| pubmed-article:20127295 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:20127295 | lifeskim:mentions | umls-concept:C0034801 | lld:lifeskim |
| pubmed-article:20127295 | lifeskim:mentions | umls-concept:C1280500 | lld:lifeskim |
| pubmed-article:20127295 | lifeskim:mentions | umls-concept:C0439857 | lld:lifeskim |
| pubmed-article:20127295 | lifeskim:mentions | umls-concept:C1883254 | lld:lifeskim |
| pubmed-article:20127295 | lifeskim:mentions | umls-concept:C1514758 | lld:lifeskim |
| pubmed-article:20127295 | lifeskim:mentions | umls-concept:C1098957 | lld:lifeskim |
| pubmed-article:20127295 | lifeskim:mentions | umls-concept:C0599473 | lld:lifeskim |
| pubmed-article:20127295 | pubmed:issue | 2 | lld:pubmed |
| pubmed-article:20127295 | pubmed:dateCreated | 2010-3-24 | lld:pubmed |
| pubmed-article:20127295 | pubmed:abstractText | Cannabinoid CB(2) receptors represent a therapeutic target that circumvents unwanted central side effects (e.g., psychoactivity and/or addiction) associated with activation of CB(1) receptors. One of the primary investigative tools used to study functions of the CB(2) receptor is the aminoalkylindole (R,S)-AM1241. However, (R,S)-AM1241 has been described as an atypical CB(2) agonist which produces antinociception mediated indirectly by opioid receptors. (R,S)-AM1241 and its enantiomers, (R)-AM1241 and (S)-AM1241, were evaluated for antinociception in response to thermal (Hargreaves) and mechanical (von Frey) stimulation. Pharmacological specificity was established using antagonists for CB(1) (rimonabant [SR141716]) and CB(2) (SR144528). The opioid antagonist naloxone was administered locally in the paw or systemically to evaluate the contribution of opioid receptors to CB(2)-mediated antinociception produced by (R,S)-AM1241, (R)-AM1241, and (S)-AM1241. Comparisons were made with the opioid analgesic morphine. (R,S)-AM1241, (R)-AM1241, and (S)-AM1241 (0.033-10 mg/kg i.p.) produced antinociception to thermal, but not mechanical, stimulation of the hindpaw in naive rats. Antinociception produced by (R,S)-AM1241 and (S)-AM1241 exhibited an inverted U-shaped dose response curve. (R)-AM1241 produced greater antinociception than either (S)-AM1241 or (R,S)-AM1241 at the lowest (0.033 and 0.1 mg/kg i.p.) and highest (10 mg/kg i.p.) doses. Similar levels of antinociception were observed at intermediate doses. (R,S)-AM1241, (R)-AM1241, and (S)-AM1241 each produced CB(2)-mediated antinociception that was blocked by SR144528 but not by rimonabant. Local and systemic naloxone blocked morphine-induced antinociception but did not block antinociceptive effects of (R,S)-AM1241, (R)-AM1241, or (S)-AM1241. The antinociceptive effects of the CB(2)-selective cannabinoid (R,S)-AM1241 and its enantiomers, (R)-AM1241 and (S)-AM1241, are not dependent upon opioid receptors. | lld:pubmed |
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| pubmed-article:20127295 | pubmed:language | eng | lld:pubmed |
| pubmed-article:20127295 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20127295 | pubmed:citationSubset | IM | lld:pubmed |
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| pubmed-article:20127295 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:20127295 | pubmed:month | Jun | lld:pubmed |
| pubmed-article:20127295 | pubmed:issn | 1550-7416 | lld:pubmed |
| pubmed-article:20127295 | pubmed:author | pubmed-author:MakriyannisAl... | lld:pubmed |
| pubmed-article:20127295 | pubmed:author | pubmed-author:ZvonokAlexand... | lld:pubmed |
| pubmed-article:20127295 | pubmed:author | pubmed-author:HohmannAndrea... | lld:pubmed |
| pubmed-article:20127295 | pubmed:author | pubmed-author:RahnElizabeth... | lld:pubmed |
| pubmed-article:20127295 | pubmed:issnType | Electronic | lld:pubmed |
| pubmed-article:20127295 | pubmed:volume | 12 | lld:pubmed |
| pubmed-article:20127295 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:20127295 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:20127295 | pubmed:pagination | 147-57 | lld:pubmed |
| pubmed-article:20127295 | pubmed:dateRevised | 2011-9-26 | lld:pubmed |
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| pubmed-article:20127295 | pubmed:year | 2010 | lld:pubmed |
| pubmed-article:20127295 | pubmed:articleTitle | Antinociceptive effects of racemic AM1241 and its chirally synthesized enantiomers: lack of dependence upon opioid receptor activation. | lld:pubmed |
