Entacapone is a potent catechol O-methyltransferase (COMT) inhibitor (IC50 = 14.3, 20.1 and 73.3 nM for rat liver soluble COMT, total COMT and membrane-bound COMT respectively) (1). It also promotes production of L-DOPA, which could make it a useful for treating Parkinson's disease (2). It also inhibits α-synuclein aggregation in vitro and inhibits α-synuclein-induced cell death in PC-12 cells (3). Entacapone also play a role in oxidative stress-induced cell death (4).
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
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