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Chemical Compound Review

Tolcapone     (3,4-dihydroxy-5-nitro- phenyl)-(4...

Synonyms: Tasmar, AC1NFJIT, CHEMBL1324, SureCN33869, Tasmar (TN), ...
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Disease relevance of Tolcapone


Psychiatry related information on Tolcapone

  • Repeated administration of tolcapone, an inhibitor of catechol-O-methyltransferase, was able to partially restore the memory deficits caused by bilateral cholinotoxin (AF64A) lesions in the basal magnocellular nuclei of Meynert [6].
  • In this paper we extend the psychometric assessment of PIMS to a new set of patients, in the context of a cross-over trial by Hoffman-La Roche Ltd, comparing two doses of tolcapone in 116 PD patients who had developed wearing off effect on levodopa [7].

High impact information on Tolcapone


Chemical compound and disease context of Tolcapone


Biological context of Tolcapone


Anatomical context of Tolcapone


Associations of Tolcapone with other chemical compounds


Gene context of Tolcapone


Analytical, diagnostic and therapeutic context of Tolcapone


  1. Tolcapone and neurotoxicity in Parkinson's disease. Kuhn, W., Woitalla, D., Gerlach, M., Russ, H., Müller, T. Lancet (1998) [Pubmed]
  2. Tolcapone improves motor function in parkinsonian patients with the "wearing-off" phenomenon: a double-blind, placebo-controlled, multicenter trial. Rajput, A.H., Martin, W., Saint-Hilaire, M.H., Dorflinger, E., Pedder, S. Neurology (1998) [Pubmed]
  3. Practical issues with COMT inhibitors in Parkinson's disease. Waters, C. Neurology (2000) [Pubmed]
  4. COMT inhibitors and liver toxicity. Watkins, P. Neurology (2000) [Pubmed]
  5. Tolcapone in stable Parkinson's disease: efficacy and safety of long-term treatment. Tolcapone Stable Study Group. Waters, C.H., Kurth, M., Bailey, P., Shulman, L.M., LeWitt, P., Dorflinger, E., Deptula, D., Pedder, S. Neurology (1998) [Pubmed]
  6. Tolcapone, an inhibitor of catechol O-methyltransferase, counteracts memory deficits caused by bilateral cholinotoxin lesions of the basal nuclei of Meynert. Khromova, I., Rauhala, P., Zolotov, N., Männistö, P.T. Neuroreport (1995) [Pubmed]
  7. The psychometric properties of the Parkinson's Impact Scale (PIMS) as a measure of quality of life in Parkinson's disease. Schulzer, M., Mak, E., Calne, S.M. Parkinsonism Relat. Disord. (2003) [Pubmed]
  8. Human catechol-O-methyltransferase: cloning and expression of the membrane-associated form. Bertocci, B., Miggiano, V., Da Prada, M., Dembic, Z., Lahm, H.W., Malherbe, P. Proc. Natl. Acad. Sci. U.S.A. (1991) [Pubmed]
  9. Population pharmacokinetics of levodopa in patients with Parkinson's disease treated with tolcapone. Jorga, K., Banken, L., Fotteler, B., Snell, P., Steimer, J.L. Clin. Pharmacol. Ther. (2000) [Pubmed]
  10. Influence of COMT inhibition on levodopa pharmacology and therapy. Goetz, C.G. Neurology (1998) [Pubmed]
  11. Effect of liver impairment on the pharmacokinetics of tolcapone and its metabolites. Jorga, K.M., Kroodsma, J.M., Fotteler, B., Heizmann, P., Meyer, J., Rasch, M.C., van Hattum, J. Clin. Pharmacol. Ther. (1998) [Pubmed]
  12. Tolcapone improves motor function and reduces levodopa requirement in patients with Parkinson's disease experiencing motor fluctuations: a multicenter, double-blind, randomized, placebo-controlled trial. Tolcapone Fluctuator Study Group I. Kurth, M.C., Adler, C.H., Hilaire, M.S., Singer, C., Waters, C., LeWitt, P., Chernik, D.A., Dorflinger, E.E., Yoo, K. Neurology (1997) [Pubmed]
  13. Differences in toxicity of the catechol-O-methyl transferase inhibitors, tolcapone and entacapone to cultured human neuroblastoma cells. Korlipara, L.V., Cooper, J.M., Schapira, A.H. Neuropharmacology (2004) [Pubmed]
  14. Effect of tolcapone on plasma and striatal apomorphine disposition in rats. Coudoré, F., Durif, F., Duroux, E., Eschalier, A., Fialip, J. Neuroreport (1997) [Pubmed]
  15. A pilot evaluation of the tolerability, safety, and efficacy of tolcapone alone and in combination with oral selegiline in untreated Parkinson's disease patients. Tolcapone De Novo Study Group. Hauser, R.A., Molho, E., Shale, H., Pedder, S., Dorflinger, E.E. Mov. Disord. (1998) [Pubmed]
  16. The effect of tolcapone on the pharmacokinetics of benserazide. Jorga, K.M., Larsen, J.P., Beiske, A., Schleimer, M., Fotteler, B., Schmitt, M., Moe, B. Eur. J. Neurol. (1999) [Pubmed]
  17. Integrated pharmacokinetics and pharmacodynamics of the novel catechol-O-methyltransferase inhibitor tolcapone during first administration to humans. Dingemanse, J., Jorga, K.M., Schmitt, M., Gieschke, R., Fotteler, B., Zürcher, G., Da Prada, M., van Brummelen, P. Clin. Pharmacol. Ther. (1995) [Pubmed]
  18. The effect of tolcapone on levodopa pharmacokinetics is independent of levodopa/carbidopa formulation. Jorga, K., Fotteler, B., Sedek, G., Nielsen, T., Aitken, J. J. Neurol. (1998) [Pubmed]
  19. Effects of entacapone and tolcapone on mitochondrial membrane potential. Haasio, K., Koponen, A., Penttilä, K.E., Nissinen, E. Eur. J. Pharmacol. (2002) [Pubmed]
  20. Catechol-O-methyltransferase inhibition increases striatal L-dopa and dopamine: an in vivo study in rats. Brannan, T., Martínez-Tica, J., Yahr, M.D. Neurology (1992) [Pubmed]
  21. Cerebrospinal fluid 3,4-dihydroxyphenylacetic acid level after tolcapone administration as an indicator of nigrostriatal degeneration. Thiffault, C., Langston, J.W., Di Monte, D.A. Exp. Neurol. (2003) [Pubmed]
  22. Optimizing levodopa pharmacokinetics with multiple tolcapone doses in the elderly. Jorga, K.M., Sedek, G., Fotteler, B., Zürcher, G., Nielsen, T., Aitken, J.W. Clin. Pharmacol. Ther. (1997) [Pubmed]
  23. D1-like dopamine receptor activation and natriuresis by nitrocatechol COMT inhibitors. Vieira-Coelho, M.A., Gomes, P., Serrão, M.P., Soares-da-Silva, P. Kidney Int. (2001) [Pubmed]
  24. Release and elimination of dopamine in vivo in mice lacking the dopamine transporter: functional consequences. Benoit-Marand, M., Jaber, M., Gonon, F. Eur. J. Neurosci. (2000) [Pubmed]
  25. Inhibitors of catecholamine metabolizing enzymes cause changes in S-adenosylmethionine and S-adenosylhomocysteine in the rat brain. Yassin, M.S., Cheng, H., Ekblom, J., Oreland, L. Neurochem. Int. (1998) [Pubmed]
  26. Haplotype relative risk study of catechol-O-methyltransferase (COMT) and attention deficit hyperactivity disorder (ADHD): association of the high-enzyme activity Val allele with ADHD impulsive-hyperactive phenotype. Eisenberg, J., Mei-Tal, G., Steinberg, A., Tartakovsky, E., Zohar, A., Gritsenko, I., Nemanov, L., Ebstein, R.P. Am. J. Med. Genet. (1999) [Pubmed]
  27. The specificity of glucuronidation of entacapone and tolcapone by recombinant human UDP-glucuronosyltransferases. Lautala, P., Ethell, B.T., Taskinen, J., Burchell, B. Drug Metab. Dispos. (2000) [Pubmed]
  28. 18F-dopa PET evidence that tolcapone acts as a central COMT inhibitor in Parkinson's disease. Ceravolo, R., Piccini, P., Bailey, D.L., Jorga, K.M., Bryson, H., Brooks, D.J. Synapse (2002) [Pubmed]
  29. Effects of tolcapone, a catechol-O-methyltransferase inhibitor, and Sinemet on intestinal electrolyte and fluid transport in conscious dogs. Larsen, K.R., Dajani, E.Z., Dajani, N.E., Dayton, M.T., Moore, J.G. Dig. Dis. Sci. (1998) [Pubmed]
  30. Catechol-O-methyltransferase inhibition with tolcapone reduces the "wearing off" phenomenon and levodopa requirements in fluctuating parkinsonian patients. Baas, H., Beiske, A.G., Ghika, J., Jackson, M., Oertel, W.H., Poewe, W., Ransmayr, G. Neurology (1998) [Pubmed]
  31. Effects of tolcapone, a novel catechol-O-methyltransferase inhibitor, on striatal metabolism of L-dopa and dopamine in rats. Napolitano, A., Zürcher, G., Da Prada, M. Eur. J. Pharmacol. (1995) [Pubmed]
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