TRK-820, a Selective к-Opioid Agonist, Produces Potent Antinociception in Cynomolgus Monkeys
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概要
- 論文の詳細を見る
TRK-820 ((−)-17-cyclopropylmethyl-3,14b-dihydroxy-4,5a-epoxy-6b-[N-methyl-trans-3-(3-furyl)acrylamide]morphinan hydrochloride) has been shown to be a potent opioid κ-receptor agonist with pharmacological properties different from those produced by κ1-opioid receptor agonists in rodents. To ascertain whether or not these properties of TRK-820 would be extended to primates, the antinociceptive effect of TRK-820 was evaluated in cynomolgus monkeys by the hot-water tail-withdrawal procedure. TRK-820 given intramuscularly (i.m.) produced a potent antinociceptive effect that was 295- and 495-fold more potent than morphine with the 50°C and 55°C hot-water tests, respectively, and 40-fold more potent than U-50,488H and 1,000-fold more potent than pentazocine in the 50°C hot-water test. The duration of antinociceptive effects of TRK-820 treatment (0.01 and 0.03 mg/kg, i.m.) lasted more than 6 h, which was much longer than those of U-50,488H. The antinociception produced by the higher dose (0.03 mg/kg, i.m.) of TRK-820 was not inhibited by nor-binaltorphimine (3.2 and 10 mg/kg, s.c.) or by naloxone (0.1 mg/kg, s.c.), although the antinociception induced by a lower dose of TRK-820 (0.01 mg/kg, i.m.) was inhibited by nor-binaltorphimine (10 mg/kg, s.c.). The same doses of nor-binaltorphimine and naloxone effectively inhibited the antinociception induced by the higher doses of U-50,488H (1.0 mg/kg, i.m.) and morphine (10 mg/kg, i.m.), respectively. These results indicate that the antinociception induced by TRK-820 is less sensitive to nor-binaltorphimine and suggest that it is mediated by the stimulation of a subtype of κ-opioid receptor different from the κ1-opioid receptor in cynomolgus monkeys.
- 社団法人 日本薬理学会の論文
- 2001-03-01
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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SUZUKI Tsutomu
Department of Applied and Environmental Chemistry, Kitami Institute of Technology
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Tseng L
Department Of Anesthesiology Medical College Of Wisconsin
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Tseng Leon
Department Of Anesthesiology Medical College Of Wisconsin
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Sawaguchi T
Department Of Emergency Medicine Tokyo Women's Medical University
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NARITA Minoru
Department of Toxicology, School of Pharmacy, Hoshi University
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KAMEI Junzo
Department of Pathophysiology, School of Pharmacy and Pharmaceutical Sciences, Hoshi University
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MIZOGUCHI Hirokazu
Department of Physiology and Anatomy, Tohoku Pharmaceutical University
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Saitoh A
Pharmaceutical Research Laboratories Toray Industries Inc.
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SUZUKI Tomohiko
Pharmaceutical Research Laboratories, Toray Industries, Inc.
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ENDOH Takashi
Pharmaceutical Laboratories, Toray Industries Inc.
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TAJIMA Atsushi
Pharmaceutical Laboratories, Toray Industries Inc.
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IZUMIMOTO Naoki
Pharmaceutical Laboratories, Toray Industries Inc.
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SAITOH Akiyoshi
Pharmaceutical Laboratories, Toray Industries Inc.
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Kamei Junzo
Department Of Pathophysiology And Therapeutics Faculty Of Pharmaceutical Sciences Hoshi University
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Kamei Junzo
Department Of Pathophysilology & Therapeutics Faculty Of Pharmaceutical Sciences Hoshi Universit
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Endoh Takashi
Pharmaceutical Laboratories Toray Industries Inc.
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Nomura Mutsuko
Department Of Toxicology Hoshi University School Of Pharmacy And Pharmaceutical Sciences
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Izumimoto Naoki
Pharmaceutical Laboratories Toray Industries Inc.
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Namiki Mizuho
Dep. Of Emergency Medicine Tokyo Women's Medical Univ. Jpn
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Namiki Mizuho
Department Of Emergency Medicine Tokyo Women's Medical University
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Narita Minoru
Department Of Emergency Medicine Tokyo Women's Medical University
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Saitoh A
Department Of Pathophysiology And Therapeutics School Of Pharmacy And Pharmaceutical Sciences Hoshi
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Mizoguchi Hirokazu
Department Of Anesthesiology Medical College Of Wisconsin
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Narita Minoru
Department Of Anesthesiology Medical College Of Wisconsin
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Nomura Mutsuko
Department Of Emergency Medicine Tokyo Women's Medical University
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Tajima Atsushi
Pharmaceutical Laboratories Toray Industries Inc.
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Kamei Junzo
Department Of Pathophysiology & Therapeutics School Of Pharmacy And Pharmaceutical Sciences Hosh
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Suzuki Tsutomu
Department Of Applied And Environmental Chemistry Kitami Institute Of Technology
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