Product Overview
Tolcapone is a novel, reversible and orally-bioavailable small-molecule catechol-O-methyltransferase (COMT) inhibitor used for as an adjunct to levodopa therapy for the treatment of Parkinson's disease (PD). The chemical structure of tolcapone contains a catechol structure with two electron withdrawing substituents of a tendency to easily deliver a proton resulting in an anion that is highly affinitive for COMT (the value of 50% inhibition concentration IC50 of 36 nM in rat liver) and displaces other catechols (such as catecholamines and levodopa) from the COMT catalytic center to prevent methylation. Study results have that the use of tolcapone reduces the dosage but enhances the therapeutic effects of levodopa to control PD symptoms. ReferenceTruong DD. Tolcapone: review of its pharmacology and use as adjunctive therapy in patients with Parkinsons disease.
Synonyms
Ro 40-7592, Ro-40-7592
Molecular Formula
C14H11NO5
Chemical Name
(3,4-dihydroxy-5-nitrophenyl)-(4-methylphenyl)methanone
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request