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

Epibatidine structure-activity relationships.

F Ivy Carroll1

  • 1Organic and Medicinal Chemistry, Research Triangle Institute, Research Triangle Park, NC 27709, USA. fic@rti.org

Bioorganic & Medicinal Chemistry Letters
|March 31, 2004
PubMed
Summary

Researchers reviewed structure-activity relationship (SAR) studies of epibatidine analogues, which are potent nicotinic acetylcholine receptor (nAChR) agonists. Few analogues have undergone in vitro or in vivo evaluation, highlighting a gap in understanding their pharmacological potential.

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

Cognitive-Enhancing Effects of Acetylcholine Receptor Agonists in Group-Housed Cynomolgus Monkeys Who Drink Ethanol.

The Journal of pharmacology and experimental therapeutics·2023
Same author

Molecular mechanism of biased signaling at the kappa opioid receptor.

Nature communications·2023
Same author

Rate of onset of dopamine transporter inhibitors assessed with intracranial self-stimulation and in vivo dopamine photometry in rats.

Psychopharmacology·2023
Same author

Pharmacological characterization of 5-iodo-A-85380, a β2-selective nicotinic receptor agonist, in mice.

Journal of psychopharmacology (Oxford, England)·2022
Same author

Blood levels of T-Cell Receptor Excision Circles (TRECs) provide an index of exposure to traumatic stress in mice and humans.

Translational psychiatry·2022
Same author

Interactions between 2'-fluoro-(carbamoylpyridinyl)deschloroepibatidine analogues and acetylcholine-binding protein inform on potent antagonist activity against nicotinic receptors.

Acta crystallographica. Section D, Structural biology·2022

Area of Science:

  • Pharmacology
  • Medicinal Chemistry
  • Neuroscience

Background:

  • Epibatidine is a powerful, nonselective agonist of nicotinic acetylcholine receptors (nAChRs).
  • The alpha4beta2 subtype of nAChRs is believed to mediate most of epibatidine's biological effects.
  • A limited number of epibatidine analogues have been synthesized and tested, with even fewer undergoing in vivo pharmacological assessment.

Purpose of the Study:

  • To review existing structure-activity relationship (SAR) studies focused on epibatidine analogues.
  • To consolidate current knowledge on the synthesis and evaluation of epibatidine derivatives.
  • To identify gaps in the pharmacological investigation of epibatidine analogues.

Main Methods:

  • Review of published literature on epibatidine analogues.

Related Experiment Videos

  • Analysis of structure-activity relationship data from in vitro assays.
  • Examination of in vivo pharmacological evaluation data for synthesized analogues.

    • Main Results:

    • A limited number of epibatidine analogues have been synthesized and characterized.
    • In vitro and in vivo pharmacological data for these analogues are scarce.
    • SAR studies provide insights into the structural requirements for nAChR interaction.

    Conclusions:

    • There is a significant need for expanded synthesis and evaluation of epibatidine analogues.
    • Further research is required to fully elucidate the pharmacological profiles and therapeutic potential of epibatidine derivatives.
    • Comprehensive SAR studies are crucial for developing selective nAChR modulators.