Source:http://linkedlifedata.com/resource/pubmed/id/10573186
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
16
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pubmed:dateCreated |
1999-12-8
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pubmed:abstractText |
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 found to be 351- and 796-fold more potent than U50,488H with acetic acid-induced abdominal constriction test. The duration of the antinociceptive effect produced by TRK-820 was longer than that produced by mu-opioid receptor agonist morphine or other kappa-opioid receptor agonists. In addition, with four other antinociceptive assays, low temperature hot plate (51 degrees C), thermal tail flick, mechanical tail pressure and tail pinch tests, TRK-820 was also found to be 68- to 328-fold more potent than U-50488H, and 41- to 349-fold more potent than morphine in producing antinociception, as comparing the weight of the different compound. However, TRK-820 was less active in inhibiting the high temperature (55 degrees C) hot plate response. The antinociceptive effects produced by TRK-820 were inhibited by nor-BNI, but not by naloxone or naltrindole (NTI) with the abdominal constriction test, indicating that the antinociception is selectively mediated by the stimulation of kappa-, but not mu- or delta-opioid receptors. Co-administration of TRK-820 with morphine slightly enhanced the antinociception induced by morphine in the mouse hot plate test. On the other hand, pentazocine significantly reduced the morphine-induced antinociception. TRK-820 produced sedation at doses, which are much higher than the doses for producing antinociception. These results indicate that the potent antinociception induced by TRK-820 is mediated via the stimulation of kappa-, but not mu- or delta-opiod receptors.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Analgesics, Non-Narcotic,
http://linkedlifedata.com/resource/pubmed/chemical/Analgesics, Opioid,
http://linkedlifedata.com/resource/pubmed/chemical/Hypnotics and Sedatives,
http://linkedlifedata.com/resource/pubmed/chemical/Morphinans,
http://linkedlifedata.com/resource/pubmed/chemical/Pentazocine,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, kappa,
http://linkedlifedata.com/resource/pubmed/chemical/Spiro Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/TRK 820
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pubmed:status |
MEDLINE
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pubmed:issn |
0024-3205
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
65
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1685-94
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:10573186-Administration, Oral,
pubmed-meshheading:10573186-Analgesics, Non-Narcotic,
pubmed-meshheading:10573186-Analgesics, Opioid,
pubmed-meshheading:10573186-Animals,
pubmed-meshheading:10573186-Constriction, Pathologic,
pubmed-meshheading:10573186-Drug Interactions,
pubmed-meshheading:10573186-Hypnotics and Sedatives,
pubmed-meshheading:10573186-Injections, Subcutaneous,
pubmed-meshheading:10573186-Male,
pubmed-meshheading:10573186-Mice,
pubmed-meshheading:10573186-Morphinans,
pubmed-meshheading:10573186-Motor Activity,
pubmed-meshheading:10573186-Nociceptors,
pubmed-meshheading:10573186-Pentazocine,
pubmed-meshheading:10573186-Receptors, Opioid, kappa,
pubmed-meshheading:10573186-Spiro Compounds
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pubmed:year |
1999
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pubmed:articleTitle |
Potent antinociceptive effects of TRK-820, a novel kappa-opioid receptor agonist.
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pubmed:affiliation |
Basic Research Laboratories, Toray Industries, Inc., Kanagawa, Japan. Takashi_Endo@nts.toray.co.jp
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pubmed:publicationType |
Journal Article
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