Syntheses of Potential Metabolites of a Potent к-Opioid Receptor Agonist, TRK-820
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概要
- 論文の詳細を見る
Chemical syntheses of three kinds of potential metabolites of TRK-820, a potent к-opioid receptor agonist, were described. One of the potential metabolites 2, 17-N-dealkylated TRK-820, was synthesized starting from noroxycodone through 8 steps in 21% total yield. Glucuronidation of intermediate 10 and compound 1, the free base of TRK-820, was carried out stereoselectively to give 3-O-β-D-glucuronides 15 and 16 in good yields, respectively. Syntheses of potential conjugated metabolites 3 and 4 were accomplished through 10 steps and 2 steps in 11% and 43% total yields, respectively. Among the potential metabolites of TRK-820, compounds 2 and 4 were identified as metabolites in human hepatocytes. The results of pharmacological studies of compounds 2, 3, and 4 are described.
- 公益社団法人日本薬学会の論文
- 2004-06-01
著者
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Nagase H
Basic Research Laboratories Toray Industries Inc.
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Nagase Hiroshi
Pharmaceutical Research Laboratories Toray Industries Inc.
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Seki Chie
Pharmaceutical Research Laboratories Toray Industries Inc.
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Kawai K
Hoshi Univ. Tokyo Jpn
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Hayakawa Jun
Hitachi Ltd. Central Research Laboratory
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Hayakawa Jun
Pharmaceutical Research Laboratories Toray Industries Inc.
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Kawai Koji
Basic Research Laboratories Toray Industries Inc.
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KAWAMURA Kuniaki
Pharmaceutical Research Laboratories, Toray Industries, Inc.
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HORIKIRI Hiromasa
Pharmaceutical Research Laboratories, Toray Industries, Inc.
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YOSHIZAWA Ken-ichi
Pharmaceutical Research Laboratories, Toray Industries, Inc.
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UMEUCHI Hideo
Pharmaceutical Research Laboratories, Toray Industries, Inc.
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Umeuchi Hideo
Pharmaceutical Research Laboratories Toray Industries Inc.
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Katsuya K
Graduate School Of Life & Environmental Sciences University Of Tsukuba
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Horikiri H
Pharmaceutical Research Laboratories Toray Industries Inc.
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Yoshizawa K
Pharmaceutical Research Laboratories Toray Industries Inc.
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