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分类

• Pharmaceuticals
• {SNA} Approved Therapeutics/Drug Candidates, Bioactive Small Molecule Alphabetical Index, Catechol-O-methyltransferase, Enzyme Inhibitors, Neuroscience, Neurotransmission, Neurotransmitter Metabolism, Roche, T, 生物活性小分子, 细胞信号转导和神经科学, 细胞生物学
• Aromatics
• Intermediates & Fine Chemicals,
• {SA} Approved Therapeutics/Drug Candidates, Bioactive Small Molecules, Catechol-O-methyltransferase, Cell Biology, Cell Signaling and Neuroscience, Enzyme Inhibitors, Neuroscience, Neurotransmission, Neurotransmitter Metabolism, Roche, T

产品应用

• Orally active inhibitor of central and peripheral catechol-O-methyltransferase (COMT). Antiparkinsonian.

相关文献及参考

• [2]. Saviana Di Giovanni, Simona Eleuteri, Katerina E. Paleologou, et al. Entacapone and Tolcapone, Two Catechol O-Methyltransferase Inhibitors, Block Fibril Formation of α-Synuclein and β-Amyloid and Protect against Amyloid-induced Toxicity. The Journal of Biological Chemistry, 2010, 285, 14941-14954.
• [3]. Panos Bitsios, Panos Roussos1. Tolcapone, COMT polymorphisms and pharmacogenomic treatment of schizophrenia. Pharmacogenomics. 2001,12 (4): 559-566.
• [4]. M.A. Vieira-Coelho, P. Soares-da-Silva. Ontogenic aspects of liver and kidney catechol-O- methyltransferase sensitivity to tolcapone. British Journal of Pharmacology.1996,117 (3):516-520.
• [5]. J. Dingemanse, K. Jorga, G. Zurcher,et al. Pharmacokinetic-pharmacodynamic interaction between the COMT inhibitor tolcapone and single-dose levodopa. British Journal of Clinical Pharmacology
• 1995, 40 (3):253-262.
• Cao YG, Zhang L, Ma C, Chang BB, Chen YC, Tang YQ, Liu XD, Liu XQ., Metabolism

安全信息

GHS Symbol

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 1600 mg/kg
TOXIC EFFECTS :
   Behavioral - somnolence (general depressed activity)
   Behavioral - ataxia
   Lungs, Thorax, or Respiration - respiratory depression
REFERENCE :
   YACHDS Yakuri to Chiryo.  Pharmacology and Therapeutics.  (Raifu Saiensu
   Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan)  V.1-    1972-
   Volume(issue)/page/year: 24(Suppl 10),S1513,199

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : >2 gm/kg
TOXIC EFFECTS :
   Behavioral - somnolence (general depressed activity)
   Behavioral - ataxia
   Lungs, Thorax, or Respiration - respiratory depression
REFERENCE :
   YACHDS Yakuri to Chiryo.  Pharmacology and Therapeutics.  (Raifu Saiensu
   Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan)  V.1-    1972-
   Volume(issue)/page/year: 24(Suppl 10),S1513,199

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 3 gm/kg
SEX/DURATION            : female 6-15 day(s) after conception
TOXIC EFFECTS :
   Reproductive - Maternal Effects - other effects
REFERENCE :
   YACHDS Yakuri to Chiryo.  Pharmacology and Therapeutics.  (Raifu Saiensu
   Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan)  V.1-    1972-
   Volume(issue)/page/year: 24(Suppl 10),S1631,199