M., Schmutz, M., Portet, C., Baumann, P., Thedinga, K., Bittiger, H. Br. J. Pharmacol. (1990) [Pubmed]
  15. Effects of the novel NMDA receptor antagonist, CGP 39551, on field potentials and the induction and expression of LTP in the dentate gyrus in vivo. Maren, S., Baudry, M., Thompson, R.F. Synapse (1992) [Pubmed]
  16. Effects of competitive NMDA receptor antagonists on excitatory amino acid-evoked currents in mouse spinal cord neurones. D'Hooge, R., Raes, A., Van de Vijver, G., Van Bogaert, P.P., De Deyn, P.P. Fundamental & clinical pharmacology. (1999) [Pubmed]
  17. Preservation of hippocampal NMDA receptors may be crucial for spatial learning after epileptic seizures in rats. Lahtinen, H., Ylinen, A., Hyvönen, M., Sirviö, J., Miettinen, R., Riekkinen, P.J. Brain Res. (1993) [Pubmed]
  18. Adaptive changes in the NMDA receptor complex in rat hippocampus after chronic treatment with CGP 39551. Mennini, T., Miari, A., Presti, M.L., Rizzi, M., Samanin, R., Vezzani, A. Eur. J. Pharmacol. (1994) [Pubmed]
  19. Weak anticonvulsant activity of CGP 37849 and CGP 39551 against kindled seizures following systemic administration. Cotterell, K.L., Croucher, M.J., Bradford, H.F. Eur. J. Pharmacol. (1992) [Pubmed]
  20. Effects of post-ethanol administration of NMDA and non-NMDA receptor antagonists on the development of ethanol tolerance in C57B1 mice. Karcz-Kubicha, M., Liljequist, S. Psychopharmacology (Berl.) (1995) [Pubmed]
  21. Protection from kainic acid neuropathological syndrome by NMDA receptor antagonists: effect of MK-801 and CGP 39551 on neurotransmitter and glial markers. Virgili, M., Migani, P., Contestabile, A., Barnabei, O. Neuropharmacology (1992) [Pubmed]
  22. Comparison of competitive and uncompetitive NMDA receptor antagonists with regard to monoaminergic neuronal activity and behavioural effects in rats. Löscher, W., Annies, R., Hönack, D. Eur. J. Pharmacol. (1993) [Pubmed]
  23. Differential behavioural and neurochemical effects of competitive and non-competitive NMDA receptor antagonists in rats. Bubser, M., Keseberg, U., Notz, P.K., Schmidt, W.J. Eur. J. Pharmacol. (1992) [Pubmed]
  24. Comparative analysis of different competitive antagonists interaction with NR2A and NR2B subunits of N-methyl-D-aspartate (NMDA) ionotropic glutamate receptor. Blaise, M.C., Sowdhamini, R., Pradhan, N. Journal of molecular modeling (Online) (2005) [Pubmed]
  25. Anticonvulsant and behavioral effects of two novel competitive N-methyl-D-aspartic acid receptor antagonists, CGP 37849 and CGP 39551, in the kindling model of epilepsy. Comparison with MK-801 and carbamazepine. Löscher, W., Hönack, D. J. Pharmacol. Exp. Ther. (1991) [Pubmed]
  26. Neuronal nitric oxide synthase is permanently decreased in the cerebellum of rats subjected to chronic neonatal blockade of N-methyl-D-aspartate receptors. Virgili, M., Facchinetti, F., Sparapani, M., Tregnago, M., Lucchi, R., Dall'Olio, R., Gandolfi, O., Contestabile, A. Neurosci. Lett. (1998) [Pubmed]
 
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