Linked Life Data

2707305

Source:http://linkedlifedata.com/resource/pubmed/id/2707305

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
1989-6-2
pubmed:abstractText
The radiolabelled derivative of the potent and selective 5-HT3 receptor antagonist, GR65630, has been shown to label 5-HT3 receptors in homogenates of rat entorhinal cortex. We now report on the specific binding of this radioligand in homogenates of 16 discrete brain areas from several species and nine areas of human brain. We have further characterised specific binding to homogenates of rat area postrema and vagus nerve. In all species examined (rat, mouse, rabbit and ferret) the highest level of specific [3H]GR65630 (0.2 nM) binding was found in homogenates of the area postrema (26-83 fmol/mg protein). Binding in forebrain areas varied with species, Rat and mouse brain had relatively high levels of binding in cortical areas. The ferret and rat had relatively high levels in forebrain dopamine-containing areas. Of the areas of human brain examined the amygdala showed the highest level of specific [3H]GR65630 (0.2 nM) binding (3.0 fmol/mg protein). Specific [3H]GR65630 (0.05-2 nM) binding to homogenates of rat vagus nerve and area postrema was saturable (Bmax: vagus nerve 89.1 fmol/mg protein, area postrema 44.4 fmol/mg protein) and of high affinity (Kd: vagus nerve 0.50 nM, area postrema 0.24 nM). Selective 5-HT3 receptor agonists and antagonists potently inhibited [3H]GR65630 (0.2 nM) binding to homogenates of rat area postrema and vagus nerve. There was a close correlation between drug affinities in each area.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jan
pubmed:issn
0014-2999
pubmed:author
pubmed:issnType
Print
pubmed:day
10
pubmed:volume
159
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
157-64
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1989
pubmed:articleTitle
Binding of the 5-HT3 ligand, [3H]GR65630, to rat area postrema, vagus nerve and the brains of several species.
pubmed:affiliation
Department of Neuropharmacology, Glaxo Group Research Ltd., Ware, Herts, U.K.
pubmed:publicationType
Journal Article, In Vitro