货号 | 14153-10mg |
描述 | Catechol O-methyltransferase (COMT) is a key enzyme involved in the degradation of catecholamines including dopamine, epinephrine, and norepinephrine.1 COMT metabolizes L-3,4-dihydroxyphenylalanine (L-DOPA) to 3-O-methyldopa (3-OMD), and then further to vanillactic acid, which is excreted in urine. Entacapone is a peripherally acting, selective and reversible COMT inhibitor with IC50 values of 150-300 nM in rat liver (Ki = 145 nM) and 10-20 nM in rat brain tissues.1 It was designed as an adjuvant to L-DOPA/dopa decarboxylase inhibitor treatment for Parkinson’s disease.2 Peripheral COMT inhibition with entacapone can decrease 3-OMD levels in the rat brain by 16-52% and prolong the bioavailability of L-DOPA in patients with Parkinson’s disease.2,3,4 |
别名 | Comtan;OR 611; |
供应商 | Cayman |
应用文献 | |
1.Männistö, P.T. and Kaakkola, S. Catechol-O-methyltransferase (COMT): Biochemistry, molecular biology, pharmacology, and clinical efficacy of the new selective COMT inhibitors. Pharmacological Reviews 51(4), 593-628 (1999). 2.Männistö, P.T.,Tuomainen, P. and Tuominen, R.K. Different in vivo properties of three new inhibitors of catechol O-methyltransferase in the rat. British Journal of Pharmacology 105, 569-574 (1992). 3.Ruottinen, H.M. and Rinne, U.K. Entacapone prolongs levodopa response in a one month double blind study in parkinsonian patients with levodopa related fluctuations. J.Neurol.Neurosurg.Psychiatry 60, 36-40 (1996). 4.Heikkinen, H.,Varhe, A.,Laine, T., et al. Entacapone improves the availability of L-dopa in plasma by decreasing its peripheral metabolism independent of L-dopa/carbidopa dose. British Journal of Clinical Pharmacology 54(4), 363-371 (2002). | |
运输条件 | Wet ice in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 305.3 |
分子式 | C14H15N3O5 |
CAS号 | 130929-57-6 |
稳定性 | ≥ 2 years |
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