Source:http://linkedlifedata.com/resource/pubmed/id/16129413
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
2005-9-9
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pubmed:abstractText |
NPFF agonists designed to be selective NPFF(2) receptor probes were synthesized. D.Asn-Pro-(N-Me)Ala-Phe-Leu-Phe-Gln-Pro-Gln-Arg-Phe-NH(2) (dNPA) displays a very high affinity (0.027nM) for NPFF(2) receptors transfected in CHO cells, and a very high selectivity with a discrimination ratio greater than 100 versus NPFF(1) receptors. dNPA acts as a potent and selective agonist in [(35)S]GTPgammaS binding experiments and inhibits intracellular cAMP production with the same efficacy as NPA-NPFF. In SH-SY5Y cells expressing NPFF(2) receptors dNPA, in the presence of carbachol, stimulates Ca(2+) release from the intracellular stores. In vivo, after intracerebroventricular injection dNPA increases body temperature in mice and reverses the morphine-induced analgesia. Also, dNPA displays anti-opioid activity after systemic administration. So far, dNPA exhibits the highest affinity and selectivity for NPFF(2) receptors and reveals that its behavioral anti-opioid activity depends on the degree of opioid-induced analgesia.
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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, Opioid,
http://linkedlifedata.com/resource/pubmed/chemical/Molecular Probes,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Muscarinic,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Neuropeptide,
http://linkedlifedata.com/resource/pubmed/chemical/neuropeptide FF receptor
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pubmed:status |
MEDLINE
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pubmed:month |
Oct
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pubmed:issn |
0006-291X
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
14
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pubmed:volume |
336
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
197-203
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:16129413-Amino Acid Sequence,
pubmed-meshheading:16129413-Analgesics, Opioid,
pubmed-meshheading:16129413-Animals,
pubmed-meshheading:16129413-Body Temperature,
pubmed-meshheading:16129413-Brain,
pubmed-meshheading:16129413-CHO Cells,
pubmed-meshheading:16129413-Cell Line, Tumor,
pubmed-meshheading:16129413-Cricetinae,
pubmed-meshheading:16129413-Humans,
pubmed-meshheading:16129413-Injections, Intraventricular,
pubmed-meshheading:16129413-Mice,
pubmed-meshheading:16129413-Molecular Probes,
pubmed-meshheading:16129413-Receptors, Muscarinic,
pubmed-meshheading:16129413-Receptors, Neuropeptide,
pubmed-meshheading:16129413-Signal Transduction
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pubmed:year |
2005
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pubmed:articleTitle |
Anti-analgesia of a selective NPFF2 agonist depends on opioid activity.
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pubmed:affiliation |
Institut de Pharmacologie et de Biologie Structurale, CNRS UMR 5089, 205 Route de Narbonne, 31077 Toulouse Cedex, France.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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