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- Publications
- Influence
Potent antinociceptive effects of TRK-820, a novel κ-opioid receptor agonist
- T. Endoh, Hirotoshi Matsuura, +8 authors H. Nagase
- Chemistry
- 10 September 1999
Abstract TRK-820, a new type of 4,5-epoxymorphinan derivative, was investigated in vivo for antinociceptive activities and its selectivity on various opioid receptors in mice. Trk-820 given s.c. or… Expand
Potent antinociceptive effects of TRK-820, a novel kappa-opioid receptor agonist.
- T. Endoh, H. Matsuura, +7 authors H. Nagase
- Medicine
- Life sciences
- 1999
TRK-820, a new type of 4,5-epoxymorphinan derivative, was investigated in vivo for antinociceptive activities and its selectivity on various opioid receptors in mice. TRK-820 given s.c. or p.o. was… Expand
TRK-820, a selective kappa-opioid agonist, produces potent antinociception in cynomolgus monkeys.
- T. Endoh, A. Tajima, +7 authors H. Nagase
- Chemistry, Medicine
- Japanese journal of pharmacology
- 1 March 2001
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 kappa-receptor agonist with… Expand
TRK-820 , a Selective-Opioid Agonist , Produces Potent Antinociception in Cynomolgus Monkeys
TRK-820 (( )-17-cyclopropylmethyl-3,14b-dihydroxy-4,5a-epoxy-6b-[N-methyl-trans-3-(3furyl)acrylamide]morphinan hydrochloride) has been shown to be a potent opioid -receptor agonist with… Expand
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Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
- K. Kawai, J. Hayakawa, +10 authors H. Nagase
- Chemistry, Medicine
- Bioorganic & medicinal chemistry
- 15 October 2008
By focusing on 4,5-epoxymorphinan, a traditional opioid skeleton but a new structure in the opioid kappa-agonist research field, and by rationally applying the 'message-address concept' and… Expand
Synthesis of a stable iminium salt and propellane derivatives.
- H. Nagase, N. Yamamoto, +8 authors H. Fujii
- Chemistry, Medicine
- The Journal of organic chemistry
- 24 September 2008
The treatment of morphinan 1 with NaH and MsCl provided very stable iminium salt 7 possessing propellane skeleton. One of the synthesized iminium salts 7, isobutyl derivative 7b, was crystallized and… Expand
Effect of repeated administration of TRK-820, a κ-opioid receptor agonist, on tolerance to its antinociceptive and sedative actions
- T. Suzuki, N. Izumimoto, Y. Takezawa, M. Fujimura, T. Endoh
- Chemistry, Medicine
- Brain Research
- 9 January 2004
Repeated administration of micro-opioid receptor agonist, morphine induces tolerance not only to the antinociceptive effect but also to other pharmacological effects, resulting in shortened working… Expand
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology: part 1.
- N. Yamamoto, H. Fujii, +6 authors H. Nagase
- Chemistry, Medicine
- Bioorganic & medicinal chemistry letters
- 1 July 2011
The observation that 17-cyclopropylmethylmorphinan derivatives without the 4,5-epoxy ring showed more κ selectivity than those with a 4,5-epoxy ring led us to develop a working hypothesis: the… Expand
Design and synthesis of a metabolically stable and potent antitussive agent, a novel delta opioid receptor antagonist, TRK-851.
- S. Sakami, K. Kawai, +12 authors H. Nagase
- Chemistry, Medicine
- Bioorganic & medicinal chemistry
- 1 September 2008
We have previously reported on antitussive effect of (5R,9R,13S,14S)-17-cyclopropylmethyl-6,7-didehydro-4,5-epoxy-5',6'-dihydro-3-methoxy-4'H-pyrrolo[3,2,1-ij]quinolino[2',1':6,7]morphinan-14-ol(1b)… Expand
Characteristics of TRK-130 (Naltalimide), a Novel Opioid Ligand, as a New Therapeutic Agent for Overactive Bladder
- Morihiro Fujimura, N. Izumimoto, +9 authors K. Kawai
- Chemistry, Medicine
- The Journal of Pharmacology and Experimental…
- 1 September 2014
We characterized TRK-130 (N-[(5R,6R,14S)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]phthalimide; naltalimide), an opioid ligand, to clarify the therapeutic potential for overactive… Expand