Formation of highly analgesic morphine-6-glucuronide following physiologic concentration of morphine in human brain.
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Yamada H, Ishii K, Ishii Y, Ieiri I, Nishio S, Morioka T, Oguri K
Formation of highly analgesic morphine-6-glucuronide following physiologic concentration of morphine in human brain.
J Toxicol Sci. 2003 Dec;28(5):395-401.
- PubMed ID
- 14746343 [ View in PubMed]
- Abstract
3H-Morphine at physiologic concentration was metabolized in vitro to its 3- and 6-glucuronides by human brain homogenate. Recombinant UGT2B7, one of the UDP-glucuronosyltransferase (UGT) isoforms, is able to glucuronidate the 3- and 6-hydroxy groups of morphine at nanomolar concentrations. These results suggest that endogenous morphine is converted to its 6-glucuronide, a more highly analgesic substance than the parent compound, to suppress effectively pain symptoms in humans.
DrugBank Data that Cites this Article
- Drug Enzymes
Drug Enzyme Kind Organism Pharmacological Action Actions Morphine UDP-glucuronosyltransferase 2B7 Protein Humans NoSubstrateDetails