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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Chemical Compound Review: 

Tocris-1019     (3S,4aR,6S,8aS)-6- (phosphonomethyl)-1,2,3...

Synonyms: SureCN195083, AG-D-76078, BPBio1_001216, LS-85439, CTK0H8339, ...
 
 
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Disease relevance of LY-274614

  • Systemic (i.p.) treatment with dizocilpine maleate (3 mg/kg) or LY 274614 (5 mg/kg i.p.), two N-methyl-D-aspartate receptor antagonists (given 15 min beforehand), prevented dendrotoxin K (35 pmol)-induced motor seizures and electrocortical epileptogenic discharges in 100% of the animals (n = 6 per group) treated [1].
  • In contrast, administration of LY 235959 (1 mg/kg) 15 min after morphine (4 mg/kg) did not reverse the hyperthermia [2].
 

Psychiatry related information on LY-274614

 

High impact information on LY-274614

  • 4. The effects of MK-801 and LY 235959 on the binding of [3H]-DPDPE to mouse brain membranes were also determined [4].
  • This can only be explained by differences in the binding kinetics of AP7 and LY 235959, since at equilibrium, with these concentrations, either antagonist essentially eliminates the agonist response to 10 microM NMDA.(ABSTRACT TRUNCATED AT 400 WORDS)[5]
  • Administration of the NMDA receptor antagonists MK-801 or LY 274614 ameliorated the decline in striatal met-enkephalin levels observed in mice after 8 weeks of infection [6].
  • MK-801 (0.01-0.10 mg/kg, i.p.) or LY 235959 (1.0-4.0 mg/kg, i.p.) given 10 min before each injection of L-arginine (200 mg/kg, i.p.) reversed the action of the letter in a dose-dependent manner on morphine antinociception [7].
  • MK-801 and LY 235959 reverse delta1- and delta2-opioid receptor agonists-induced down-regulation of brain delta1-opioid receptor, respectively, apparently by different mechanisms [8].
 

Biological context of LY-274614

 

Associations of LY-274614 with other chemical compounds

  • An NMDA antagonist (LY 235959) attenuates abstinence-induced withdrawal of planarians following acute exposure to a cannabinoid agonist (WIN 52212-2) [10].
 

Gene context of LY-274614

  • The effects of MK-801, a noncompetitive antagonist of the N-methy1-D-aspartate (NMDA) receptor, and of LY 235959, a competitive antagonist of the NMDA receptor, on the development of tolerance to the analgesic action of [D-Pen2,D-Pen5]enkephalin (DPDPE), a delta 1-opioid receptor agonist were determined in mice [11].

References

  1. N-methyl-D-aspartate and non-N-methyl-D-aspartate receptors mediate seizures and CA1 hippocampal damage induced by dendrotoxin-K in rats. Bagetta, G., Iannone, M., Palma, E., Nisticò, G., Dolly, J.O. Neuroscience (1996) [Pubmed]
  2. NMDA receptors modulate morphine-induced hyperthermia. Rawls, S.M., Adler, M.W., Gaughan, J.P., Baron, A., Geller, E.B., Cowan, A. Brain Res. (2003) [Pubmed]
  3. Dizocilpine-like discriminative stimulus effects of competitive NMDA receptor antagonists in mice. Geter-Douglass, B., Witkin, J.M. Psychopharmacology (Berl.) (1997) [Pubmed]
  4. Effects of competitive and noncompetitive antagonists of the N-methyl-D-aspartate receptor on the analgesic action of delta 1- and delta 2-opioid receptor agonists in mice. Bharagava, H.N., Zhao, G.M. Br. J. Pharmacol. (1996) [Pubmed]
  5. Structure-activity analysis of binding kinetics for NMDA receptor competitive antagonists: the influence of conformational restriction. Benveniste, M., Mayer, M.L. Br. J. Pharmacol. (1991) [Pubmed]
  6. The pattern of neurotransmitter alterations in LP-BM5 infected mice is consistent with glutamatergic hyperactivation. Kustova, Y., Ha, J.H., Espey, M.G., Sei, Y., Morse, D., Basile, A.S. Brain Res. (1998) [Pubmed]
  7. Evidence for a role of N-methyl-D-aspartate receptors in L-arginine-induced attenuation of morphine antinociception. Bhargava, H.N., Sharma, S.S., Bian, J.T. Brain Res. (1998) [Pubmed]
  8. Effects of NMDA receptor antagonists on delta1- and delta2-opioid receptor agonists-induced changes in the mouse brain [3H]DPDPE binding. Cao, Y.J., Bian, J.T., Bhargava, H.N. Eur. J. Pharmacol. (1997) [Pubmed]
  9. Enhancement of morphine actions in morphine-naive and morphine-tolerant mice by LY 235959, a competitive antagonist of the NMDA receptor. Bhargava, H.N. Gen. Pharmacol. (1997) [Pubmed]
  10. An NMDA antagonist (LY 235959) attenuates abstinence-induced withdrawal of planarians following acute exposure to a cannabinoid agonist (WIN 52212-2). Rawls, S.M., Gomez, T., Raffa, R.B. Pharmacol. Biochem. Behav. (2007) [Pubmed]
  11. Effect of antagonism of the NMDA receptor on tolerance to [D-Pen2,D-Pen5]enkephalin, a delta 1-opioid receptor agonist. Zhao, G.M., Bhargava, H.N. Peptides (1996) [Pubmed]
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