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Potent antinociceptive effects of TRK-820, a novel κ-opioid receptor agonist
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. orExpand
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Potent antinociceptive effects of TRK-820, a novel kappa-opioid receptor agonist.
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. wasExpand
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TRK-820, a selective kappa-opioid agonist, produces potent antinociception in cynomolgus monkeys.
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 withExpand
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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 withExpand
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Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
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' andExpand
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Synthesis of a stable iminium salt and propellane derivatives.
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 andExpand
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Effect of repeated administration of TRK-820, a κ-opioid receptor agonist, on tolerance to its antinociceptive and sedative actions
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 workingExpand
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Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology: part 1.
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: theExpand
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Design and synthesis of a metabolically stable and potent antitussive agent, a novel delta opioid receptor antagonist, TRK-851.
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
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Characteristics of TRK-130 (Naltalimide), a Novel Opioid Ligand, as a New Therapeutic Agent for Overactive Bladder
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 overactiveExpand
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