Linked Life Data

17178132

Source:http://linkedlifedata.com/resource/pubmed/id/17178132

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3
pubmed:dateCreated
2007-2-16
pubmed:abstractText
Cloned, human dopamine D(1) receptors recruit multiple effectors but the G-protein subtype(s) activated by cerebral populations remain poorly defined, a question addressed using a rapid immunocapture technique. In rat striatum, dopamine (DA) and four selective, benzazepine agonists at D(1) receptors concentration-dependently enhanced [(35)S]GTPgammaS binding to Galphas/olf. For all drugs, Galphaq was also recruited with similar potencies and efficacies. Comparable observations were made in the cortex wherein profiles of Galphas/olf vs Galphaq activation were also highly correlated. In contrast to Galphas/olf and Galphaq, Galphao and Galphai were activated neither in the striatum nor in the cortex, except for SKF82958. As compared to DA, both SKF81297 and SKF82958 were full agonists at Gs/olf and Gq in cortex and striatum, whereas SKF38393 behaved as a partial agonist. Likewise, the "atypical" agonist, SKF83959 only partially activated Galphaq and also Gs/olf in these two regions. In both striatum and cortex, the selective D(1) receptor antagonist, SCH23390, abolished the recruitment of Galphaq and Galphas by DA, and the action of DA was partially attenuated by SKF83959. These findings demonstrate that, in native CNS tissue, DA and other D(1) receptor agonists activate Galphas and Galphaq with similar potencies and efficacies, suggesting their recruitment via pharmacologically-indistinguishable populations of D(1) receptors, and show that SPA technology is well-adapted to study the coupling of native DA receptors.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Mar
pubmed:issn
0028-3908
pubmed:author
pubmed:issnType
Print
pubmed:volume
52
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1003-14
pubmed:dateRevised
2011-11-17
pubmed:meshHeading
pubmed-meshheading:17178132-Animals, pubmed-meshheading:17178132-Antibodies, pubmed-meshheading:17178132-Antibody Specificity, pubmed-meshheading:17178132-Benzazepines, pubmed-meshheading:17178132-Binding, Competitive, pubmed-meshheading:17178132-Binding Sites, Antibody, pubmed-meshheading:17178132-Cerebral Cortex, pubmed-meshheading:17178132-Corpus Striatum, pubmed-meshheading:17178132-Dopamine Agonists, pubmed-meshheading:17178132-Dopamine Antagonists, pubmed-meshheading:17178132-Dose-Response Relationship, Drug, pubmed-meshheading:17178132-Drug Interactions, pubmed-meshheading:17178132-GTP-Binding Protein alpha Subunits, Gq-G11, pubmed-meshheading:17178132-GTP-Binding Protein alpha Subunits, Gs, pubmed-meshheading:17178132-Guanosine 5'-O-(3-Thiotriphosphate), pubmed-meshheading:17178132-Radioligand Assay, pubmed-meshheading:17178132-Rats, pubmed-meshheading:17178132-Receptors, Dopamine D1
pubmed:year
2007
pubmed:articleTitle
Dopamine D1 receptor coupling to Gs/olf and Gq in rat striatum and cortex: a scintillation proximity assay (SPA)/antibody-capture characterization of benzazepine agonists.
pubmed:affiliation
Institut de Recherche Servier, Psychopharmacology Department, 125, chemin de Ronde, 78290 Croissy sur Seine, France. clotilde.mannourylacour@fr.netgrs.com
pubmed:publicationType
Journal Article