Entacapone
Entacapone is an inhibitor of catechol-O-methyltransferase (COMT), an enzyme responsible for metabolism of dopamine. Entacapone is commonly used to treat Parkinson’s disease and is given with L-DOPA as it reduces clearance of L-DOPA and improves motor function. Entacapone also displays other neuroprotective benefit, particularly in models of Alzheimer’s disease; it prevents α-synuclein and amyloid-β (Aβ) oligomerization and fibril formation. This compound decreases striatal homovanillic acid levels.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18914082
| Cas No. |
116314-67-1 |
|---|---|
| Purity |
≥98% |
| Formula |
C14H15N3O5 |
| Formula Wt. |
305.29 |
| Chemical Name |
(E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethylprop-2-enamide |
| IUPAC Name |
(E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethylprop-2-enamide |
| Appearance |
Light yellow or yellow crystalline powder |
Di Giovanni S, Eleuteri S, Paleologou KE, et al. 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. 2010 May 14;285(20):14941-54. PMID: 20150427.
Hamaue N, Ogata A, Terado M, et al. Entacapone, a catechol-O-methyltransferase inhibitor, improves the motor activity and dopamine content of basal ganglia in a rat model of Parkinsons disease induced by Japanese encephalitis virus. Brain Res. 2010 Jan 14;1309:110-5. PMID: 19879254.
Deleu D, Northway MG, Hanssens Y. Clinical pharmacokinetic and pharmacodynamic properties of drugs used in the treatment of Parkinsons disease. Clin Pharmacokinet. 2002;41(4):261-309. PMID: 11978145.
Törnwall M, Tuomainen P, Männistö PT. Modulation of rat brain endogenous dopamine metabolism by new inhibitors of catechol O-methyltransferase. Eur J Pharmacol. 1993 Aug 3;239(1-3):39-45. PMID: 8223912.
