Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Experiment Videos

Structural requirements for delta opioid receptor binding.

H I Mosberg, J R Omnaas, A Goldstein

    Molecular Pharmacology
    |June 1, 1987
    PubMed
    Summary
    This summary is machine-generated.

    Related Concept Videos

    You might also read

    Related Articles

    Articles linked to this work by shared authors, journal, and citation graph.

    Sort by
    Same author

    Efficacy of self-management program associated with a spa therapy for knee osteoarthritis patients (GETT 2): a research protocol for a randomized trial.

    Trials·2023
    Same author

    A bright γ-ray flare interpreted as a giant magnetar flare in NGC 253.

    Nature·2021
    Same author

    Involvement of the Spinal Cord in Primary Mitochondrial Disorders: A Neuroimaging Mimicker of Inflammation and Ischemia in Children.

    AJNR. American journal of neuroradiology·2021
    Same author

    Use of Co<sup>2+</sup>:MgAl<sub>2</sub>O<sub>4</sub> transparent ceramics in passive Q-switching of an Er:Glass laser at 1.534 µm.

    Optics express·2020
    Same author

    The Perirolandic Sign: A Unique Imaging Finding Observed in Association with Polymerase γ-Related Disorders.

    AJNR. American journal of neuroradiology·2020
    Same author

    Prediction-based neural mechanisms for shielding the self from existential threat.

    NeuroImage·2019
    Same journal

    Regulation of organic anion transporting polypeptide 1B1 transport function by lysine deacetylase 6.

    Molecular pharmacology·2026
    Same journal

    Neuroprotective in vitro effects of histone deacetylase 6-selective inhibitor SW-100 toward oxaliplatin-derived toxicity.

    Molecular pharmacology·2026
    Same journal

    Emerging roles of platelet DNA in cancer detection and noninvasive prenatal testing.

    Molecular pharmacology·2026
    Same journal

    Binding affinities for histamine receptors 1 to 4: Systematic comparison of ligands from the Psychoactive Drug Screening Program K<sub>i</sub> database and International Union of Basic and Clinical Pharmacology/British Pharmacological Society Guide to Pharmacology.

    Molecular pharmacology·2026
    Same journal

    Molecular pharmacology of mGlu<sub>7/8</sub> heterodimers reveals unique properties of orthosteric agonists and positive allosteric modulators.

    Molecular pharmacology·2026
    Same journal

    Effects of ivermectin on the activation and desensitization of the human GABA<sub>A</sub> receptor.

    Molecular pharmacology·2026
    See all related articles

    Structural modifications of enkephalin analogs impact opioid receptor binding. Compact conformations are crucial for delta opioid receptor affinity, while bulky residues at position 2 reduce potency at both delta and mu receptors.

    Area of Science:

    • Medicinal Chemistry
    • Neuroscience
    • Pharmacology

    Background:

    • Enkephalins are endogenous opioid peptides that modulate pain and mood.
    • Understanding structure-activity relationships is key to developing novel analgesics.
    • Previous studies focused on cyclic disulfide enkephalin analogs.

    Purpose of the Study:

    • To investigate how structural changes in enkephalin analogs affect opioid receptor binding.
    • To synthesize and evaluate cyclic dithioether and linear enkephalin analogs.
    • To determine the role of conformational flexibility and side-chain bulk in receptor interaction.

    Main Methods:

    • Synthesis of cyclic dithioether and linear enkephalin analogs.
    • Measurement of opioid receptor binding affinities (delta and mu).

    Related Experiment Videos

  • Comparison of binding affinities between different analog series.

    • Main Results:

    • Increasing ring size from disulfide to dithioether significantly decreased delta opioid receptor binding affinity.
    • Compact conformations are necessary for optimal delta opioid receptor binding.
    • Bulky hydrophobic residues at position 2 of linear analogs drastically reduced potency at delta and mu receptors.

    Conclusions:

    • Conformational restriction plays a critical role in enkephalin analog binding to delta opioid receptors.
    • Steric hindrance from bulky residues at position 2 negatively impacts binding to both delta and mu opioid receptors.
    • These findings provide insights for designing more selective and potent opioid-based therapeutics.