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GABA Receptor antagonists/agonists

GABA transporters with extracellular glycosylation sites and intracellular consensus sites for phosphorylation and 12TM domains, including GAT-1, GAT-2, GAT-3 and BGT-1, play key role in the termination of the synaptic actions of neurotransmitters and utilize sodium and chloride electrochemical gradients to enable GABA sequestration in presynaptic nerve terminals and surrounding glia.

Other Neuronal Signaling Related Inhibitors

Secretase GluR Dopamine Receptor 5-HT Receptor P2 Receptor AChR Histamine Receptor MAO Beta Amyloid BACE

Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
S2133 Gabapentin Gabapentin is a GABA analogue, used to treat seizures and neuropathic pain.
Mol Oncol, 2022, 10.1002/1878-0261.13281
Molecular Oncology, 2022, 2920-2935
Molecular Pharmacology, 2022, 236-245
S6611 Cyclothiazide Cyclothiazide is a positive allosteric modulator of ionotropic α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA)-type glutamate receptors with critical roles in neurological development and function.
J Clin Invest, 2025, 135(24)e191772
Nucleic Acids Res, 2025, 53(18)gkaf965
Nucleic Acids Res, 2024, gkae761
S2399 Dihydromyricetin Dihydromyricetin (Ampelopsin, Ampeloptin) is a natural antioxidant flavonoid from Ampelopsis grossedentata.
Front Pharmacol, 2022, 13:932092
Molecules, 2021, 26(5)1210
Cell Signal, 2020, 65:109431
Verified customer review of Dihydromyricetin
S1332 Flumazenil Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
Communications Medicine, 2025, 420
Toxicological Sciences, 2024, kfae148
Journal of Experimental Medicine, 2022, e20220541
S0303 CGP52432 CGP52432 is a potent and selective antagonist of GABAB autoreceptor with IC50 of 0.085 μM.
Translational Psychiatry, 2025, 271
Research Square, 2024, 10.21203/rs.3.rs-3480364/v1
J Cell Biochem, 2022, 10.1002/jcb.30231
S1338 Gabapentin HCl Gabapentin HCl(Neurontin HCl) is a GABA analogue, used to treat seizures and neuropathic pain.
Mol Pharmacol, 2022, 101(4):236-245
Int J Clin Exp Pathol, 2018, 11(12):5536-5546
J Aging Sci, 2017, 5:1
S3072 (R)-baclofen (R)-baclofen (STX 209) is a derivative of gamma-aminobutyric acid primarily used to treat spasticity.
Journal of Cellular Biochemistry, 2022, 863-877
J Cell Biochem, 2022, 10.1002/jcb.30231
S4587 Pentylenetetrazol Pentylenetetrazol (Pentylenetetrazole, Metrazole, pentetrazol, pentamethylenetetrazol, Corazol, Cardiazol, PTZ) displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GABA(A) receptor antagonist.This compound can be used to induce animal models of (Acute or Chronic) Epilepsy.
Cellular and Molecular Life Sciences, 2024, 104
Cell Mol Life Sci, 2024, 81(1):104
International Journal of Pharmacology, 2023, 206-211
S2026 Ginkgolide A Ginkgolide A (BN52020) is an extract from in Ginkgo biloba and a g-aminobutyric acid (GABA) antagonist with a Ki of 14.5 μM.
Cell Rep, 2020, 21;31(3):107521
S4675 Tiagabine Tiagabine (Gabitril, NO050328, NO328, TGB) is an anti-convulsive medication and a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
Journal of Neurogenetics, May 02, 2018, 106-117

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