Ligand Gated Ion Channel Assays
Ligand gated ion channels are a class of transmembrane ion channel proteins that open in response to the binding of a chemical messenger, such as a neurotransmitter, allowing ions such as Na+, K+, Ca2+, and Cl- to pass through the membrane. These receptor proteins usually have at least two domains: a transmembrane domain that contains the ion pore and an extracellular domain that contains the ligand binding site.
Creative Biolabs offers ligand gated ion channel assays to identify active compounds for ion channel targets. Ligand gated ion channels have a role in a wide range of physiological processes, and they are both attractive therapeutic targets and significant off-targets for in vitro pharmacological profiling.
| Classification | Function | Subunits |
|---|---|---|
| GABAA Assays | The majority of GABA's physiological functions in the central nervous system are mediated by GABAA receptors. The presence of an α and a β subunit is the bare minimum for producing a GABA-gated ion channel. |
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| Glutamate Receptor Assays | Glutamate receptors are critical participants in synaptic plasticity, which is important for learning and memory, and mediate the bulk of excitatory synaptic transmission throughout the central nervous system. |
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| Acetylcholine Nicotinic Channel Assays | Many species have Acetylcholine Nicotinic Channels in their central and peripheral nervous systems, muscles, and other tissues. |
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| Glycine Receptor Assays | The glycine receptor is involved in several physiological functions, including modulating inhibitory neurotransmission in the spinal cord and brainstem. |
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| GluR6 Assays | Synaptic plasticity, learning, and memory may all be affected by this receptor. It may also play a role in visual information transfer from the retina to the hypothalamus. | |
| 5HT3A Assays | This receptor causes fast, depolarizing responses in neurons after activation. |
Pharmacology
Ligand-gated ion channels are thought to be the primary site where anaesthetic drugs and ethanol exert their effects. Anaesthetic drugs, in particular, impact the GABA and NMDA receptors at doses similar to those employed in clinical anaesthesia.
Structure
Ligand gated ion channels are multisubunit (4 or 5 subunits) receptors that produce a membrane ion channel that permits Na+, K+, Ca2+, or Cl- to flow through when open. Each subunit usually has four hydrophobic transmembrane domains connected by hydrophilic groups. When these channels are activated, they respond quickly, allowing ions to flow down their electrochemical gradients.
