Biochemicals & reagents
1) Forsberg et al. (2003), Pharmacokinetics and pharmacodynamics of entacapone and tolcapone after acute and repeated administration: a comparative study in the rat; J. Pharmacol. Exp. Ther., 304 498 2) Merello et al. (1994), Effect of entacapone, a peripherally acting catechol-O-methyltransferase inhibitor, on the motor response to acute treatment with levodopa in patients with Parkinson’s disease; J. Neurol. Neurosurg. Psychiatry, 57 186 3) Giovanni et al. (2010), Entacapone and tolcapone, two catechol O-methyltransferase inhibitors, block fibril formation of alpha-synuclein and beta amyloid and protect against amyloid-induced toxicity; J. Biol. Chem., 285 14941 4) Chen et al. (2016), Entacapone is an Antioxident More Potent than Vitamin C and Vitamin E for Scavenging of Hypochlorous Acid and Peroxynitrite, and the Inhibition of Oxidative Stress-induced Cell Death; Med. Sci. Monit., 22 687
Entacapone is a potent catechol O-methyltransferase (COMT) inhibitor with IC50 = 14.3, 20.1 and 73.3 nM for rat liver soluble COMT, total COMT and membrane-bound COMT respectively (1). This compound increases the bioavailability of L-DOPA as adjunct therapy for Parkinson's disease (2), inhibits α-synuclein aggregation in vitro and inhibits α-synuclein-induced cell death in PC-12 cells (3), is an antioxidant and also inhibits oxidative stress-induced cell death (4).