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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
1988-7-27
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pubmed:abstractText |
Phencyclidine (PCP) receptors were successfully solubilized from rat forebrain membranes with 1% sodium cholate. Approximately 58% of the initial protein and 20-30% of the high-affinity PCP binding sites were solubilized. The high affinity toward PCP-like drugs, the stereo-selectivity of the sites, and the sensitivity to N-methyl-D-aspartate (NMDA) receptor ligands were preserved. Binding of the potent PCP receptor ligand N-[3H][1-(2-thienyl)cyclohexyl] piperidine ([3H]TCP) to the soluble receptors was saturable (KD = 35 nM), and PCP-like drugs inhibited [3H]TCP binding in a rank order of potency close to that observed for the membrane-bound receptors; the most potent inhibitors were TCP (Ki = 31 nM) and the anticonvulsant MK-801 (Ki = 50 nM). The NMDA receptor antagonist 2-amino-5-phosphonovaleric acid inhibited binding of [3H]TCP to the soluble receptors; glutamate or NMDA diminished this inhibition in a dose-dependent manner. Taken together, the results indicate that the soluble PCP receptor preparation contains the glutamate recognition sites and may represent a single receptor complex for PCP and NMDA, as suggested by electrophysiological data. The successful solubilization of the PCP receptors in an active binding form should now facilitate their purification.
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pubmed:grant |
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/1-(1-(2-thienyl)cyclohexyl)piperidin...,
http://linkedlifedata.com/resource/pubmed/chemical/2-Amino-5-phosphonovalerate,
http://linkedlifedata.com/resource/pubmed/chemical/Aspartic Acid,
http://linkedlifedata.com/resource/pubmed/chemical/Cholic Acid,
http://linkedlifedata.com/resource/pubmed/chemical/Cholic Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Detergents,
http://linkedlifedata.com/resource/pubmed/chemical/Glutamates,
http://linkedlifedata.com/resource/pubmed/chemical/Glutamic Acid,
http://linkedlifedata.com/resource/pubmed/chemical/N-Methylaspartate,
http://linkedlifedata.com/resource/pubmed/chemical/Phencyclidine,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, N-Methyl-D-Aspartate,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Neurotransmitter,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Phencyclidine,
http://linkedlifedata.com/resource/pubmed/chemical/Valine
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
0022-3042
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
51
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
133-40
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:2898002-2-Amino-5-phosphonovalerate,
pubmed-meshheading:2898002-Animals,
pubmed-meshheading:2898002-Aspartic Acid,
pubmed-meshheading:2898002-Binding, Competitive,
pubmed-meshheading:2898002-Brain Chemistry,
pubmed-meshheading:2898002-Cell Membrane,
pubmed-meshheading:2898002-Cholic Acid,
pubmed-meshheading:2898002-Cholic Acids,
pubmed-meshheading:2898002-Detergents,
pubmed-meshheading:2898002-Glutamates,
pubmed-meshheading:2898002-Glutamic Acid,
pubmed-meshheading:2898002-Male,
pubmed-meshheading:2898002-N-Methylaspartate,
pubmed-meshheading:2898002-Phencyclidine,
pubmed-meshheading:2898002-Rats,
pubmed-meshheading:2898002-Receptors, N-Methyl-D-Aspartate,
pubmed-meshheading:2898002-Receptors, Neurotransmitter,
pubmed-meshheading:2898002-Receptors, Phencyclidine,
pubmed-meshheading:2898002-Solubility,
pubmed-meshheading:2898002-Valine
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pubmed:year |
1988
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pubmed:articleTitle |
Solubilization of rat brain phencyclidine receptors in an active binding form that is sensitive to N-methyl-D-aspartate receptor ligands.
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pubmed:affiliation |
Department of Biochemistry, George S. Wise Faculty of Life Sciences, Tel Aviv University, Israel.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
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