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

Receptor blockade and synaptic function.

D M Quastel, P Pennefather

    Journal of Neural Transmission. Supplementum
    |January 1, 1983
    PubMed
    Summary

    Synaptic responses are not always affected by blocking receptors, especially when receptor density is high. Significant receptor blockade is needed to alter synaptic function, challenging simple kinetic models.

    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

    Power of narrative: a case study about documenting private insightful experiences while dealing with pain and associated disability.

    Frontiers in digital health·2024
    Same author

    Bilateral hypopyon following streptokinase treatment for acute myocardial infarction.

    Eye (London, England)·2003
    Same author

    The development and evaluation of a new aerosol irritant assay with minimal animal stress.

    Pulmonary pharmacology & therapeutics·2002
    Same author

    Distinct functional and pharmacological properties of tonic and quantal inhibitory postsynaptic currents mediated by gamma-aminobutyric acid(A) receptors in hippocampal neurons.

    Molecular pharmacology·2001
    Same author

    Pulse oximetry, severe retinopathy, and outcome at one year in babies of less than 28 weeks gestation.

    Archives of disease in childhood. Fetal and neonatal edition·2001
    Same author

    Differential time-course of slow afterhyperpolarizations and associated Ca2+ transients in rat CA1 pyramidal neurons: further dissociation by Ca2+ buffer.

    Neuroscience·1999

    Area of Science:

    • Neuroscience
    • Pharmacology
    • Biophysics

    Background:

    • Neurotransmitter release into synaptic clefts triggers target cell responses and removal systems.
    • Synaptic transmission operates dynamically, not at equilibrium, making equilibrium kinetics unsuitable for predicting system modifications.
    • Receptor blockade and density changes can have complex effects on synaptic function.

    Purpose of the Study:

    • To investigate the impact of receptor blockade and density on synaptic responses.
    • To challenge the application of equilibrium kinetics in predicting synaptic function modifications.
    • To compare the effects of different drug actions on neurotransmitter receptor function.

    Main Methods:

    • Mathematical modeling of subsynaptic response to neurotransmitter quanta.
    • Experimental validation using voltage-clamped mouse neuromuscular junction.
    • Assessment of miniature end-plate current (MEPC) changes under receptor blockade and acetylcholinesterase poisoning.

    Main Results:

    • Mathematical models predicted that subsynaptic responses can be insensitive to competitive receptor blockade or density changes if receptor capture is efficient.
    • Experimental data from mouse neuromuscular junctions confirmed this, requiring ~80% receptor blockade (90% with acetylcholinesterase poisoning) to halve MEPC.
    • Drugs interfering with receptor function (e.g., desensitization, anesthetics) were effective blockers, comparable to or exceeding those preventing acetylcholine binding.

    Conclusions:

    • Extrapolation from receptor number/occupancy data to synaptic function consequences requires caution.
    • Synaptic function is robust to significant receptor loss under normal conditions.
    • Non-specific agents and receptor desensitization highlight complex drug interactions at synapses.

    Related Experiment Videos