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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
1999-1-21
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pubmed:abstractText |
Single treatment with the serotonin (5-hydroxytryptamine) 5-HT1A receptor agonists 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) and alnespirone (S-20499) reduces the extracellular 5-HT concentration (5-HText) in the rat midbrain and forebrain. Given the therapeutic potential of selective 5-HT1A agonists in the treatment of affective disorders, we have examined the changes in 5-HT1A receptors induced by 2-week minipump administration of alnespirone (0.3 and 3 mg/kg/day) and 8-OH-DPAT (0.1 and 0.3 mg/kg/day). The treatment with alnespirone did not modify baseline 5-HText but significantly attenuated the ability of 0.3 mg/kg s.c. alnespirone to reduce 5-HText in the dorsal raphe nucleus (DRN) and frontal cortex. In contrast, the ability of 8-OH-DPAT (0.025 and 0.1 mg/kg s.c.) to reduce 5-HText in both areas was unchanged by 8-OH-DPAT pretreatment. Autoradiographic analysis revealed a significant reduction of [3H]8-OH-DPAT and [3H]WAY-100635 [3H-labeled N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridyl)cyclohexa necarboxamide x 3HCl] binding to somatodendritic 5-HT1A receptors (but not to postsynaptic 5-HT1A receptors) of rats pretreated with alnespirone but not with 8-OH-DPAT. In situ hybridization analysis revealed no change of the density of the mRNA encoding the 5-HT1A receptors in the DRN after either treatment. These data indicate that continuous treatment for 2 weeks with alnespirone, but not with 8-OH-DPAT, causes a functional desensitization of somatodendritic 5-HT1A receptors controlling 5-HT release in the DRN and frontal cortex.
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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/8-Hydroxy-2-(di-n-propylamino)tetral...,
http://linkedlifedata.com/resource/pubmed/chemical/RNA, Messenger,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin, 5-HT1,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Receptor Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Spiro Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/alnespirone
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0022-3042
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
72
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
262-72
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:9886078-8-Hydroxy-2-(di-n-propylamino)tetralin,
pubmed-meshheading:9886078-Animals,
pubmed-meshheading:9886078-Anxiety,
pubmed-meshheading:9886078-Autoradiography,
pubmed-meshheading:9886078-Brain Chemistry,
pubmed-meshheading:9886078-Dendrites,
pubmed-meshheading:9886078-Depression,
pubmed-meshheading:9886078-Dose-Response Relationship, Drug,
pubmed-meshheading:9886078-Frontal Lobe,
pubmed-meshheading:9886078-Gene Expression,
pubmed-meshheading:9886078-In Situ Hybridization,
pubmed-meshheading:9886078-Male,
pubmed-meshheading:9886078-Microdialysis,
pubmed-meshheading:9886078-RNA, Messenger,
pubmed-meshheading:9886078-Radioligand Assay,
pubmed-meshheading:9886078-Raphe Nuclei,
pubmed-meshheading:9886078-Rats,
pubmed-meshheading:9886078-Rats, Wistar,
pubmed-meshheading:9886078-Receptors, Serotonin,
pubmed-meshheading:9886078-Receptors, Serotonin, 5-HT1,
pubmed-meshheading:9886078-Serotonin,
pubmed-meshheading:9886078-Serotonin Receptor Agonists,
pubmed-meshheading:9886078-Spiro Compounds
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pubmed:year |
1999
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pubmed:articleTitle |
Differential regulation of somatodendritic serotonin 5-HT1A receptors by 2-week treatments with the selective agonists alnespirone (S-20499) and 8-hydroxy-2-(Di-n-propylamino)tetralin: microdialysis and autoradiographic studies in rat brain.
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pubmed:affiliation |
Department of Neurochemistry, Instituto de Investigaciones Biomédicas de Barcelona, CSIC, Spain.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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