Entacapone
Chemical Name: (2E)-2-Cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethyl-2-propenamide
Purity: ≥99%
Biological Activity
Entacapone is a potent catechol O-methyltransferase (COMT) inhibitor (IC50 values are 14.3, 20.1 and 73.3 nM for rat liver soluble COMT, total COMT and membrane-bound COMT respectively). Increases bioavailability of levodopa when given as an adjunct therapy for Parkinson's disease. Inhibits α-synuclein aggregation in an in vitro assay; blocks α-synuclein-induced cell death in PC-12 cells.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Entacapone and tolcapone, two catechol O-methyltransferase inhibitors, block fibril formation of alpha-synuclein and beta-amyloid and protect against amyloid-induced toxicity.
Di Giovanni et al.
J.Biol.Chem., 2010;285:14941 -
Pharmacokinetics and pharmacodynamics of entac. and tolc. after acute and repeated administration: a comparative study in the rat.
Forsberg et al.
J.Pharmacol.Exp.Ther., 2003;304:498 -
Effect of entacapone, a peripherally acting catechol-O-methyltransferase inhibitor, on the motor response to acute treatment with lev. in patients with Parkinson's disease.
Merello et al.
J.Neurol.Neurosurg.Psychiatry, 1994;57:186
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