• Interaction

    AccNo. 50446 Score 0.49
    Name PM_2875170
    Kd 1.0

    Peptide

    AccNo. 50324
    Name YXXF
    Sequence YXXF
    50324_small
    Internalized no
    Is Motif no

    Interactor

    AccNo. 49946
    Name unknown

    Experiment

    AccNo. 50287
    Classification incorrect?
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    Voting_motivation
    CA CVD DM APO ANG MI BD
    0.70 0.79 0.42 0.49 0.51 0.14 0.89 Vote
    plus plus plus plus plus plus plus Yes
    minus minus minus minus minus minus minus No
    Name PM_2875170
    Detection unspecified method, MI:0686
    Source Pubmed Text Id 2875170
    Journal J Pharmacol Exp Ther. 1986 Sep;238(3):769-72.
    Title Opioid agonist activity of ICI 174864 and its carboxypeptidase degradation product, LY281217.
    Authors Cohen ML, Shuman RT, Osborne JJ, Gesellchen PD
    Text The opioid peptide antagonist, ICI 174864 ([allyl]2-Tyr-alpha-amino-isobutyric acid (Aib)-Aib-Phe-Leu-OH), can produce analgesic effects in mice. The present study explored the possibility that ICI 174864 1) may have affinity and agonist efficacy at mu receptors and/or 2) may form a carboxypeptidase degradation product in vivo that possesses mu agonist activity. In vitro, ICI 174864 (10(-7) to 10(-4) M) inhibited the twitch in the electrically stimulated mouse vas deferens (ED50 = 90 microM) and guinea pig ileum (ED50 greater than 10(-4) M). The in vitro partial agonist activity of ICI 174864 was due to interaction with delta and not mu receptors because the apparent dissociation constant for naloxone using ICI 174864 as the agonist was similar to the apparent dissociation constant for the interaction of naloxone with delta and not mu receptors. Thus, ICI 174864 is a weak partial agonist at delta receptors with little affinity or efficacy at mu receptors. The incubation of ICI 174864 with carboxypeptidase A generated a peptide, LY281217 [(allyl)2-Tyr-Aib-Aib-Phe-OH], which was a more potent agonist in the mouse vas deferens and guinea pig ileum than ICI 174864. The agonist activity of LY281217 was due to interaction with mu and not delta receptors because LY281217 was approximately 100-fold more potent than ICI 174864 as an agonist in the guinea pig ileum, the apparent dissociation constant for naloxone using LY281217 as the agonist was similar to the apparent dissociation constant for the interaction of naloxone with mu receptors and the delta selective antagonist.(ABSTRACT TRUNCATED AT 250 WORDS)
    Mesh Terms Analgesics, Opioid/pharmacology; Animals; Carboxypeptidases/pharmacology; Carboxypeptidases A; Enkephalin, Leucine/analogs & derivatives; Enkephalin, Leucine/pharmacology; Guinea Pigs; Ileum/drug effects; Male; Mice; Mice, Inbred ICR; Naloxone/pharmacology; Narcotic Antagonists/pharmacology; Oligopeptides/pharmacology; Receptors, Opioid/drug effects; Receptors, Opioid, delta; Receptors, Opioid, mu; Vas Deferens/drug effects
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