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

Specific kappa opioid receptor agonists.

G Ronsisvalle1, A Marrazzo, L Pasquinucci

  • 1Department of Pharmaceutical Sciences, University of Catania, Italy. ggrmedch@mbox.unict.it

Farmaco (Societa Chimica Italiana : 1989)
|May 12, 2001
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

The simultaneous activation of μ- and δ-opioid receptors by (-)-2<i>S</i>-LP2 rescues allodynia with the contribution of TGF-β1 signaling in a rat chronic constriction injury model.

Current research in pharmacology and drug discovery·2025
Same author

Simultaneous Ipsilateral Vascularized Lymph Node Transplantation and Contralateral Lymphovenous Anastomosis in Bilateral Extremity Lymphedema with Different Severities.

Annals of surgical oncology·2020
Same author

Bulk and Surface Electronic Structure of the Dual-Topology Semimetal Pt_{2}HgSe_{3}.

Physical review letters·2020
Same author

Many-body perturbation theory calculations using the yambo code.

Journal of physics. Condensed matter : an Institute of Physics journal·2019
Same author

(+)-and (-)-Phenazocine enantiomers: Evaluation of their dual opioid agonist/σ<sub>1</sub> antagonist properties and antinociceptive effects.

European journal of medicinal chemistry·2016
Same author

Caspase-3 activation in human melanoma A375 cell line by a novel selective sigma-2 agonist.

Die Pharmazie·2016
Same journal

Chemical and biochemical transformations of 5-ethoxycarbonyl-5-phenyl-2-isoxazolines.

Farmaco (Societa chimica italiana : 1989)·2005
Same journal

Nasal administration of heparin-loaded microspheres based on poly(lactic acid).

Farmaco (Societa chimica italiana : 1989)·2005
Same journal

New 8-substituted xanthiene derivatives as potent bronchodilators.

Farmaco (Societa chimica italiana : 1989)·2005
Same journal

In situ and in vivo efficacy of peroral absorption enhancers in rats and correlation to in vitro mechanistic studies.

Farmaco (Societa chimica italiana : 1989)·2005
Same journal

Synthesis of 3-aryl-5-decapentyl-1,2,4-oxadiazoles possessing antiinflammatory and antitumor properties.

Farmaco (Societa chimica italiana : 1989)·2005
Same journal

Syntheses, in vitro antibacterial and antifungal activities of a series of N-alkyl, 1,4-dithiines.

Farmaco (Societa chimica italiana : 1989)·2005
See all related articles

Researchers designed novel heterocyclic scaffolds for the dynorphin A pharmacophore, revealing structure-affinity relationships. These ligands offer insights into benzomorphan derivatives binding to the kappa opioid receptor.

Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Neuroscience

Background:

  • The dynorphin A peptide system and its target, the kappa opioid receptor (KOR), are implicated in pain and mood disorders.
  • Benzomorphan derivatives are a known class of KOR ligands, but their precise binding modes require further elucidation.
  • Developing selective KOR modulators is a therapeutic goal for various neurological conditions.

Purpose of the Study:

  • To design novel heterocyclic scaffolds that mimic the dynorphin A pharmacophore.
  • To investigate structure-affinity relationships within the MPCB/CCB series of ligands.
  • To gain insights into the binding interactions of benzomorphan derivatives with the kappa opioid receptor.

Main Methods:

  • Synthesis of a novel series of heterocyclic compounds.

Related Experiment Videos

  • Structure-activity relationship (SAR) studies to determine ligand affinity.
  • Molecular modeling or docking studies to predict binding modes (implied).

    • Main Results:

    • Successful design and synthesis of heterocyclic scaffolds targeting the dynorphin A pharmacophore.
    • Identification of key structural features governing affinity for the kappa opioid receptor within the MPCB/CCB series.
    • Representative ligands demonstrated specific binding interactions, providing insights into benzomorphan derivative binding modes.

    Conclusions:

    • The developed heterocyclic scaffolds represent promising starting points for novel kappa opioid receptor ligands.
    • Understanding structure-affinity relationships is crucial for optimizing benzomorphan derivatives for therapeutic applications.
    • These findings contribute to the knowledge of ligand-receptor interactions at the kappa opioid receptor.