rdf:type |
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lifeskim:mentions |
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pubmed:issue |
9
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pubmed:dateCreated |
1984-10-18
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pubmed:abstractText |
Some in vivo agonist and antagonist properties of the putative k-compound bremazocine were characterized in rats. Bremazocine, at doses from 0.015-32 mg/kg i.p., delayed nociceptive reaction on a 55 degrees C hot-plate with a dose-response curve not readily fitting a single straight line; this effect was antagonized by high doses of naloxone. In the same rats bremazocine did not delay the intestinal transit of a charcoal meal fed 5 min earlier and prevented morphine-induced constipation. This antagonism appeared to be opioid-specific and competitive, with apparent pA2 value 8.56. Catatonia induced by etorphine (0.004 mg/kg s.c.) and constipation induced by etorphine (0.004 mg/kg s.c.) and D-Ala2-D-Leu5-enkephalin (0.1 mg/kg i.p.) were completely antagonized by bremazocine (0.03-8 mg/kg i.p.). Antinociception induced by morphine (10 mg/kg i.v.) and etorphine (0.004 mg/kg s.c.) was only partly prevented. Naloxone (1 mg/kg) and bremazocine (0.015-1 mg/kg i.p.) precipitated a withdrawal syndrome, evaluated as jumping frequency, in rats rendered dependent to morphine. These data suggest the involvement of more than one opioid receptor population in bremazocine action in vivo.
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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/Analgesics,
http://linkedlifedata.com/resource/pubmed/chemical/Benzomorphans,
http://linkedlifedata.com/resource/pubmed/chemical/Enkephalin, Leucine,
http://linkedlifedata.com/resource/pubmed/chemical/Enkephalin, Leucine-2-Alanine,
http://linkedlifedata.com/resource/pubmed/chemical/Etorphine,
http://linkedlifedata.com/resource/pubmed/chemical/Morphinans,
http://linkedlifedata.com/resource/pubmed/chemical/Morphine,
http://linkedlifedata.com/resource/pubmed/chemical/Naloxone,
http://linkedlifedata.com/resource/pubmed/chemical/bremazocine
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pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
0024-3205
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
27
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pubmed:volume |
35
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
917-27
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:6381949-Analgesics,
pubmed-meshheading:6381949-Animals,
pubmed-meshheading:6381949-Benzomorphans,
pubmed-meshheading:6381949-Catatonia,
pubmed-meshheading:6381949-Constipation,
pubmed-meshheading:6381949-Dose-Response Relationship, Drug,
pubmed-meshheading:6381949-Enkephalin, Leucine,
pubmed-meshheading:6381949-Enkephalin, Leucine-2-Alanine,
pubmed-meshheading:6381949-Etorphine,
pubmed-meshheading:6381949-Gastrointestinal Motility,
pubmed-meshheading:6381949-Humans,
pubmed-meshheading:6381949-Male,
pubmed-meshheading:6381949-Morphinans,
pubmed-meshheading:6381949-Morphine,
pubmed-meshheading:6381949-Naloxone,
pubmed-meshheading:6381949-Rats,
pubmed-meshheading:6381949-Substance Withdrawal Syndrome,
pubmed-meshheading:6381949-Substance-Related Disorders
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pubmed:year |
1984
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pubmed:articleTitle |
Bremazocine induces antinociception, but prevents opioid-induced constipation and catatonia in rats and precipitates withdrawal in morphine-dependent rats.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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