1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. GABA Receptor
  3. Gabazine free base

Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of 0.2 μM for GABA receptor.

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CAS No. : 105538-73-6

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Top Publications Citing Use of Products

    Gabazine free base purchased from MedChemExpress. Usage Cited in: Nature. 2025 Oct;646(8087):1243-1253.  [Abstract]

    A small fraction of the currents remained in two cells, after d-AP5 exposure, presented a shape consistent with GABAA receptor-mediated currents and could be inhibited with the GABAA receptor blocker Gabazine (Gbz) (12.5 μM).

    Gabazine free base purchased from MedChemExpress. Usage Cited in: Elife. 2024 May 29.

    The effects of ICV injection of different doses of Gabazine (2 or 4 μg/mL; 2000 nL) on the recovery time of midazolam. Compared with the vehicle, ICV injection of Gabazine could reduce the recovery time.

    Gabazine free base purchased from MedChemExpress. Usage Cited in: Elife. 2024 May 29.

    The peak ΔF/F in the Before RORR and RORR-Recovery stages with or without intracerebroventricular injection of Gabazine (4 μg/mL). Gabazine could increase the ΔF/F peak of calcium signaling in LCNE neurons.

    Gabazine free base purchased from MedChemExpress. Usage Cited in: Elife. 2024 May 29.

    The effects of intra-LC injection of Gabazine (4 μg/mL)and intra-VLPO injection of prazosin on the recovery time of midazolam. Microinjection of Gabazine into the LC could reduce the recovery time.
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    Description

    Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of 0.2 μM for GABA receptor[1].

    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    349 nM
    Compound: 2, SR95531
    Antagonist activity at human recombinant GABA A receptor alpha1beta2gamma2S expressed in HEK293 cells assessed as inhibition of GABA-induced current by patch clamp electrophysiology
    Antagonist activity at human recombinant GABA A receptor alpha1beta2gamma2S expressed in HEK293 cells assessed as inhibition of GABA-induced current by patch clamp electrophysiology
    [PMID: 21664131]
    IMR-32 IC50
    7.38 μM
    Compound: SR 95531
    Antagonist activity against GABA type-A receptor in human IMR32 cells assessed as GABA-induced response preincubated for 10 mins followed by GABA addition measured at 140 mins by Epic DMR assay
    Antagonist activity against GABA type-A receptor in human IMR32 cells assessed as GABA-induced response preincubated for 10 mins followed by GABA addition measured at 140 mins by Epic DMR assay
    10.1039/C5MD00442J
    Molecular Weight

    287.31

    Formula

    C15H17N3O3

    CAS No.
    SMILES

    O=C(CCCN1N=C(C2=CC=C(OC)C=C2)C=CC1=N)O

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    Room temperature in continental US; may vary elsewhere.

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    Please store the product under the recommended conditions in the Certificate of Analysis.

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    Gabazine free base
    Cat. No.:
    HY-117256
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