|
rdf:type |
|
|
lifeskim:mentions |
umls-concept:C0050079,
umls-concept:C0205314,
umls-concept:C0231491,
umls-concept:C0290799,
umls-concept:C0379900,
umls-concept:C0679622,
umls-concept:C0756356,
umls-concept:C0871261,
umls-concept:C1280500,
umls-concept:C1704632,
umls-concept:C1706817,
umls-concept:C2911692
|
|
pubmed:issue |
1
|
|
pubmed:dateCreated |
1998-9-1
|
|
pubmed:abstractText |
The neurochemical profile at both post and presynaptic 5-HT1A receptors of a novel 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) analog, 5-methyl-8-hydroxy-2-(di-n-propylamino)tetralin ¿(+/-)-5-Me-8-OH-DPAT¿ and its stereoisomers was determined and compared to that of the highly selective 5-HT1A receptor antagonist, N-[4-(2-methoxyphenyl)-1-piperazinyl]-N-(2-pyridinyl) cyclo-hexanecarboxamide (WAY 100635). We evaluated their effects on 8-OH-DPAT-induced decrease in cAMP production, on 8-OH-DPAT-induced decrease in rat ventral hippocampal extracellular 5-hydroxytryptamine (5-HText) levels and in body temperature in mice. Both (+/-)- and (-)-5-Me-8-OH-DPAT blocked the 8-OH-DPAT-induced inhibition of forskolin-stimulated cAMP production. Moreover, while having no significant effect when injected alone, (+/-)-, (-)-5-Me-8-OH-DPAT and WAY 100635 antagonized the 8-OH-DPAT-induced decrease in 5-HText in rats and hypothermia in mice. By contrast, the (+) isomer inhibited the cAMP synthesis and did not modify the 8-OH-DPAT response on 5-HText in ventral hippocampus. These data suggest that (+/-)-5-Me-8-OH-DPAT acts selectively, its activity residing in the (-) enantiomer, this latter compound acting similarly to WAY 100635 as a full, selective and silent 5-HT1A antagonist.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/8-Hydroxy-2-(di-n-propylamino)tetral...,
http://linkedlifedata.com/resource/pubmed/chemical/Adenylate Cyclase,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclic AMP,
http://linkedlifedata.com/resource/pubmed/chemical/Forskolin,
http://linkedlifedata.com/resource/pubmed/chemical/Piperazines,
http://linkedlifedata.com/resource/pubmed/chemical/Pyridines,
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 Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Receptor Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/WAY 100635
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Apr
|
|
pubmed:issn |
0014-2999
|
|
pubmed:author |
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
17
|
|
pubmed:volume |
347
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
41-9
|
|
pubmed:dateRevised |
2010-11-18
|
|
pubmed:meshHeading |
pubmed-meshheading:9650846-8-Hydroxy-2-(di-n-propylamino)tetralin,
pubmed-meshheading:9650846-Adenylate Cyclase,
pubmed-meshheading:9650846-Animals,
pubmed-meshheading:9650846-Body Temperature,
pubmed-meshheading:9650846-Cyclic AMP,
pubmed-meshheading:9650846-Drug Interactions,
pubmed-meshheading:9650846-Female,
pubmed-meshheading:9650846-Forskolin,
pubmed-meshheading:9650846-Hippocampus,
pubmed-meshheading:9650846-Male,
pubmed-meshheading:9650846-Mice,
pubmed-meshheading:9650846-Microdialysis,
pubmed-meshheading:9650846-Piperazines,
pubmed-meshheading:9650846-Pyridines,
pubmed-meshheading:9650846-Rats,
pubmed-meshheading:9650846-Rats, Sprague-Dawley,
pubmed-meshheading:9650846-Receptors, Serotonin,
pubmed-meshheading:9650846-Receptors, Serotonin, 5-HT1,
pubmed-meshheading:9650846-Serotonin,
pubmed-meshheading:9650846-Serotonin Antagonists,
pubmed-meshheading:9650846-Serotonin Receptor Agonists,
pubmed-meshheading:9650846-Stereoisomerism,
pubmed-meshheading:9650846-Stimulation, Chemical
|
|
pubmed:year |
1998
|
|
pubmed:articleTitle |
Effects of WAY 100635 and (-)-5-Me-8-OH-DPAT, a novel 5-HT1A receptor antagonist, on 8-OH-DPAT responses.
|
|
pubmed:affiliation |
Lab. Neuropharmacol. JE MESR 92-372, Fac. Pharmacie, Institut de Signalisation et Innovation Thérapeutique, Univ. Paris Sud, Châtenay-Malabry, France. a-c.trillat@cep.u-psud.fr
|
|
pubmed:publicationType |
Journal Article,
Comparative Study
|
