Tolcapone may be used in COMT-mediated cell signaling studies. Tolcapone has been used in methyltransferase assay in human embryonic kidney 293 cells.
synthetische
preparation by demethylation of 4-hydroxy-3-methoxy-4′-methyl-5-nitrobenzophenone with hydrobromic acid in refluxing aque-ous acetic acid.
Allgemeine Beschreibung
Tolcapone, 3,4-dihydroxy-4'-methyl-5-nitrobenzophenone (Tasmar), is a yellow, odorless, nonhygroscopic,crystalline compound (pKa=4.78). Tolcapone israpidly absorbed after oral administration. Tolcapone ishighly bound to plasma albumin (>98%), and its distributionis therefore restricted. Tolcapone has low first-pass metabolism.It is almost completely metabolized in the liver before excretion, and 60% is excreted by the kidney. The majormetabolite of tolcapone is an inactive glucuronide conjugate.COMT inhibitors increase chronotropic and arrhythmogeniceffects of epinephrine.Tolcapone is indicated as an adjunctto levodopa/carbidopa for the management of signs andsymptoms of PD.
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Tolcapone
Tolcapone (1670207)
3,4-Dihydroxy-4'-methyl-5-nitrobenzophenone
134308-13-7
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134308-13-7
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