Source:http://linkedlifedata.com/resource/pubmed/id/16051396
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
6
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| pubmed:dateCreated |
2005-9-6
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| pubmed:abstractText |
We investigated the effect of 5-HT receptor antagonists on mechanical hyperalgesia observed in a neuropathic pain rat model prepared by chronic constriction injury of the sciatic nerve. NAN-190, a 5-HT 1A receptor antagonist, (-)-pindolol, a 5-HT 1A/1B receptor antagonist, and tropisetron, a 5-HT(3/4) receptor antagonist, did not affect the pain threshold in the hyperalgesic hind limb to the same extent as in the normal hind limb. However, sarpogrelate and ketanserin, 5-HT 2A receptor antagonists, significantly elevated the pain threshold in the hyperalgesic hind limb, but not in the normal hind limb. In spite of its high affinity for the 5-HT 2A receptor, methysergide only slightly elevated the pain threshold in the hyperalgesic hind limb. Pre-treatment with methysergide significantly antagonized the inhibitory effect of sarpogrelate on hyperalgesia. Furthermore, the 5-HT 2A receptor specific binding activity of 3H-ketanserin determined for the hyperalgesic hind limb did not differ from that of the normal hind limb. From these results, we propose that the 5-HT 2A receptor in the hyperalgesic hind paw function as an agonist-independent active receptor following constriction of the sciatic nerve, and that sarpogrelate and ketanserin act as inverse agonists of this receptor and suppress its activation. Methysergide may act as a neutral antagonist that blocks the effect of inverse agonists on the 5-HT 2A receptor.
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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/Ketanserin,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Serotonin, 5-HT2A,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin 5-HT2 Receptor Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Receptor Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Succinates,
http://linkedlifedata.com/resource/pubmed/chemical/sarpogrelate
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| pubmed:status |
MEDLINE
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| pubmed:month |
Nov
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| pubmed:issn |
0197-0186
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| pubmed:author | |
| pubmed:issnType |
Print
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| pubmed:volume |
47
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| pubmed:owner |
NLM
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| pubmed:authorsComplete |
Y
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| pubmed:pagination |
394-400
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| pubmed:dateRevised |
2010-11-18
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| pubmed:meshHeading |
pubmed-meshheading:16051396-Animals,
pubmed-meshheading:16051396-Binding, Competitive,
pubmed-meshheading:16051396-Binding Sites,
pubmed-meshheading:16051396-Denervation,
pubmed-meshheading:16051396-Disease Models, Animal,
pubmed-meshheading:16051396-Drug Interactions,
pubmed-meshheading:16051396-Hyperalgesia,
pubmed-meshheading:16051396-Ketanserin,
pubmed-meshheading:16051396-Ligation,
pubmed-meshheading:16051396-Male,
pubmed-meshheading:16051396-Neuralgia,
pubmed-meshheading:16051396-Pain Threshold,
pubmed-meshheading:16051396-Peripheral Nerves,
pubmed-meshheading:16051396-Peripheral Nervous System Diseases,
pubmed-meshheading:16051396-Radioligand Assay,
pubmed-meshheading:16051396-Rats,
pubmed-meshheading:16051396-Rats, Sprague-Dawley,
pubmed-meshheading:16051396-Receptor, Serotonin, 5-HT2A,
pubmed-meshheading:16051396-Sciatic Neuropathy,
pubmed-meshheading:16051396-Sensory Receptor Cells,
pubmed-meshheading:16051396-Serotonin 5-HT2 Receptor Antagonists,
pubmed-meshheading:16051396-Serotonin Antagonists,
pubmed-meshheading:16051396-Serotonin Receptor Agonists,
pubmed-meshheading:16051396-Succinates
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| pubmed:year |
2005
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| pubmed:articleTitle |
Contribution of the peripheral 5-HT 2A receptor to mechanical hyperalgesia in a rat model of neuropathic pain.
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| pubmed:affiliation |
Department of Pharmacology, Faculty of Pharmacy and Pharmaceutical Sciences, Fukuyama University, Fukuyama, Hiroshima 729-0292, Japan.
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| pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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