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Merck
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重要文件

SML0150

Sigma-Aldrich

Tolcapone

≥98% (HPLC)

同義詞:

3,4-Dihydroxy-4′-methyl-5-nitrobenzophenone, Ro 40-7592

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About This Item

經驗公式(希爾表示法):
C14H11NO5
CAS號碼:
分子量::
273.24
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

品質等級

化驗

≥98% (HPLC)

形狀

powder

儲存條件

desiccated

顏色

yellow

溶解度

DMSO: ≥15 mg/mL

起源

Roche

儲存溫度

2-8°C

SMILES 字串

Cc1ccc(cc1)C(=O)c2cc(O)c(O)c(c2)[N+]([O-])=O

InChI

1S/C14H11NO5/c1-8-2-4-9(5-3-8)13(17)10-6-11(15(19)20)14(18)12(16)7-10/h2-7,16,18H,1H3

InChI 密鑰

MIQPIUSUKVNLNT-UHFFFAOYSA-N

基因資訊

human ... COMT(1312)

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應用

Tolcapone may be used in COMT-mediated cell signaling studies.
Tolcapone has been used in methyltransferase assay in human embryonic kidney 293 cells.

生化/生理作用

Inhibition of catechol-O-methyltransferase by tolcapone increases the half-life and bioavailabilty of levodopa. It therefore is an effective adjunctive therapy in patients with Parkinson′s disease with motor response fluctuations.
Orally active catechol-O-methyltransferase (COMT) inhibitor: inhibits both central and peripheral COMT.
Tolcapone is an orally active catechol-O-methyltransferase (COMT) inhibitor. It inhibits both central and peripheral COMT. Tolcapone crosses the blood-brain barrier, and has been used for L-DOPA adjunct therapy in the treatment of Parkinson′s Disease.

特點和優勢

This compound was developed by Roche. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

象形圖

Environment

訊號詞

Warning

危險聲明

防範說明

危險分類

Aquatic Acute 1

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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Sandro Zambito Marsala et al.
Clinical neuropharmacology, 35(4), 185-190 (2012-07-19)
Catechol-O-methyltransferase (COMT) inhibitors are drugs commonly used in the management of patients with Parkinson disease complicated by motor fluctuations. Among them, entacapone is the most commonly used. Tolcapone has been reintroduced in patients where entacapone has proved to be ineffective
Andrew J Lees
CNS neuroscience & therapeutics, 14(1), 83-93 (2008-05-17)
The relative efficacy has not been adequately established for the two catechol-O-methyltransferase (COMT) inhibitors that are currently available for adjunctive therapy in Parkinson's disease; tolcapone and entacapone. A recent Cochrane meta-analysis of 14 studies in 2566 patients, conducted to assess
H Baas et al.
Journal of neurology, neurosurgery, and psychiatry, 63(4), 421-428 (1997-10-29)
More than 50% of patients with Parkinson's disease develop motor response fluctuations (the "wearing off" phenomenon) after more than five years of levodopa therapy. Inhibition of catechol-O-methyltransferase by tolcapone has been shown to increase levodopa bioavailability and plasma elimination half
Gillian M Keating et al.
CNS drugs, 19(2), 165-184 (2005-02-09)
Tolcapone (Tasmar) is a selective, reversible inhibitor of peripheral and central catechol-O-methyltransferase (COMT). Results of well designed studies indicate that oral tolcapone is an effective adjunct to levodopa plus a peripheral dopa-decarboxylase inhibitor (DDCI) in patients with fluctuating Parkinson's disease.
Jenny J Fischer et al.
Toxicological sciences : an official journal of the Society of Toxicology, 113(1), 243-253 (2009-09-29)
Capture compound mass spectrometry (CCMS) is a novel technology that helps understand the molecular mechanism of the mode of action of small molecules. The Capture Compounds are trifunctional probes: A selectivity function (the drug) interacts with the proteins in a

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