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Predicate | Object |
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rdf:type | |
lifeskim:mentions |
umls-concept:C0019564,
umls-concept:C0030685,
umls-concept:C0034693,
umls-concept:C0034721,
umls-concept:C0036751,
umls-concept:C0073661,
umls-concept:C0110907,
umls-concept:C0243192,
umls-concept:C0391871,
umls-concept:C0535025,
umls-concept:C0680255,
umls-concept:C1283071,
umls-concept:C1515655,
umls-concept:C1707455,
umls-concept:C1963578
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pubmed:issue |
3
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pubmed:dateCreated |
1992-4-15
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pubmed:abstractText |
We have compared the ability of the new putatively specific 5-HT1B receptor agonist CP-93,129 (3-(1,2,5,6-tetrahydropyrid-4-yl)pyrrolo[3,2-b] pyrid-5-one) and the structurally related mixed 5-HT1A/5-HT1B receptor ligand RU 24969, to influence 5-HT release in brain in vivo, using microdialysis techniques in chloral hydrate-anaesthetised rats. CP-93,129 (3 or 10 microM, via the dialysis perfusion medium) caused a concentration-dependent and methiothepin (10 microM)-sensitive suppression of ventral hippocampal 5-HT output. The effect of RU 24969 on 5-HT output was dependent on whether or not the 5-HT reuptake blocker citalopram was present in the perfusion medium. Thus, RU 24969 (0.1 microM) induced a decrease, or an increase followed by a decrease (1 microM), in 5-HT output in the absence of citalopram, but monotonically decreased (1 microM) 5-HT release when citalopram (1 microM) was present. CP-93,129 decreased dialysate 5-HT in either condition. Our findings are consistent with the characterisation of CP-93,129 as a 5-HT1B receptor agonist, and may thus represent in vivo support for 5-HT1B autoreceptor-mediated feedback control of 5-HT release in the rat brain. The 5-HT1B selectivity of CP-93,129, and its lack of 5-HT reuptake blocking properties, suggests that the compound compares favourably with other purported 5-HT1B receptor agonists.
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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/3-(1,2,5,6-tetrahydropyrid-4-yl)pyrr...,
http://linkedlifedata.com/resource/pubmed/chemical/5-methoxy...,
http://linkedlifedata.com/resource/pubmed/chemical/Citalopram,
http://linkedlifedata.com/resource/pubmed/chemical/Indoles,
http://linkedlifedata.com/resource/pubmed/chemical/Methiothepin,
http://linkedlifedata.com/resource/pubmed/chemical/Pyridines,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrroles,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
0014-2999
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
17
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pubmed:volume |
209
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
249-52
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:1797566-Animals,
pubmed-meshheading:1797566-Brain Chemistry,
pubmed-meshheading:1797566-Citalopram,
pubmed-meshheading:1797566-Dialysis,
pubmed-meshheading:1797566-Hippocampus,
pubmed-meshheading:1797566-Indoles,
pubmed-meshheading:1797566-Male,
pubmed-meshheading:1797566-Methiothepin,
pubmed-meshheading:1797566-Pyridines,
pubmed-meshheading:1797566-Pyrroles,
pubmed-meshheading:1797566-Rats,
pubmed-meshheading:1797566-Rats, Inbred Strains,
pubmed-meshheading:1797566-Receptors, Serotonin,
pubmed-meshheading:1797566-Serotonin
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pubmed:year |
1991
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pubmed:articleTitle |
The putative 5-HT1B receptor agonist CP-93,129 suppresses rat hippocampal 5-HT release in vivo: comparison with RU 24969.
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pubmed:affiliation |
Department of Pharmacology, University of Göteborg, Sweden.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
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