Human liver morphine UDP-glucuronyl transferase enantioselectivity and inhibition by opioid congeners and oxazepam
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منابع مشابه
Androgen UDP-glucuronyl transferase activity is found primarily in the liver in the human.
In this study, androgen UDP-glucuronyl transferase (UDPGT) activity was determined in microsomes of human liver, skin, and prostate. Androgen UDPGT activity was highest in the liver microsomes using 5 alpha-androstane-3 alpha, 17 beta-diol (3 alpha DIOL), androsterone (AN) and dihydrotestosterone (DHT) as substrates. The Km and Vmax values and enzyme velocity at the physiological concentration ...
متن کاملStudies on human liver bilirubin-UDP-glycosyl transferase. I. Assay methods for bilirubin-UDP-glucuronyl and -xylosyl transferases of human liver specimen.
Micromethods for estimation of bilirubin uridine diphosphate-glucuronyl and -xylosyl transferases in liver are described. With these methods, a liver specimen as small as 10 mg is sufficient for assay of either enzyme activity and 15 mg is sufficient for assay of both enzymes. Normal values for livers with minimal elevation of SGOT and minimal histological change were 0.260-0.400 U/g protein fo...
متن کاملUDP-glucuronyl transferase enzyme family in both human and Balb/c mouse lung.
endogenous and xenobiotic compounds. The UDPglucuronyl transferase (UGT) enzyme family catalysing glucuronidation is located in endoplasmic reticulum and expressed predominantly in the liver. This enzyme family has been identified in extrahepatic tissue, including lung tissue, for some time [l]. UGT enzyme activity has also been described in human fetal liver tissue to both planar phenol compou...
متن کاملAndrogen UDP-glucuronyl transferase activity is found primarily in liver in the rat.
UDP-glucuronyl transferase (UDPGT) activity was determined for androgens in tissue minces and microsomal fractions from the liver and extrahepatic tissues (kidney, skin, prostate, and preputial glands) of the male rat. Liver microsomes showed the highest UDPGT activity with each of the androgens tested (Vmax = 7, 3, and 10 nmol/minute/mg protein for testosterone, androsterone, and androstanedio...
متن کاملStereoselective conjugation of oxazepam by human UDP-glucuronosyltransferases (UGTs): S-oxazepam is glucuronidated by UGT2B15, while R-oxazepam is glucuronidated by UGT2B7 and UGT1A9.
(R,S)-Oxazepam is a 1,4-benzodiazepine anxiolytic drug that is metabolized primarily by hepatic glucuronidation. In previous studies, S-oxazepam (but not R-oxazepam) was shown to be polymorphically glucuronidated in humans. The aim of the present study was to identify UDP-glucuronosyltransferase (UGT) isoforms mediating R- and S-oxazepam glucuronidation in human liver, with the long term object...
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ژورنال
عنوان ژورنال: British Journal of Pharmacology
سال: 1988
ISSN: 0007-1188
DOI: 10.1111/j.1476-5381.1988.tb11598.x