G Protein-Gated Ion Channel Related Research Reagents

G protein-gated ion channels are a family of transmembrane ion channels in neurons and atrial muscle cells, which are directly controlled by G protein. G protein-gated ion channels affect the flow of potassium (K^⁺), calcium (Ca^2⁺), sodium (Na^⁺) and chloride (Cl^-) across the plasma membrane.

Generally, G protein-gated ion channels are specific ion channels located in the plasma membrane of cells, which are directly activated by a series of related proteins. Ion channels allow certain ions to move selectively across the plasma membrane in the cell. More specifically, in nerve cells, together with ion transporters, they are responsible for maintaining the electrochemical gradient across the cell.

G protein-gated ion channels are associated with specific types of G protein-coupled receptors. G protein is a family of intracellular proteins that can mediate signal transduction pathways. Each G protein is a heterotrimer of three subunits: α-, β- and γ-subunits. The receptor protein has a large extracellular binding domain, which will bind to its respective ligands (such as neurotransmitters and hormones). Once the ligand binds to its receptor, a conformational change occurs. This conformational change of the G protein allows Gα to bind to GTP. Different types of G protein-coupled receptors have many known functions, including cAMP and phosphatidylinositol signal transduction pathways. A class of receptors called metabotropic glutamate receptors play an important role in the activation of G protein indirect ion channels. These pathways are activated by second messengers, which trigger a signal cascade involving various proteins that are important for the cell's response.

Fig.1 G protein-gated ion channel.

Clinical Significance

G protein mutations associated with G protein-gated ion channels have been shown to be associated with diseases such as epilepsy, muscle diseases, neurological diseases, and chronic pain.

Epilepsy, chronic pain and addictive drugs such as cocaine, opioids, cannabinoids and ethanol can affect neuronal excitability and heart rate. Gated inwardly-rectifying potassium (GIRK) channels have been shown to be associated with seizure susceptibility, cocaine addiction, and increased tolerance to opioids, cannabinoids, and ethanol. This connection suggests that GIRK channel modulators may be useful therapeutic agents for the treatment of these diseases. GIRK channel inhibitors can be used to treat cocaine, opioid, cannabinoid and ethanol addiction, while GIRK channel activators can be used to treat withdrawal symptoms.

The research of G protein-gated ion channels requires a series of scientific research products. Creative Biolabs has been devoted to the research and development of the most advanced reagents to assist ion channel research. Our product portfolio covers a complete list of GPCR activators and blockers, monoclonal antibodies, labeled antibodies, proteins and assay kits.

Please browse the options to take a deeper look at the tools for your research needs.

For Research Use Only. Not For Clinical Use.

Target

CaSR

ADRA1B

GPCR GPR19

Metabotropic Glutamate Receptor 5

GPCR GPR63

Arrestin 3

PDE7B

VPAC1

Melatonin Related Receptor

M2 Muscarinic Receptor

RAMP1

P2Y12

VPAC2

Histamine H3 Receptor

Delta Opioid Receptor

Metabotropic Glutamate Receptor 7/MGLUR7

Dopamine Receptor D1

CD97

GRK1

alpha 1a Adrenergic Receptor/ADRA1A

S31

GALR3

PTGFR

hCG receptor/LHR

Prostaglandin F2 alpha Receptor/PTGFR

Neurotensin Receptor 1/NTSR1

MC1-R

mGluR1a

GRK2

mGluR5

alpha 2C Adrenergic Receptor/ADRA2C

Dopamine Receptor D3/DRD3