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GABA Channels

    GABA Channels

    GABAA receptors are the major inhibitory transmitter receptors in the brain. They are ligand-gated chloride channels composed of five subunits that can belong to different subunit classes. Each subunit contains 4 transmembrane domains. These receptors are located in the cell membranes of neurons, and most of them are on the synaptic back membranes.

    1. Detailed information

    GABAA receptors are the major inhibitory transmitter receptors in the brain. They are ligand-gated chloride channels composed of five subunits that can belong to different subunit classes. Each subunit contains 4 transmembrane domains. These receptors are located in the cell membranes of neurons, and most of them are on the synaptic back membranes.

    GABA is the endogenous ligand of GABAA receptors, its binding changes the receptor composition on the cell membrane which alternatively open the channel leading to the passage of the chlorine ion through the channel along the potential and concentration gradient.

    As, the reversing potential of chlorine ions on most of the neurons is near the resting membrane potential of the cell, or slightly below the resting potential, the activation of the GABAA receptor can make the resting potential more stable and even hyperpolarizes the cell, which weakens the depolarization effect of the excited neurotransmitter and the possibility of producing the action potential. Therefore, the receptor mainly plays an inhibitory role in reducing neuronal activity.

    In the human body, it has the following sub-types:

    Six α sub-types (GABRA1, GABRA2, GABRA3, GABRA4, GABRA5, GABRA6)

    Three β sub-types (GABRB1, GABRB2, GABRB3)

    Three γ sub-types (GABRG1, GABRG2, GABRG3)

    one δ (GABRD), one ε

    (GabRE), one π (GABRP) and one θ GABRQ

    ICE Biosciences has established the GABAA1-A6 channel, which expresses a variety of sub-base combinations, providing screening services for drugs related to anesthesia, depression, etc.

    ICE Established GABA cell lines

    Targets

    Subunits

    Cells

    Catalog number

    GABAA1

    α1β2γ2

    HEK293

    ICE-HEK-GABA-A1

    GABAA1

    α1β3γ2

    HEK293

    ICE-HEK-GABA-A1

    GABAA2

    α2β3γ2

    HEK293

    ICE-HEK-GABA-A2

    GABAA3

    α3β2γ3

    HEK293

    ICE-HEK-GABA-A3

    GABAA4

    α4β2γ3

    HEK293

    ICE-HEK-GABA-A4

    GABAA4

    α4β3δ

    HEK293

    ICE-HEK-GABA-A4

    GABAA5

    α5β3γ2

    HEK293

    ICE-HEK-GABA-A5

    GABAA6

    α6β2γ2

    HEK293

    ICE-HEK-GABA-A6

    GABAA1β2γ2) Assay Data Sheet


    Channel

    GABAA1β2γ2)

    Gene

    GABRA1/GABRB2/GABRG2

    Catalog Reference

    ICE-HEK-GABA-A1

    Sources

    Human

    Expression System

    HEK293

    Method

    whole cell patch clamp

    Standard Time

    2-4 weeks

    Reference Compound

    Diazepam, Bicuculline

    Target

    Convulsive, Sedative, Anxiolytic.

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    GABAA(α4β3δ)Assay Data Sheet

    Channel

    GABAA4β3δ)

    Gene

    GABRA4/GABRB3/GABRD

    Catalog Reference

    ICE-HEK-GABA-A4-transient

    Sources

    Human

    Expression System

    HEK293

    Method

    whole cell patch clamp

    Standard Time

    2-4 weeks

    Reference Compound

    Diazepam, Bicuculline

    Linked Disorders

    Convulsive, Sedative, Anxiolytic.


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    Fluorescence Assay of GABAA Channels


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    EC50 of GABA and IC50 of Bicuculline on α1-α6 GABAA receptor subtypes

     Targets

    GABA EC50 (μM)

     Z'factor

    Bicuculline IC50 (μM)

     Z'factor

    GABA α1β2γ2

    14.6

    0.879

    14.29

    0.65

    GABA α2β3γ2

    7.195

    0.784

    24.99

    0.72

    GABA α3β2γ3

    1.513

    0.825

    52.89

    0.75

    GABA α4β2γ3

    2.409

    0.929

    23.85

    0.61

    GABA α5β3γ2

    0.5458

    0.759

    45.16

    0.83

    GABA α6β3δ

    0.4823

    0.598

    -

    -


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