Regular ArticleIdentification of the Uridine Diphosphate Glucuronosyltransferase Isoform UGT1A6 in Rat Brain and in Primary Cultures of Neurons and Astrocytes☆
References (33)
- et al.
J. Pharm. Sci.
(1967) - et al.
Neuropharmacology
(1987) - et al.
Brain Res. Rev.
(1991) - et al.
Neurosci. Lett.
(1993) - et al.
J. Biol. Chem.
(1951) - et al.
Life Sci.
(1997) - et al.
J. Biol. Chem.
(1986) - et al.
Biochem. Biophys. Res. Commun.
(1984) - et al.
Pharmacol. Ther.
(1989) - et al.
Biochem. Pharmacol.
(1993)
Conjugation Reactions in Drug Metabolism
Annu. Rev. Pharmacol. Toxicol.
Pharmacogenetics
Glucuronidation of Drugs and Other Compounds
NIDA Res. Monogr.
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Molecular mechanisms involved in the protective actions of Selective Estrogen Receptor Modulators in brain cells
2019, Frontiers in NeuroendocrinologyCitation Excerpt :This metabolism is carried out by the hepatic UDP-glucuronosyltransferases (UGT) 1A and 1A9, and for this reason, patients treated with this compound have high levels of glucuronides and only 1% of raloxifene in plasma (D. Sun et al., 2013). These UGT are well expressed in astrocytes and endothelial cells, but neurons have lower expression (Gradinaru et al., 2012; Suleman et al., 1998). Raloxifene has shown beneficial effects against neurotoxicity and inflammation in neurodegenerative disorders, autoimmune diseases and stroke.
Endogenous morphine and its metabolites in mammals: History, synthesis, localization and perspectives
2013, NeuroscienceCitation Excerpt :These UGT isoforms form M3G, whereas only the UGT2B7 isoform appears to produce both M3G and M6G. In addition to their localization in the liver, the UGT1A6 and 2B7 isoforms are also expressed in neurons and astrocytes, suggesting that morphine can be glucuronidated in CNS cells (Suleman et al., 1998; King et al., 1999; Nagano et al., 2000; Yamada et al., 2003; Buckley and Klaassen, 2007). Concerning their activities, M6G is 1–600 times more analgesic than morphine, whereas M3G has long been considered devoid of any activity (reviewed in: (Lotsch and Geisslinger, 2001; Coller et al., 2009)).
In vitro morphine metabolism by rat microglia
2013, NeuropharmacologyEffect of oxidative stress on UDP-glucuronosyltransferases in rat astrocytes
2012, Toxicology LettersCitation Excerpt :Also, previous studies evidenced an increase in rat brain conjugation activities of 1-naphthol during aging (Gradinaru et al., 1999). At cellular level, the 1-naphthol UGT1A6 specific activity was 10-fold higher in astrocytes, as compared with neurons and endothelial cerebrovascular cells, suggesting an important role in the protection against neurotoxic actions of drugs or environmental pollutants (Suleman et al., 1998). Another isoform – UGT1A7, which is widely active toward benzo(a)pyrene metabolites, particularly the phenols, exhibits a similar pattern of constitutive expression with UGT1A6 (Grove et al., 1997; Webb et al., 2005).
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Mulder, G. J.
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