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Chemical Compound Review

Lopac-D-131     3,5-dinitrobenzene-1,2-diol

Synonyms: Tocris-0483, CHEMBL168276, D131_SIGMA, OR-486, KBioGR_001074, ...
 
 
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Psychiatry related information on Lopac-D-131

 

High impact information on Lopac-D-131

  • Inhibitors of cytochromes P-450, alpha-naphthoflavone and izoniazide, decreased the cytotoxicity of several polyphenols, whereas 3,5-dinitrocatechol, an inhibitor of catechol-o-methyltransferase (COMT), increased it [2].
  • As for tolcapone, 3,5-dinitrocatechol was more potent against MB- than against S-COMT when a fixed amount of total protein was used, but showed the same potency when a fixed concentration of COMT was used [3].
  • Tyrosine hydroxylase was not inhibited until micromolar concentrations of these compounds were used: the IC50 values for OR-462 and OR-486 were 10 and 14 microM, respectively [4].
  • With L-[beta-11C]fluoroDOPA as a tracer, similar results were observed although the increase in the pancreas by OR-486 had a lower magnitude [5].
 

Biological context of Lopac-D-131

 

Associations of Lopac-D-131 with other chemical compounds

  • Oral OR-462 did not penetrate into the brain in doses up to 30 mg/kg while the same dose of OR-486 had some effect on striatal COMT activity [4].

References

  1. Role of adenosine in drug-induced catatonia in mice. Singh, A., Kulkarni, S.K. Indian J. Exp. Biol. (2002) [Pubmed]
  2. Quantitative structure-activity relationships in prooxidant cytotoxicity of polyphenols: role of potential of phenoxyl radical/phenol redox couple. Nemeikaite-Ceniene, A., Imbrasaite, A., Sergediene, E., Cenas, N. Arch. Biochem. Biophys. (2005) [Pubmed]
  3. Effects of tolcapone upon soluble and membrane-bound brain and liver catechol-O-methyltransferase. Vieira-Coelho, M.A., Soares-da-Silva, P. Brain Res. (1999) [Pubmed]
  4. Inhibition of catechol-O-methyltransferase activity by two novel disubstituted catechols in the rat. Nissinen, E., Lindén, I.B., Schultz, E., Kaakkola, S., Männistö, P.T., Pohto, P. Eur. J. Pharmacol. (1988) [Pubmed]
  5. Modulation of organ uptake of 11C-labelled L-DOPA. Bergström, M., Lu, L., Marquez, M., Fasth, K.J., Bjurling, P., Watanabe, Y., Eriksson, B., Långström, B. Nucl. Med. Biol. (1997) [Pubmed]
  6. Redox properties of novel antioxidant 5,8-Dihydroxycoumarin: implications for its prooxidant cytotoxicity. Nemeikaite-Ceniene, A., Maroziene, A., Pukalskas, A., Venskutonis, P.R., Cenas, N. Z. Naturforsch., C, J. Biosci. (2005) [Pubmed]
 
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