Characteristic glucuronidation pattern of physiologic concentration of morphine in rat brain

Characteristic glucuronidation pattern of physiologic concentration of morphine in rat brain

Formation of conjugated metabolites from morphine at a very low level in brain was studied in vitro in rats. Incubation of a low concentration of 3H-morphine with brain homogenate followed by two successive high-performance liquid chromatographic analyses showed that endogenous morphine is converted...

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Bibliographic Details
Published in:Life sciences (1973) Vol. 67; no. 20; pp. 2453 - 2464
Main Authors: Nagano, Emiko, Yamada, Hideyuki, Oguri, Kazuta
Format: Journal Article
Language:English
Published: Netherlands Elsevier Inc 06-10-2000
Subjects:
Animals
Brain
Brain - enzymology
Brain Stem - metabolism
Cerebellum - metabolism
Chromatography, High Pressure Liquid
Codeine - analogs & derivatives
Codeine - metabolism
Codeine glucuronide
Endogenous morphine
Glucuronides - metabolism
Glucuronosyltransferase - metabolism
Liver - metabolism
Male
Microsomes, Liver - enzymology
Microsomes, Liver - metabolism
Morphine - metabolism
Morphine Derivatives - metabolism
Morphine-3-glucuronide
Morphine-6-glucuronide
Rat
Rats
Rats, Sprague-Dawley
Telencephalon - metabolism
UDP-Glucuronosyltransferase
Brain
Codeine glucuronide
Morphine-6-glucuronide
Rat
UDP-Glucuronosyltransferase
Endogenous morphine
Morphine-3-glucuronide
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Summary:Formation of conjugated metabolites from morphine at a very low level in brain was studied in vitro in rats. Incubation of a low concentration of 3H-morphine with brain homogenate followed by two successive high-performance liquid chromatographic analyses showed that endogenous morphine is converted by brain enzymes to its 3- and 6-glucuronides (M-3-G and M-6-G), and codeine glucuronide (Cod-G). However, the formation of morphine-6-sulfate was likely to be low if it was produced at all. All of the cerebral hemisphere, brain stem and cerebellum were capable of producing M-3-G, M-6-G and Cod-G, although there were differences in selectivity. The capacity of the brain for glucuronide formation was far less than that of the liver, but UDP-glucuronosyltransferase in brain was much more selective in forming M-6-G and Cod-G than liver enzymes.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
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ISSN:0024-3205
1879-0631
DOI:10.1016/S0024-3205(00)00825-0