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

Hideyuki Yamada; Kumiko Ishii; Yuji Ishii; Ichiro Ieiri; Syunji Nishio; Takato Morioka; Kazuta Oguri

doi:10.2131/jts.28.395

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

Hideyuki Yamada, Kumiko Ishii, Yuji Ishii, Ichiro Ieiri, Syunji Nishio, Takato Morioka, Kazuta Oguri

Pharmaceutical Health Care and Sciences

Research output: Contribution to journal › Article › peer-review

46 Citations (Scopus)

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.

Original language	English
Pages (from-to)	395-401
Number of pages	7
Journal	Journal of Toxicological Sciences
Volume	28
Issue number	5
DOIs	https://doi.org/10.2131/jts.28.395
Publication status	Published - Dec 2003

All Science Journal Classification (ASJC) codes

Toxicology

Access to Document

10.2131/jts.28.395

Cite this

@article{c7cae0ced6654c1588ae648d0bacf184,

title = "Formation of highly analgesic morphine-6-glucuronide following physiologic concentration of morphine in human brain",

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.",

author = "Hideyuki Yamada and Kumiko Ishii and Yuji Ishii and Ichiro Ieiri and Syunji Nishio and Takato Morioka and Kazuta Oguri",

year = "2003",

month = dec,

doi = "10.2131/jts.28.395",

language = "English",

volume = "28",

pages = "395--401",

journal = "Journal of Toxicological Sciences",

issn = "0388-1350",

publisher = "Japanese Society of Toxicological Sciences",

number = "5",

}

TY - JOUR

T1 - Formation of highly analgesic morphine-6-glucuronide following physiologic concentration of morphine in human brain

AU - Yamada, Hideyuki

AU - Ishii, Kumiko

AU - Ishii, Yuji

AU - Ieiri, Ichiro

AU - Nishio, Syunji

AU - Morioka, Takato

AU - Oguri, Kazuta

PY - 2003/12

Y1 - 2003/12

N2 - 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.

AB - 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.

UR - http://www.scopus.com/inward/record.url?scp=1642513343&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=1642513343&partnerID=8YFLogxK

U2 - 10.2131/jts.28.395

DO - 10.2131/jts.28.395

M3 - Article

C2 - 14746343

AN - SCOPUS:1642513343

SN - 0388-1350

VL - 28

SP - 395

EP - 401

JO - Journal of Toxicological Sciences

JF - Journal of Toxicological Sciences

IS - 5

ER -

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

Abstract

All Science Journal Classification (ASJC) codes

Access to Document

Other files and links

Fingerprint

Cite this