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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
1988-5-27
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pubmed:abstractText |
The effect of guanine nucleotides and ions on (+)-[3H]3-(3-hydroxyphenyl)-N-(1-propyl)piperidine [+ )-[3H]3-PPP), (+)-N-[3H]allylnormetazocine ((+)-[3H]SKF 10047) and [3H]1-[1-(3-hydroxyphenyl)-cyclohexyl]piperidine ([3H]PCP-3-OH) specific binding to rat brain membranes was examined. These 3 compounds are proposed as prototypical ligands for the labeling of the sigma- and phencyclidine (PCP)-receptor subtypes. Competition binding experiments of (+)-SKF 10047 with (+)-[3H]3-PPP yielded a biphasic inhibition curve which transformed to a monophasic curve when membranes were incubated in the presence of Gpp(NH)p (0.1 mM). The common (+)-[3H]3-PPP/(+)-SKF 10047 binding component is more susceptible to Gpp(NH)p than the high affinity [3H]PCP-3-OH/(+)-SKF 10047 common binding component. Low affinity [3H]PCP-3-OH binding, which may represent a PCP-selective site, is not affected by GTP and Gpp(NH)p. Mono- and divalent cations markedly inhibit high affinity [3H]PCP-3-OH binding but they had a differential inhibitory effect on the binding of the other radioligands tested. These findings suggest differences in the regulation of multiple psychotomimetic (sigma- and PCP) binding sites by guanine nucleotides and ions.
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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-hydroxyphencyclidine,
http://linkedlifedata.com/resource/pubmed/chemical/Cations,
http://linkedlifedata.com/resource/pubmed/chemical/Guanine Nucleotides,
http://linkedlifedata.com/resource/pubmed/chemical/Phenazocine,
http://linkedlifedata.com/resource/pubmed/chemical/Phencyclidine,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Neurotransmitter,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Phencyclidine,
http://linkedlifedata.com/resource/pubmed/chemical/SK&F 10047,
http://linkedlifedata.com/resource/pubmed/chemical/n-N-propyl-3-(3-hydroxyphenyl)piperi...
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0304-3940
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
85
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
147-52
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:2834673-Animals,
pubmed-meshheading:2834673-Binding, Competitive,
pubmed-meshheading:2834673-Brain,
pubmed-meshheading:2834673-Cations,
pubmed-meshheading:2834673-Guanine Nucleotides,
pubmed-meshheading:2834673-Male,
pubmed-meshheading:2834673-Phenazocine,
pubmed-meshheading:2834673-Phencyclidine,
pubmed-meshheading:2834673-Piperidines,
pubmed-meshheading:2834673-Rats,
pubmed-meshheading:2834673-Receptors, Neurotransmitter,
pubmed-meshheading:2834673-Receptors, Phencyclidine,
pubmed-meshheading:2834673-Subcellular Fractions
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pubmed:year |
1988
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pubmed:articleTitle |
Regulation of the binding of sigma- and phencyclidine (PCP)-receptor ligands in rat brain membranes by guanine nucleotides and ions.
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pubmed:affiliation |
Department of Pharmacology, Hadassah School of Medicine, Hebrew University, Jerusalem, Israel.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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