General Pharmacology: The Vascular System
ReviewGeneral properties and clinical possibilities of new selective inhibitors of catechol O-methyltransferase
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2020, Drug Delivery Devices and Therapeutic SystemsPharmacodynamic evaluation of novel Catechol-O-methyltransferase inhibitors
2019, European Journal of PharmacologyCitation Excerpt :S-COMT has a higher enzymatic capacity than MB-COMT (Vmax up to nearly 15,000 pmol/min per mg protein in liver) (Guldberg and Marsden, 1975; Roth, 1992). S-COMT has therefore a more predominant role when substrate levels are high and is believed to be primarily involved in the O-methylation and elimination of biologically active, toxic and mainly exogenous catechols (such as food-derived catechol compounds in the gut), acting as an enzymatic detoxifying barrier between the blood and other tissues (Kaakkola et al., 1994; Mannisto and Kaakkola, 1999; Mannisto et al., 1992). On the other hand, MB-COMT has a low enzymatic capacity (Vmax of only 2–40 pmol/min per mg protein), a higher affinity for catechol substrates, and a lower Km value (Km = 10 μM) for dopamine than S-COMT (Km = 108 μM), and as such is thought to be predominant at low substrate levels (Malherbe et al., 1992).
Methyltransferases
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