Linked Life Data

9225292

Source:http://linkedlifedata.com/resource/pubmed/id/9225292

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4-5
pubmed:dateCreated
1997-9-15
pubmed:abstractText
The effects of a range of phenothiazines were examined on 5-hydroxytryptamine3 (5-HT3) receptors in membranes from NIE-115 neuroblastoma cells using radioligand binding. Chlorpromazine, fluphenazine, perphenazine, trifluoperazine and prochlorperazine inhibited specific binding of both the 5-HT3 receptor antagonist [3H]GR65630 and agonist [3H]meta-chlorophenylbiguanide (mCPBG), with Ki values ranging from 0.4 to 3.9 microM. The mode of action of chlorpromazine was further examined using photoaffinity labelling in the presence and absence of 5-HT. Saturation radioligand binding data with both [3H]GR65630 and [3H]mCPBG showed that photoaffinity labelling with chlorpromazine (1 microM) caused a decrease in the maximum number of binding sites observed (35% and 28% for agonist and antagonist, respectively). This decrease was not observed when the membranes were incubated in the presence of 5-HT. The results demonstrate a direct interaction of a range of phenothiazines at the 5-HT3 receptor binding site.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
0028-3908
pubmed:author
pubmed:issnType
Print
pubmed:volume
36
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
665-70
pubmed:dateRevised
2010-11-18
pubmed:meshHeading
pubmed:articleTitle
Radioligand binding and photoaffinity labelling studies show a direct interaction of phenothiazines at 5-HT3 receptors.
pubmed:affiliation
Neurobiology Division, MRC Laboratory of Molecular Biology, Cambridge, U.K.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't