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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
13
|
pubmed:dateCreated |
1985-5-8
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pubmed:abstractText |
The ability of m-trifluoromethylphenylpiperazine (TFMPP) and an N-substituted derivative, LY 165163 (p-NH2-PE-TFMPP), to discriminate 5-HT-1 binding sites labelled by [3H]5-HT is compared in rat corpus striatum and rat cortex. TFMPP displays at least a 30 fold selectivity for the 5-HT-1b subtype. Furthermore, TFMPP reveals heterogeneity within the 5-HT-1b binding sites. TFMPP displays a Kd of 6 nM for approximately two-thirds of the 5-HT-1b binding sites and a Kd of 273 nM for the remaining one third of the 5-HT-1b sites. p-NH2-PE-TFMPP, on the other hand, discriminates the 5-HT-1 sites in a manner similar to spiperone, displaying a 110 fold selectivity for the 5-HT-1a sites. p-NH2-PE-TFMPP displays a Kd of about 3 nM for the 5-HT-1a sites. p-NH2-PE-TFMPP does not discriminate subtypes within the 5-HT-1b binding sites. The significance of the selectivity of these two compounds as well as structurally related compounds is discussed.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Apr
|
pubmed:issn |
0024-3205
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pubmed:author | |
pubmed:issnType |
Print
|
pubmed:day |
1
|
pubmed:volume |
36
|
pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1265-73
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:3982214-Animals,
pubmed-meshheading:3982214-Binding, Competitive,
pubmed-meshheading:3982214-Binding Sites,
pubmed-meshheading:3982214-Brain,
pubmed-meshheading:3982214-Cerebral Cortex,
pubmed-meshheading:3982214-Corpus Striatum,
pubmed-meshheading:3982214-Male,
pubmed-meshheading:3982214-Piperazines,
pubmed-meshheading:3982214-Rats,
pubmed-meshheading:3982214-Rats, Inbred Strains,
pubmed-meshheading:3982214-Receptors, Serotonin,
pubmed-meshheading:3982214-Spiperone
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pubmed:year |
1985
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pubmed:articleTitle |
5-HT-1a and 5-HT-1b selectivity of two phenylpiperazine derivatives: evidence for 5-HT-1b heterogeneity.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, U.S. Gov't, P.H.S.
|