Document Detail


Characterization of [3H]naltrindole binding to delta opioid receptors in rat brain.
MedLine Citation:
PMID:  1313133     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
[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.
Authors:
M S Yamamura; R Horvath; G Toth; F Otvos; E Malatynska; R J Knapp; F Porreca; V J Hruby; H I Yamamura
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Life sciences     Volume:  50     ISSN:  0024-3205     ISO Abbreviation:  Life Sci.     Publication Date:  1992  
Date Detail:
Created Date:  1992-04-29     Completed Date:  1992-04-29     Revised Date:  2007-11-14    
Medline Journal Info:
Nlm Unique ID:  0375521     Medline TA:  Life Sci     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  PL119-24     Citation Subset:  IM    
Affiliation:
Department of Pharmacology, University of Arizona, College of Medicine, Tucson 85724.
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MeSH Terms
Descriptor/Qualifier:
Animals
Binding, Competitive
Brain / metabolism*
Indoles / metabolism*
Male
Membranes / metabolism
Morphinans / metabolism*
Naltrexone* / analogs & derivatives*
Rats
Rats, Inbred Strains
Receptors, Opioid / metabolism*
Receptors, Opioid, delta
Grant Support
ID/Acronym/Agency:
DA 06284/DA/NIDA NIH HHS; NS 19972/NS/NINDS NIH HHS; T35HI07479/HI/NHLBI NIH HHS
Chemical
Reg. No./Substance:
0/Indoles; 0/Morphinans; 0/Receptors, Opioid; 0/Receptors, Opioid, delta; 111555-53-4/naltrindole; 16590-41-3/Naltrexone

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