Short communicationFlavin-containing monooxygenase mediated metabolism of psychoactive drugs by human brain microsomes
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Cited by (43)
Unraveling the metabolic pathway of choline-TMA-TMAO: Effects of gypenosides and implications for the therapy of TMAO related diseases
2021, Pharmacological ResearchCitation Excerpt :Laboratory-extracted microsomal enzymes mainly include P450 enzymes and FMO3. It has been reported that the P450 enzyme is inactive under high pH, while the FMO3 enzyme is significantly increased in enzyme activity [27]. When we used different enzyme culture conditions, it was found that FMO3 enzymes were greatly inhibited under the conditions of FMO3 enzyme inhibitor methimazole, organic solvents, and high temperature, while the oxidation activity of FMO3 could be greatly increased at pH 9 (Fig. 1E-F).
A sensitive capillary LC-UV method for the simultaneous analysis of olanzapine, chlorpromazine and their FMO-mediated N-oxidation products in brain microdialysates
2017, TalantaCitation Excerpt :Expression of FMO in the human brain indicates a potential relevance for FMO in the central nervous system. It has been suggested that FMO can significantly be involved in the local metabolism and modulation of the pharmacological activity of psychoactive drugs [15]. Relatively little is known concerning substrate preferences for the different FMOs, although FMO-3 tends to prefer oxidation of smaller nucleophilic heteroatoms compared to FMO-1, which prefers drugs with bulkier side-chains [16].
Phase I biotransformation reactions-flavin monooxygenase
2007, xPharm: The Comprehensive Pharmacology ReferenceMammalian flavin-containing monooxygenases: Structure/function, genetic polymorphisms and role in drug metabolism
2005, Pharmacology and TherapeuticsCell-, tissue-, sex- and developmental stage-specific expression of mouse flavin-containing monooxygenases (Fmos)
2004, Biochemical PharmacologyCitation Excerpt :The abundance of FMO mRNAs in the kidney, in female, is FMO1>FMO5≥FMO4>FMO3>FMO2 and in male FMO1≈FMO5>FMO4>FMO2>FMO3. FMO activity has been detected in human [47,48] and rat [49,50] brain and FMO4 mRNA in rabbit brain [51]. It is also known that, in mouse and rat, the neurotoxin N-methyl-1,2,3,6-tetrahydropyridine (MPTP) undergoes N-oxidation by FMOs [52,53].