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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
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pubmed:dateCreated |
1993-9-27
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pubmed:abstractText |
High-affinity mu-opioid receptors have been solubilized from 7315c cell membranes. Occupancy of the membrane-associated receptors with morphine before their solubilization in the detergent 3-[(3-cholamidopropyl) dimethyl]-1-propane sulfonate was critical for stabilization of the receptor. The solubilized opioid receptor bound [3H]-etorphine with high affinity (KD = 0.304 +/- 0.06 nM; Bmax = 154 +/- 33 fmol/mg of protein). Of the membrane-associated [3H]etorphine binding sites, 40 +/- 5% were recovered in the solubilized fraction. Both mu-selective and non-selective enkephalins competed with [3H]etorphine for the solubilized binding sites; in contrast, delta- and kappa-opioid enkephalins failed to compete with [3H]etorphine for the solubilized binding sites at concentrations of < 1 microM. The mu-selective ligand [3H][D-Ala2,N-Me-Phe4,Gly5-ol]enkephalin also bound with high affinity (KD = 0.79 nM; Bmax = 108 +/- 17 fmol/mg of protein) to the solubilized material. Of the membrane-associated [3H][D-Ala2,N-Me-Phe4,Gly5-ol]-enkephalin binding sites, 43 +/- 3% were recovered in the solubilized material. Guanosine 5'-O-(3-thiotriphosphate), GTP, and guanosine 5'-O-(2-thiodiphosphate), but not adenylylimidodiphosphate, diminished [3H][D-Ala2,N-Me-Phe4,Gly5-ol] enkephalin binding in a concentration-dependent manner. Finally, mu-opioid receptors from rat brain membranes were also solubilized in a high-affinity, guanine nucleotide-sensitive state if membrane-associated receptors were occupied with morphine before and during their solubilization with the detergent 3-[(3-cholamidopropyl)dimethyl]-1-propane sulfonate.
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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-((3-cholamidopropyl)dimethylammoni...,
http://linkedlifedata.com/resource/pubmed/chemical/Cholic Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Detergents,
http://linkedlifedata.com/resource/pubmed/chemical/Enkephalin, Ala(2)-MePhe(4)-Gly(5)-,
http://linkedlifedata.com/resource/pubmed/chemical/Enkephalins,
http://linkedlifedata.com/resource/pubmed/chemical/Etorphine,
http://linkedlifedata.com/resource/pubmed/chemical/Guanine Nucleotides,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, mu
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0022-3042
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
61
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
973-8
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:8395567-Animals,
pubmed-meshheading:8395567-Binding, Competitive,
pubmed-meshheading:8395567-Binding Sites,
pubmed-meshheading:8395567-Brain,
pubmed-meshheading:8395567-Cell Membrane,
pubmed-meshheading:8395567-Cholic Acids,
pubmed-meshheading:8395567-Detergents,
pubmed-meshheading:8395567-Enkephalin, Ala(2)-MePhe(4)-Gly(5)-,
pubmed-meshheading:8395567-Enkephalins,
pubmed-meshheading:8395567-Etorphine,
pubmed-meshheading:8395567-Guanine Nucleotides,
pubmed-meshheading:8395567-Rats,
pubmed-meshheading:8395567-Receptors, Opioid, mu,
pubmed-meshheading:8395567-Solubility
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pubmed:year |
1993
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pubmed:articleTitle |
Solubilization of high-affinity, guanine nucleotide-sensitive mu-opioid receptors from 7315c cell membranes.
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pubmed:affiliation |
Department of Pharmacology, Uniformed Services University of the Health Sciences, Bethesda, Maryland 20814-4799.
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pubmed:publicationType |
Journal Article
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