Document Detail

Allosteric modulation by leucine-enkephalin of [3H]naloxone binding in rat brain.
MedLine Citation:
PMID:  6268425     Owner:  NLM     Status:  MEDLINE    
The interaction of morphine and leucine-enkephalin with the binding site labeled by [3H]naloxone in the presence of sodium was compared. The effect of fixed concentrations of morphine and leucine enkephalin on the saturation binding of [3H]naloxone demonstrated that whereas morphine was a competitive inhibitor, leucine enkephalin caused a dose-dependent masking of binding sites. From these data we conclude that the enkephalin receptor is allosterically coupled to the morphine receptor.
R B Rothman; T C Westfall
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Publication Detail:
Type:  In Vitro; Journal Article; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  European journal of pharmacology     Volume:  72     ISSN:  0014-2999     ISO Abbreviation:  Eur. J. Pharmacol.     Publication Date:  1981 Jul 
Date Detail:
Created Date:  1981-11-22     Completed Date:  1981-11-22     Revised Date:  2007-11-14    
Medline Journal Info:
Nlm Unique ID:  1254354     Medline TA:  Eur J Pharmacol     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  365-8     Citation Subset:  IM    
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MeSH Terms
Allosteric Site / drug effects
Binding, Competitive
Brain / metabolism*
Endorphins / metabolism*
Enkephalin, Leucine
Enkephalins / metabolism*
Naloxone / metabolism*
Rats, Inbred Strains
Receptors, Opioid / metabolism*
Grant Support
02668//PHS HHS; 12615//PHS HHS
Reg. No./Substance:
0/Endorphins; 0/Enkephalins; 0/Receptors, Opioid; 465-65-6/Naloxone; 58822-25-6/Enkephalin, Leucine

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