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Entacapone is a reversible catechol O-methyltransferase (COMT) inhibitor (IC50s = 10, 10, 20, and 160 nM for rat duodenum, brain, erythrocyte, and liver COMT, respectively). It is selective for COMT over monoamine oxidase A (MAO-A) and MAO-B and phenolsulphotransferase M (PST-M) and PST-P (IC50s = >50 µM). Entacapone (10 mg/kg), in combination with L-DOPA (Cay-13248) and carbidopa (Cay-23783), reduces 3-O-methyldopa (3-OMD) levels in the rat striatum and hypothalamus to 52 and 27%, respectively, of the levels in control animals receiving only L-DOPA and carbidopa. In a 6-OHDA rat model of Parkinson's disease, entacapone (10 mg/kg), in combination with L-DOPA and benserazide (Cay-20298), increases contralateral turning behavior and striatal extracellular dopamine levels. Entacapone also inhibits contraction of colon longitudinal muscle explants from a 6-OHDA rat model of Parkinson's disease (EC50 = 200 µM). Formulations containing entacapone have been used in the treatment of Parkinson's disease.Formal Name: 2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethyl-2E-propenamide. CAS Number: 130929-57-6. Synonyms: OR-611. Molecular Formula: C14H15N3O5. Formula Weight: 305.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml, Ethanol: 5 mg/ml. lambdamax: 224, 309 nm. SMILES: OC1=C(O)C([N+]([O-])=O)=CC(/C=C(C#N)/C(N(CC)CC)=O)=C1. InChi Code: InChI=1S/C14H15N3O5/c1-3-16(4-2)14(20)10(8-15)5-9-6-11(17(21)22)13(19)12(18)7-9/h5-7,18-19H,3-4H2,1-2H3/b10-5+. InChi Key: JRURYQJSLYLRLN-BJMVGYQFSA-N.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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