著者

山田 英之 小栗 一太

出版者

公益社団法人 日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.34, no.9, pp.895-899, 1998-09-01 (Released:2018-08-26)

参考文献数

24

著者

小栗 一太 吉村 英敏

出版者

公益社団法人 日本薬学会

雑誌

衛生化学 (ISSN:0013273X)

巻号頁・発行日

vol.32, no.6, pp.413-426, 1986-12-31 (Released:2008-05-30)

参考文献数

105

被引用文献数

1 1

---

Recent progress of forensic toxicology of morphine and heroin, and of the boundary area was reviewed. Topics included in this review were 1) opioid peptides, 2) opioid receptors, 3) endogenous morphine, 4) metabolism of morphine : glucuronidation, sulfate conjugation, N-demethylation and dehydrogenation, 5) pharmacological activity of morphine conjugates, 6) metabolism of heroin, 7) analytical methods of morphine and heroin for forensic toxicological purpose.

著者

山田 英之 福島 直 小栗 一太

出版者

日本毒性学会

雑誌

Journal of toxicological sciences (ISSN:03881350)

巻号頁・発行日

vol.23, pp.App.161-App.170, 1998-11-26

参考文献数

39

著者

小栗 一太

出版者

The Japanese Society for the Study of Xenobiotics

雑誌

薬物動態 (ISSN:09161139)

巻号頁・発行日

vol.15, no.2, pp.136-142, 2000 (Released:2007-03-29)

参考文献数

17

---

Here, I briefly review studies on an active metabolite of morphine and characterization of enzymes responsible for the formation of the glucuronide in our laboratory. Morphine has been used extensively in pain clinic and was found biotransformed mainly by glucuronidation to a major inactive glucuronide; morphine-3-glucuronide (M-3-G) and also to a minor active metabolite; morphine-6-glucuronide (M-6-G). The very potent metabolite has been attracted much interest in a role of morphine analgesia in humans. The pharmacokinetic results are now interpreted as demonstrating that the active glucuronide had a positive effect on the analgesia. Recently, researchers have disclosed the presence of an unique opioid receptor for the glucuronide. Our recent experimental evidence from expression of two cDNA clones of glucuronidating enzymes from guinea pig liver supported the view that the enzymes form hetero-oligomers by accessing a broader range of compounds as in the active metabolite than homo-oligomers. A natural follow-up to the present evidence would be to carry out for the genomic information in regulatory molymorphism in drug metabolism by glucuronidation.