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

GABA agonists. Development and interactions with the GABA receptor complex.

P Krogsgaard-Larsen, E Falch

    Molecular and Cellular Biochemistry
    |August 11, 1981
    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 orthosteric GABAA receptor ligand Thio-4-PIOL displays distinctly different functional properties at synaptic and extrasynaptic receptors.

    British journal of pharmacology·2013
    Same author

    Lack of a high affinity uptake system for the GABA agonists THIP and isoguvacine in neurons and astrocytes cultured from mouse brain.

    Neurochemistry international·2010
    Same author

    Characterization of the uptake of GABA, nipecotic acid and cis-4-OH-nipecotic acid in cultured neurons and astrocytes.

    Neurochemistry international·2010
    Same author

    Multi-component analysis of marine lipids in fish gonads with emphasis on phospholipids using high resolution NMR spectroscopy.

    Chemistry and physics of lipids·2006
    Same author

    Modification of the philanthotoxin-343 polyamine moiety results in different structure-activity profiles at muscle nicotinic ACh, NMDA and AMPA receptors.

    Neuropharmacology·2003
    Same author

    Recent advances in the medicinal chemistry of polyamine toxins.

    Mini reviews in medicinal chemistry·2002
    Same journal

    PER1 reduces HIF-1α nuclear accumulation and modulates vascular remodeling in hepatocellular carcinoma.

    Molecular and cellular biochemistry·2026
    Same journal

    FCGR2A promoter variant reveals shared genetic susceptibility between IBD and stroke.

    Molecular and cellular biochemistry·2026
    Same journal

    Chlamydia psittaci induces GSDME-mediated pyroptosis via the ROS-JNK signaling pathway.

    Molecular and cellular biochemistry·2026
    Same journal

    Pentraxin 3 is an inflammation-related biomarker that distinguishes early-stage from mid-advanced cardiovascular-kidney-metabolic syndrome.

    Molecular and cellular biochemistry·2026
    Same journal

    High glucose-induced mitochondrial fission promotes Müller cell activation via suppression of the Hippo pathway.

    Molecular and cellular biochemistry·2026
    Same journal

    Correction to: Estradiol inhibits vascular endothelial cells pro-inflammatory activation induced by C-reactive protein.

    Molecular and cellular biochemistry·2026
    See all related articles

    Researchers developed specific GABA receptor agonists, like THIP, by modifying muscimol. These compounds offer improved safety and brain penetration, advancing GABAergic synapse research.

    Area of Science:

    • Neuroscience
    • Pharmacology
    • Medicinal Chemistry

    Background:

    • GABA (gamma-aminobutyric acid) is the primary inhibitory neurotransmitter in the central nervous system.
    • Developing specific GABA receptor agonists is crucial for understanding GABAergic neurotransmission and for therapeutic applications.
    • Muscimol is a potent but non-specific GABA agonist, necessitating the development of more selective compounds.

    Purpose of the Study:

    • To review the development of highly specific GABA receptor agonists.
    • To discuss structural parameters essential for designing effective GABA agonists.
    • To explore the interaction of these agonists with the GABA receptor complex, including the benzodiazepine binding site.

    Main Methods:

    • Extensive structural modifications of muscimol to create novel GABA agonists.

    Related Experiment Videos

  • Evaluation of the biological activity and receptor affinity of synthesized compounds.
  • Analysis of structure-activity relationships and pharmacokinetic properties.

    • Main Results:

    • Identification of specific GABA agonists such as THIP, isoguvacine, and piperidine-4-sulphonic acid (P4S).
    • Demonstration that molecular rigidity (e.g., THIP) activates GABA receptors, while conformational mobility is key for stimulating diazepam binding.
    • THIP exhibits favorable toxicological profiles and brain penetration compared to muscimol and isoguvacine.

    Conclusions:

    • Specific GABA agonists can be rationally designed through structural modifications.
    • GABA receptor function involves conformational changes, influencing agonist interactions.
    • THIP represents a well-tolerated, brain-penetrant GABA agonist with potential therapeutic applications.