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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.
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 305.29. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.28 mL||16.38 mL||32.76 mL|
|5 mM||0.66 mL||3.28 mL||6.55 mL|
|10 mM||0.33 mL||1.64 mL||3.28 mL|
|50 mM||0.07 mL||0.33 mL||0.66 mL|
References are publications that support the biological activity of the product.
Di 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 PMID: 20150427
Forsberg et al (2003) Pharmacokinetics and pharmacodynamics of entac. and tolc. after acute and repeated administration: a comparative study in the rat. J.Pharmacol.Exp.Ther. 304 498 PMID: 12538800
Merello et al (1994) 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. J.Neurol.Neurosurg.Psychiatry 57 186 PMID: 8126502
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Literature in this Area
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Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.