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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
16
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pubmed:dateCreated |
1992-4-29
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pubmed:abstractText |
[3H]Naltrindole binding characteristics were determined using homogenized rat brain tissue. Saturation binding studies at 25 degrees C measured an equilibrium dissociation constant (Kd) value of 37.0 +/- 3.0 pM and a receptor density (Bmax) value of 63.4 +/- 2.0 fmol/mg protein. Association binding studies showed that equilibrium was reached within 90 min at a radioligand concentration of 30 pM. Naltrindole, as well as the ligands selective for delta (delta) opioid receptors, such as pCI-DPDPE and Deltorphin II inhibited [3H]naltrindole binding with nanomolar IC50 values. Ligands selective for mu (mu) and kappa (kappa) opioid receptors were only effective in inhibiting [3H]naltrindole binding at micromolar concentrations. From these data, we conclude that [3H]naltrindole is a high affinity, selective radioligand for delta opioid receptors.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Indoles,
http://linkedlifedata.com/resource/pubmed/chemical/Morphinans,
http://linkedlifedata.com/resource/pubmed/chemical/Naltrexone,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, delta,
http://linkedlifedata.com/resource/pubmed/chemical/naltrindole
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pubmed:status |
MEDLINE
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pubmed:issn |
0024-3205
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
50
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
PL119-24
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:1313133-Animals,
pubmed-meshheading:1313133-Binding, Competitive,
pubmed-meshheading:1313133-Brain,
pubmed-meshheading:1313133-Indoles,
pubmed-meshheading:1313133-Male,
pubmed-meshheading:1313133-Membranes,
pubmed-meshheading:1313133-Morphinans,
pubmed-meshheading:1313133-Naltrexone,
pubmed-meshheading:1313133-Rats,
pubmed-meshheading:1313133-Rats, Inbred Strains,
pubmed-meshheading:1313133-Receptors, Opioid,
pubmed-meshheading:1313133-Receptors, Opioid, delta
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pubmed:year |
1992
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pubmed:articleTitle |
Characterization of [3H]naltrindole binding to delta opioid receptors in rat brain.
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pubmed:affiliation |
Department of Pharmacology, University of Arizona, College of Medicine, Tucson 85724.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
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