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Gabazine free base

(Synonyms: SR95531 free base)

9 Cited Publications

Customer Review

Based on 9 publication(s) in Google Scholar

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

For research use only. We do not sell to patients.

CAS No.: 105538-73-6
Formula: C₁₅H₁₇N₃O₃
Molecular Weight:287.31

Storage:

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

Data Sheet (264 KB)

Gabazine free base Chemical Structure

CAS No.: 105538-73-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
Chemical Information
Publications (9)
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

Gabazine is a selective and competitive antagonist of GABA_A 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

Chemical Information

CAS No. 105538-73-6
Molecular Weight 287.31
Formula C₁₅H₁₇N₃O₃
SMILES

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

SR95531 free base
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Publications (9)

All Bio/Physico-chemical AssayIn Vivo Efficacy Study

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Nature

Functional synapses between neurons and small cell lung cancer. [Abstract]

2025 Oct;646(8087):1243-1253. PMID: 40931078

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).
Nat Neurosci

Emergence of consciousness from anesthesia through ubiquitin degradation of KCC2 in the ventral posteromedial nucleus of the thalamus. [Abstract]

2023 May;26(5):751-764. PMID: 36973513
Mol Psychiatry

BDNF restores impaired long-term potentiation of GABAergic synapses induced by chronic ethanol exposure in the VTA and attenuates reward-seeking behavior. [Abstract]

2026 Mar 23. PMID: 41872517
Acta Pharmacol Sin

GluN2A-NMDA receptor inhibition disinhibits the prefrontal cortex, reduces forced swim immobility, and impairs sensorimotor gating. [Abstract]

2025 Sep 10. PMID: 40931040
Phytomedicine

Geraniol enhances inhibitory inputs to the paraventricular thalamic nucleus and induces sedation in mice. [Abstract]

2022 Jan 29;98:153965. PMID: 35144136
Elife

2024 May 29.

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.
iScience

Synaptic scaling of corticostriatal circuits underlies hyperactivity in GABA Transporter-1 deficient mice. [Abstract]

2023 Mar 3;26(4):106322. PMID: 36968092
bioRxiv

Cholinergic activation of corticofugal circuits in the adult mouse prefrontal cortex. [Abstract]

2023 Jul 22:2023.04.28.538437. PMID: 37163128
Oxid Med Cell Longev

Activation of TGR5 Ameliorates Streptozotocin-Induced Cognitive Impairment by Modulating Apoptosis, Neurogenesis, and Neuronal Firing. [Abstract]

2022 Apr 15;2022:3716609. PMID: 35464765

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (264 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Ueno S,et al. Bicuculline and gabazine are allosteric inhibitors of channel opening of the GABAA receptor. J Neurosci. 1997 Jan 15;17(2):625-34. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

Gabazine free base

9 Cited Publications

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Biological Activity
- Description
Chemical Information
Publications (9)
Purity & Documentation
References

1/16
1/16

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

Customer Validation
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).
1/16

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

Customer Validation
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.
1/16

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

Customer Validation
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.
1/16

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

Customer Validation
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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Gabazine free base

Publications Citing Use of MedChemExpress (MCE) Gabazine free base

Biological Activity

Chemical Information

Publications (9)

Purity & Documentation

References

Calculators

Help & FAQs

Gabazine free base Related Classifications

Cat. No.: HY-117256