Source:http://linkedlifedata.com/resource/pubmed/id/16219031
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
6
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| pubmed:dateCreated |
2005-12-20
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| pubmed:abstractText |
Antagonists at NK1 substance P receptors have demonstrated similar antidepressant properties in both animal paradigms and in human as selective serotonin reuptake inhibitors (SSRIs) that induce desensitization of 5-HT 1A autoreceptors within the dorsal raphe nucleus (DRN). We investigated whether this receptor adaptation also occurs upon NK1 receptor blockade. C57B/L6J mice were treated for 21 days with the selective NK1 receptor antagonist GR 205171 (10 mg/kg daily) through subcutaneously implanted osmotic mini pumps, and DRN 5-HT 1A autoreceptor functioning was assessed using various approaches. Recording of DRN serotonergic neurons in brainstem slices showed that GR 205171 treatment reduced (by approximately 1.5 fold) the potency of the 5-HT 1A receptor agonist, ipsapirone, to inhibit cell firing. In parallel, the 5-HT 1A autoreceptor-mediated [35S]GTP-gamma-S binding induced by 5-carboxamidotryptamine onto the DRN in brainstem sections was significantly decreased in GR 205171-treated mice. In vivo microdialysis showed that the cortical 5-HT overflow caused by acute injection of the SSRI paroxetine (1 mg/kg) was twice as high in GR 205171-treated as in vehicle-treated controls. In the DRN, basal 5-HT outflow was significantly enhanced by GR 205171 treatment. These data supported the hypothesis that chronic NK1 receptor blockade induces a functional desensitization of 5-HT 1A autoreceptors similar to that observed with SSRIs.
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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/Autoreceptors,
http://linkedlifedata.com/resource/pubmed/chemical/GR 205171,
http://linkedlifedata.com/resource/pubmed/chemical/Guanosine 5'-O-(3-Thiotriphosphate),
http://linkedlifedata.com/resource/pubmed/chemical/Paroxetine,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Serotonin, 5-HT1A,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Neurokinin-1,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Uptake Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Tetrazoles
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| pubmed:status |
MEDLINE
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| pubmed:month |
Dec
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| pubmed:issn |
0022-3042
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| pubmed:author | |
| pubmed:issnType |
Print
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| pubmed:volume |
95
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| pubmed:owner |
NLM
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| pubmed:authorsComplete |
Y
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| pubmed:pagination |
1713-23
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| pubmed:dateRevised |
2006-11-15
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| pubmed:meshHeading |
pubmed-meshheading:16219031-Animals,
pubmed-meshheading:16219031-Autoradiography,
pubmed-meshheading:16219031-Autoreceptors,
pubmed-meshheading:16219031-Electrophysiology,
pubmed-meshheading:16219031-Guanosine 5'-O-(3-Thiotriphosphate),
pubmed-meshheading:16219031-Male,
pubmed-meshheading:16219031-Mice,
pubmed-meshheading:16219031-Mice, Inbred C57BL,
pubmed-meshheading:16219031-Mice, Knockout,
pubmed-meshheading:16219031-Microdialysis,
pubmed-meshheading:16219031-Paroxetine,
pubmed-meshheading:16219031-Piperidines,
pubmed-meshheading:16219031-Raphe Nuclei,
pubmed-meshheading:16219031-Receptor, Serotonin, 5-HT1A,
pubmed-meshheading:16219031-Receptors, Neurokinin-1,
pubmed-meshheading:16219031-Serotonin Antagonists,
pubmed-meshheading:16219031-Serotonin Uptake Inhibitors,
pubmed-meshheading:16219031-Tetrazoles
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| pubmed:year |
2005
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| pubmed:articleTitle |
Sustained pharmacological blockade of NK1 substance P receptors causes functional desensitization of dorsal raphe 5-HT 1A autoreceptors in mice.
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| pubmed:affiliation |
INSERM/UPMC, Neuropsychopharmacologie, CHU Pitié-Salpêtrière, Paris, France.
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| pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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