Source:http://linkedlifedata.com/resource/pubmed/id/21672568
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
7
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| pubmed:dateCreated |
2011-7-15
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| pubmed:abstractText |
Nociceptin/orphanin FQ (N/OFQ), the endogenous ligand for the N/OFQ peptide (NOP) receptors, has been shown to be metabolized into some fragments. We examined to determine whether intrathecal (i.t.) N/OFQ (1-13), (1-11) and (1-7) have antinociceptive activity in the pain-related behavior after intraplantar injection of capsaicin. The i.t. administration of N/OFQ (0.3-1.2 nmol) produced an appreciable and dose-dependent inhibition of capsaicin-induced paw-licking/biting response. The N-terminal fragments of N/OFQ, (1-13) and (1-11), were antinociceptive with a potency lower than N/OFQ. Calculated ID?? values (nmol, i.t.) were 0.83 for N/OFQ, 2.5 for N/OFQ (1-13) and 4.75 for N/OFQ (1-11), respectively. The time-course effect revealed that the antinociceptive effects of these N-terminal fragments lasted longer than those of N/OFQ. Removal of amino acids down to N/OFQ (1-7) led to be less potent than N/OFQ and its fragments, (1-13) and (1-11). Antinociception induced by N/OFQ or N/OFQ (1-13) was reversed significantly by i.t. co-injection of [Nphe¹]N/OFQ (1-13)NH?, a peptidergic antagonist for NOP receptors, whereas i.t. injection of the antagonist did not interfere with the action of N/OFQ (1-11) and (1-7). Pretreatment with the opioid receptor antagonist naloxone hydrochloride did not affect the antinociception induced by N/OFQ and its N-terminal fragments. These results suggest that N-terminal fragments of N/OFQ are active metabolites and may modulate the antinociceptive effect of N/OFQ in the spinal cord. The results also indicate that N/OFQ (1-13) still possess antinociceptive activity through NOP 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,
http://linkedlifedata.com/resource/pubmed/chemical/Capsaicin,
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/Peptide Fragments,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid,
http://linkedlifedata.com/resource/pubmed/chemical/nociceptin
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| pubmed:status |
MEDLINE
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| pubmed:month |
Jul
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| pubmed:issn |
1873-5169
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| pubmed:author | |
| pubmed:copyrightInfo |
Copyright © 2011 Elsevier Inc. All rights reserved.
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| pubmed:issnType |
Electronic
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| pubmed:volume |
32
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| pubmed:owner |
NLM
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| pubmed:authorsComplete |
Y
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| pubmed:pagination |
1530-5
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| pubmed:meshHeading |
pubmed-meshheading:21672568-Analgesics,
pubmed-meshheading:21672568-Animals,
pubmed-meshheading:21672568-Behavior, Animal,
pubmed-meshheading:21672568-Capsaicin,
pubmed-meshheading:21672568-Dose-Response Relationship, Drug,
pubmed-meshheading:21672568-Drug Interactions,
pubmed-meshheading:21672568-Inhibitory Concentration 50,
pubmed-meshheading:21672568-Injections, Spinal,
pubmed-meshheading:21672568-Injections, Subcutaneous,
pubmed-meshheading:21672568-Male,
pubmed-meshheading:21672568-Mice,
pubmed-meshheading:21672568-Mice, Inbred Strains,
pubmed-meshheading:21672568-Naloxone,
pubmed-meshheading:21672568-Narcotic Antagonists,
pubmed-meshheading:21672568-Opioid Peptides,
pubmed-meshheading:21672568-Pain,
pubmed-meshheading:21672568-Pain Measurement,
pubmed-meshheading:21672568-Pain Perception,
pubmed-meshheading:21672568-Peptide Fragments,
pubmed-meshheading:21672568-Receptors, Opioid,
pubmed-meshheading:21672568-Spinal Cord,
pubmed-meshheading:21672568-Structure-Activity Relationship
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| pubmed:year |
2011
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| pubmed:articleTitle |
Antinociceptive effects of spinally administered nociceptin/orphanin FQ and its N-terminal fragments on capsaicin-induced nociception.
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| pubmed:affiliation |
Department of Pharmacology, Daiichi College of Pharmaceutical Sciences, 22-1 Tamagawa-cho, Minami-ku, Fukuoka 815-8511, Japan.
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| pubmed:publicationType |
Journal Article
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