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Research ArticleArticle

The Glucuronidation of Opioids, Other Xenobiotics, and Androgens by Human UGT2B7Y(268) and UGT2B7H(268)

Birgit L. Coffman, Christopher D. King, Gladys R. Rios and Thomas R. Tephly
Drug Metabolism and Disposition January 1998, 26 (1) 73-77;
Birgit L. Coffman
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Christopher D. King
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Gladys R. Rios
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Thomas R. Tephly
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Abstract

UGT2B7 has been cloned and expressed previously in COS cells and HK293 cells. Two forms have been identified: one with a tyrosine and one with a histidine at position 268. UGT2B7 has been shown to catalyze NSAIDs, catechol estrogens, and morphine-3- and -6-glucuronidation. cDNAs for UGT2B7Y268 and H268 were cloned and stably expressed in HK 293 cells. Studies were designed to test each form for reactivity toward a number of opioid compounds, xenobiotics such as menthol, oxazepam, and propranolol, and androgens such as androsterone and testosterone using membrane preparations derived from HK 293 cells. Both UGT2B7Y and UGT2B7H are highly reactive with many opioids, menthol, androsterone, and (R)- and (S)-propranolol, and similar kinetic values were observed. UGT2B7Y and UGT2B7H react poorly with oxazepam and no difference in (R)- or (S)-glucuronidation rate ratios was found. Thus, UGT2B7Y and H cannot account for the variability in the plasma or urine concentrations of these glucuronides in human populations. Our data suggest that UGT2B7 is a major isoform responsible for the glucuronidation of androsterone. Neither UGT2B7Y nor H catalyzes the glucuronidation of testosterone although each catalyzes the glucuronidation of epitestosterone. UGT2B7 seems to be a major human isoform responsible for the glucuronidation of opioids of the morphinan and oripavine class and is capable of catalyzing the glucuronidation of both the 3- and 6-hydroxyl moieties on these molecules. Thus, UGT2B7 plays a major role in the conversion of morphine to morphine-6-glucuronide, the potent analgesic metabolite of morphine.

Footnotes

  • Send reprint requests to: Dr. Thomas R. Tephly, 2–452 Bowen Science Building, Department of Pharmacology, University of Iowa, Iowa City, IA 52242. E-mail: Thomas-Tephly{at}uiowa.edu.

  • This research was supported by NIH grant GM26221.

  • Abbreviations used are::
    UGT
    UDP-glucuronosyltransferase
    UGT2B7Y
    UGT2B7(Y268)
    UGT2B7H
    UGT2B7(H268)
    UDP-GlcUA
    UDP-glucuronic acid
    NSAID
    non-steroid anti-inflammatory drug
    • Received July 31, 1997.
    • Accepted October 20, 1997.
  • The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition
Vol. 26, Issue 1
1 Jan 1998
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Research ArticleArticle

The Glucuronidation of Opioids, Other Xenobiotics, and Androgens by Human UGT2B7Y(268) and UGT2B7H(268)

Birgit L. Coffman, Christopher D. King, Gladys R. Rios and Thomas R. Tephly
Drug Metabolism and Disposition January 1, 1998, 26 (1) 73-77;

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Research ArticleArticle

The Glucuronidation of Opioids, Other Xenobiotics, and Androgens by Human UGT2B7Y(268) and UGT2B7H(268)

Birgit L. Coffman, Christopher D. King, Gladys R. Rios and Thomas R. Tephly
Drug Metabolism and Disposition January 1, 1998, 26 (1) 73-77;
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