Formation of highly analgesic morphine-6-glucuronide following physiologic concentration of morphine in human brain.

Article Details

Citation

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
DrugEnzymeKindOrganismPharmacological ActionActions
MorphineUDP-glucuronosyltransferase 2B7ProteinHumans
No
Substrate
Details