134308-13-7 Tolcapone AKSci G884
 
 
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  G884    AKSci Reference Standard
Tolcapone, 97% (HPLC)
 
3,4-Dihydroxy-4'-methyl-5-nitrobenzophenone
IDENTITY
CAS Number:134308-13-7
MDL Number:MFCD00866569
MF:C14H11NO5
MW:273.24
SPECIFICATIONS & PROPERTIES
Min. Purity Spec:97% (HPLC)
Physical Form (at 20°C):Solid
Melting Point:140-148°C
Long-Term Storage:Store long-term at 2-8°C
DOT/IATA TRANSPORT INFORMATION
Not hazardous material

BIOLOGICAL INFO
Solubility:DMSO: =15 mg/mL

REVIEW
 The precise mechanism of action of tolcapone is unknown, but it is believed to be related to its ability to inhibit COMT and alter the plasma pharmacokinetics of levodopa, resulting in an increase in plasma levodopa concentrations. The inhibition of COMT also causes a reduction in circulating 3-OMD as a result of decreased peripheral metabolism of levodopa. This may lead to an increase distribution of levodopa into the CNS through the reduction of its competitive substrate, 3-OMD, for transport mechanisms. Sustained levodopa concentrations presumably result in more consistent dopaminergic stimulation, resulting in greater reduction in the manifestations of parkinsonian syndrome.

REFERENCES
[1]Guay DR: Tolcapone, a selective catechol-O-methyltransferase inhibitor for treatment of Parkinson's disease. Pharmacotherapy. 1999 Jan;19(1):6-20.
[2] Keating GM, Lyseng-Williamson KA: Tolcapone: a review of its use in the management of Parkinson's disease. CNS Drugs. 2005;19(2):165-84.
[3] Truong DD: Tolcapone: review of its pharmacology and use as adjunctive therapy in patients with Parkinson's disease. Clin Interv Aging. 2009;4:109-13. Epub 2009 May 14.
[4] Forsberg M, Lehtonen M, Heikkinen M, Savolainen J, Jarvinen T, Mannisto PT: Pharmacokinetics and pharmacodynamics of entacapone and tolcapone after acute and repeated administration: a comparative study in the rat. J Pharmacol Exp Ther. 2003 Feb;304(2):498-506.

GLOBALLY HARMONIZED SYSTEM (GHS)

Pictograms

Signal Word
Warning

Hazard Statements
H410

Precautionary Statements
P273; P391; P501

Current as of July 4, 2025

AKSci Reference Standards are high-purity, low-impurity compounds suitable for use as standards.


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CATEGORIES
 APIs and Bioactives > COMT Inhibitors


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