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  • Title: Inhibition of the antisecretory effects of [D-Ala2,D-Leu5]enkephalin in the guinea-pig ileum by a selective delta opioid antagonist.
    Author: Vinayek R, Brown DR, Miller RJ.
    Journal: Eur J Pharmacol; 1983 Oct 14; 94(1-2):159-61. PubMed ID: 6317398.
    Abstract:
    The novel opioid antagonist [diallyl-Tyr1,(CH2)S-Phe4,Leu5]enkephalin (M154,129) was examined for its ability to block the antisecretory effects of [D-Ala2,D-Leu5]enkephalin (DADLE) in isolated mucosal segments of the guinea-pig ileum, actions mediated predominantly through the delta opiate receptor. DADLE reduced transepithelial potential difference and short-circuit current (ED50 18 nM); these effects were competitively antagonized by M154,129 with a Ke value of 746 nM. These results are consistent with others demonstrating M154,129 is a relatively selective although not highly potent blocker of delta opiate receptors.
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