Document Detail

Mu-receptor specificity of the opioid peptide irreversible reagent, [3H]DALECK.
MedLine Citation:
PMID:  3029618     Owner:  NLM     Status:  MEDLINE    
A novel affinity reagent DALECK, i.e. D-Ala2-Leu5-enkephalin with a C-terminal chloromethyl ketone group, was previously synthesized in normal and in tritiated form and shown to react irreversibly at opioid receptors, with some evidence for selectivity for the mu subtype. DALECK tritiated in its phenolic group has been synthesized at 13-fold higher specific radioactivity than in the previous study. In the irreversible reaction of this product at pH 8.1 with rat brain membranes it was confirmed that only one polypeptide there is labelled, of apparent Mr 58,000. Competition between this reaction and ligands highly selective for the mu, delta or kappa binding sites yielded curves demonstrating the very high selectivity of the DALECK irreversible reaction for the mu site. The results provide evidence that the mu opioid receptor protein contains only one type of binding subunit, whose apparent Mr is 58,000, this size being dependent upon the conditions used in the gel electrophoresis and being higher when stringent conditions which would reduce all internal disulphide bonds are applied.
E L Newman; A Borsodi; G Toth; F Hepp; E A Barnard
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Neuropeptides     Volume:  8     ISSN:  0143-4179     ISO Abbreviation:  Neuropeptides     Publication Date:    1986 Nov-Dec
Date Detail:
Created Date:  1987-04-03     Completed Date:  1987-04-03     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  8103156     Medline TA:  Neuropeptides     Country:  SCOTLAND    
Other Details:
Languages:  eng     Pagination:  305-15     Citation Subset:  IM    
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MeSH Terms
Amino Acid Chloromethyl Ketones / metabolism*
Binding, Competitive
Brain / metabolism*
Cell Membrane / metabolism
Macromolecular Substances
Receptors, Opioid / isolation & purification,  metabolism*
Receptors, Opioid, mu
Reg. No./Substance:
0/Amino Acid Chloromethyl Ketones; 0/Macromolecular Substances; 0/Receptors, Opioid; 0/Receptors, Opioid, mu; 10028-17-8/Tritium; 76960-26-4/tyrosyl-alanyl-glycyl-phenylalanyl-leucine chloromethyl ketone

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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