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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
24
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pubmed:dateCreated |
2001-8-13
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pubmed:abstractText |
Small-molecule nociceptin antagonists were synthesized to examine their therapeutic potential. After a 4-aminoquinoline derivative was found to bind with the human ORL(1) receptor, a series of 4-aminoquinolines and related compounds were synthesized and their binding was evaluated. Elucidation of structure-activity relationships eventually led to the optimum compounds. One of these compounds, N-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl)benzamide hydrochloride (11) not only antagonized nociceptin-induced allodynia in mice but also showed analgesic effect in a hot plate test using mice and in a formalin test using rats. Its analgesic effect was not antagonized by the opioid antagonist naloxone. These results indicate that this nociceptin antagonist has the potential to become a novel type of analgesic that differs from mu-opioid agonists.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Adenosine Monophosphate,
http://linkedlifedata.com/resource/pubmed/chemical/Aminoquinolines,
http://linkedlifedata.com/resource/pubmed/chemical/Analgesics,
http://linkedlifedata.com/resource/pubmed/chemical/Benzamides,
http://linkedlifedata.com/resource/pubmed/chemical/Naloxone,
http://linkedlifedata.com/resource/pubmed/chemical/Narcotic Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Opioid Peptides,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, delta,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, kappa,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, mu,
http://linkedlifedata.com/resource/pubmed/chemical/nociceptin
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
30
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pubmed:volume |
43
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4667-77
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:11101358-Adenosine Monophosphate,
pubmed-meshheading:11101358-Aminoquinolines,
pubmed-meshheading:11101358-Analgesics,
pubmed-meshheading:11101358-Animals,
pubmed-meshheading:11101358-Benzamides,
pubmed-meshheading:11101358-Cell Line,
pubmed-meshheading:11101358-Drug Evaluation, Preclinical,
pubmed-meshheading:11101358-Humans,
pubmed-meshheading:11101358-Male,
pubmed-meshheading:11101358-Mice,
pubmed-meshheading:11101358-Mice, Inbred ICR,
pubmed-meshheading:11101358-Naloxone,
pubmed-meshheading:11101358-Narcotic Antagonists,
pubmed-meshheading:11101358-Opioid Peptides,
pubmed-meshheading:11101358-Pain Measurement,
pubmed-meshheading:11101358-Radioligand Assay,
pubmed-meshheading:11101358-Receptors, Opioid, delta,
pubmed-meshheading:11101358-Receptors, Opioid, kappa,
pubmed-meshheading:11101358-Receptors, Opioid, mu,
pubmed-meshheading:11101358-Structure-Activity Relationship
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pubmed:year |
2000
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pubmed:articleTitle |
4-Aminoquinolines: novel nociceptin antagonists with analgesic activity.
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pubmed:affiliation |
Central Pharmaceutical Research Institute, JT Inc., 1-1 Murasaki-cho, Takatsuki, Osaka 569-1125, Japan. hisashi.shinkai@ims.jti.co.jp
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pubmed:publicationType |
Journal Article
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