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  • Title: Binding selectivity of short [D-Arg2,Leu5]enkephalin analogues to mu- and delta-subclasses of opiate receptors.
    Author: Rosenthal GF, Inkina NM, Abissova NA, Bobrova IV, Chipens GI.
    Journal: Biomed Sci; 1990 Apr; 1(4):414-6. PubMed ID: 1966782.
    Abstract:
    [D-Arg2,Leu5]enkephalin and its analogues, shortened from the C-terminus, were studied in a rat brain membrane fraction with the aid of radioreceptor analysis. The interaction between these compounds and the peripheral opiate receptors of isolated organs (guinea pig ileum and mouse vas deferens) was also investigated. The ethyl ester of the [D-Arg2]tripeptide retains approximately 10% of the mu-receptor activity of leucine-enkephalin. This implies that for interaction with the mu-subclass of opiate receptors there is no requirement for a second aromatic ring in addition to the tyramine group in the minimal active moiety of the enkephalin molecule.
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