Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
1999-1-21
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.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jan
pubmed:issn
0022-3042
pubmed:author
pubmed:issnType
Print
pubmed:volume
72
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
262-72
pubmed:dateRevised
2010-11-18
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
pubmed:year
1999
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.
pubmed:affiliation
Department of Neurochemistry, Instituto de Investigaciones Biomédicas de Barcelona, CSIC, Spain.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't