GABA Receptor Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
E1247	SR95531	Gabazine(SR95531) is a potent competitive and allosteric antagonist of the GABAA receptor, with an IC50 for the GABA receptor of 9 µM.
E2848	Afoxolaner	Afoxolaner (NexGard) is a new insecticide/acaricide molecule from the isoxazoline family that acts on the insect gamma-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.
S2996	L-DAB HBR	L-DAB HBR (L-Dab Hydrobromide, L-2,4-Diaminobutyric acid hydrobromide) is an inhibitor of GABA (Gamma-aminobutyric acid) transaminase with IC50 of >500 μM. This compound exhibits antitumor activity.
E0599	Arecaidine hydrochloride	Arecaidine hydrochloride, a constituent of the nut of Areca catechu, inhibits the uptake of GABA and beta-alanine, but not that of glycine.
S4661	Tiagabine hydrochloride	Tiagabine Hydrochloride (Gabitril, NO050328, NO328, TGB) is the hydrochloride salt form of tiagabine, a nipecotic acid derivative with anticonvulsant property. A selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
S4675	Tiagabine	Tiagabine (Gabitril, NO050328, NO328, TGB) is an anti-convulsive medication and a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
E2232	Guvacine hydrochloride	Guvacine hydrochloride is an alkaloid from the nut of Areca catechu, acts as an inhibitor of GABA transporter, and displays modest selectivity for cloned GABA transporters with IC50s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3).
S6470	Fluralaner	Fluralaner (A1443, AH252723) is a systemic insecticide and acaricide that is administered orally. This compound inhibits γ-aminobutyric acid (GABA)-gated chloride channels (GABAA receptors) and L-glutamate-gated chloride channels (GluCls)
E6042	Riluzole hydrochloride	Riluzole hydrochloride (PK 26124 hydrochloride) is an antiepileptic drug, a state-dependent inhibitor of Na+ channels and a selective inhibitor of glutamate release. It also inhibits GABA uptake with an IC50 of 43 µM.
E3508	Magnolia Obovata Extract	Magnolia Obovata Extract is extracted from magnolia obovata, which has an anxiolytic effect through enhancement of the GABA receptor and anti-neuroinflammatory mechanisms.
S1168	Valproic Acid sodium	Valproic Acid sodium is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. Valproic acid induces Notch1 signaling in small cell lung cancer (SCLC) cells. Valproic acid is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α.	J Exp Clin Cancer Res, 2024, 43(1):152 J Immunother Cancer, 2024, 12(11)e009805 Front Pharmacol, 2024, 15:1534772
S3018	Niflumic acid	Niflumic acid (Nifluril) is an inhibitor of cyclooxygenase-2 used for joint and muscular pain.	Oncol Lett, 2020, 20(4):39