Related Experiment Video

Updated: Dec 12, 2025

Identification and Classification of Position-specific GABAA Receptor Subunit Missense Variants for Their Role In Hippocampal Pyramidal Neurons
08:04

Identification and Classification of Position-specific GABAA Receptor Subunit Missense Variants for Their Role In Hippocampal Pyramidal Neurons

Published on: June 6, 2025

1.1K

Contingency between Historical Substitutions in the Acetylcholine Receptor Pore

Johnathon R Emlaw, Kelly M Burkett, Corrie J B daCosta

    ACS Chemical Neuroscience
    |August 14, 2020
    PubMed
    Summary

    Reconstructed ancestral acetylcholine receptors show reduced conductance due to specific amino acid changes. The order of these evolutionary substitutions critically impacts channel function, revealing history-dependent protein evolution.

    Keywords:
    Ion channelancestral reconstructioncys-loop receptorhistorical contingencynicotinic acetylcholine receptorpatch clamppentameric ligand-gated ion channelprotein evolutionsingle-molecule biophysics

    More Related Videos

    Using an α-Bungarotoxin Binding Site Tag to Study GABA A Receptor Membrane Localization and Trafficking11:57

    Using an α-Bungarotoxin Binding Site Tag to Study GABA A Receptor Membrane Localization and Trafficking

    Published on: March 28, 2014

    16.2K
    Measuring Nucleotide Binding to Intact, Functional Membrane Proteins in Real Time08:33

    Measuring Nucleotide Binding to Intact, Functional Membrane Proteins in Real Time

    Published on: March 11, 2021

    2.2K

    Related Concept Videos

    Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:29

    Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

    Indirect-acting cholinergic agonists are agents that interact with the acetylcholinesterase enzyme in the synaptic cleft, preventing the breakdown of acetylcholine into choline and acetate. Consequently, the concentration of acetylcholine in the synaptic cleft increases. These agonists can be classified into reversible and irreversible inhibitors based on their duration of action.
    Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
    807
    Ligand-Gated Ion Channel Receptor: Gating Mechanism01:30

    Ligand-Gated Ion Channel Receptor: Gating Mechanism

    Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
    3.5K
    Indirect-Acting Cholinergic Agonists: Mechanism of Action01:18

    Indirect-Acting Cholinergic Agonists: Mechanism of Action

    Indirect-acting cholinergic agonists work by interacting with an enzyme called acetylcholinesterase (AChE) in the synaptic cleft. They can be reversible or irreversible inhibitors and have different effects on the enzyme.
    Reversible inhibitors like edrophonium bind to a specific part of the enzyme called the anionic catalytic site. They form noncovalent bonds, which means they are not strongly attached to the enzyme. This creates a temporary and less stable enzyme–inhibitor complex,...
    2.4K
    Cholinergic Receptors: Nicotinic01:15

    Cholinergic Receptors: Nicotinic

    Nicotinic receptors are ligand-gated ion channels that are activated by acetylcholine and nicotine. Upon activation, they cause a rapid increase in the permeability of cells to K+, Na+, and Ca2+, followed by depolarization and excitation. They are in the autonomic ganglia, skeletal neuromuscular junction, CNS, and adrenal medulla.
    There are two types of nicotinic receptors: neuromuscular (NM/NM/N1) and neuronal (NN/NN/N2). The two families differ based on their location and selectivity to...
    4.9K
    Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:22

    Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

    Cholinergic agonists or cholinomimetics mimic the action of acetylcholine to stimulate the parasympathetic nervous system. They are categorized into direct-acting and indirect-acting agents. The direct-acting cholinergic drugs induce the parasympathetic response by directly binding to the muscarinic or nicotine receptors. In comparison, the indirect-acting cholinergic drugs prevent acetylcholine hydrolysis, indirectly contributing to the extended parasympathetic response.
    The direct-acting...
    1.8K
    Cholinergic Receptors: Muscarinic01:25

    Cholinergic Receptors: Muscarinic

    The pharmacological actions of acetylcholine are elicited via its binding to two families of cholinergic receptors or cholinoceptors, namely, muscarinic and nicotinic receptors. Muscarinic receptors are G protein-coupled receptors and have five subtypes, M1–M5. All mAChR subtypes are activated by acetylcholine and blocked by the antagonist, atropine. 
    The subtypes M1, M3, and M5 couple with the Gq subunit and activate the phospholipase C (PLC) activity, mobilizing intracellular Ca2+....
    4.4K