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GABA Receptor Agonists

Cat.No. Product Name Information Product Use Citations Product Validations
S1332 Flumazenil Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
J Exp Med, 2022, 219-12e20220541
Biomed Pharmacother, 2018, 107:1674-1681
Holist Nurs Pract, 2017, 31(3):193-203
S0303 CGP52432 CGP52432 is a potent and selective antagonist of GABAB autoreceptor with IC50 of 0.085 μM.
Research Square, 2024, 10.21203/rs.3.rs-3480364/v1
J Cell Biochem, 2022, 10.1002/jcb.30231
Front Neurosci, 2021, 15:741214
S2026 Ginkgolide A Ginkgolide A (BN52020) is an extract from Ginkgo biloba and a g-aminobutyric acid (GABA) antagonist with a Ki of 14.5 μM.
Cell Rep, 2020, 21;31(3):107521
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.
Cell Mol Life Sci, 2024, 81(1):104
S9249 Securinine Securinine, a major natural alkaloid product from the root of the plant Securinega suffruticosa, acts as a γ-amino butyric acid (GABA) receptor antagonist.
E6459New Phaclofen Phaclofen is a selective antagonist of GABAB receptor. Phaclofen is a peripheral and central baclofen antagonist that is used in determining the physiological significance of central and peripheral bicuculline-insensitive receptors with which GABA and (-)-baclofen interact.
S6008 p-Hydroxybenzaldehyde p-Hydroxybenzaldehyde (4-Hydroxybenzaldehyde, 4-Formylphenol, p-Formylphenol), which can be found in the orchids Gastrodia elata, Galeola faberi and vanilla, is a hydroxybenzaldehyde that reacts with NAD+ and H2O to produce 4-hydroxybenzoate, NADH, and 2 protons. This compound at 101.7 μM can significantly reduce the GABA-induced chloride current of expressed GABAA receptors(α1β2γ2S subtype).
S4197 Bemegride Bemegride (Bemegrid, 3-Ethyl-3-methylglutarimide) is a central nervous system stimulant and antidote for barbiturate poisoning.
S5049 Thiocolchicoside Thiocolchicoside (Thiocolchicine 2-glucoside analogue, Coltramyl) is a naturally occurring glycoside originated from the flower seeds of Superba gloriosa with anti-inflammatory and analgesic properties as well as pronounced convulsant activity. It is also an antagonist of GABAA receptor.
S6094 Imidazole-4(5)-acetic Acid Hydrochloride Imidazole-4(5)-acetic Acid Hydrochloride is a competitive antagonist at GABAC receptors.
S6100 Picrotoxin Picrotoxin (Picrotin, Cocculin, Cocculus, NSC 403139), a plant alkaloid, is a non-competitive antagonist of neuronal GABA and glycine receptors.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.
S9176 Pimpinellin Pimpinellin is a furocoumarin that acts as an antagonist of proteins with GABA receptor activity.
S7071 (+)-Bicuculline (+)-Bicuculline (d-Bicuculline) is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.
Commun Biol, 2024, 7(1):1408
Front Pharmacol, 2024, 15:1525753
bioRxiv, 2024, 2024.12.27.630524
Verified customer review of (+)-Bicuculline
S5194 Furosemide sodium Furosemide (Frusemide) sodium is a potent and orally active inhibitor of Na-K-Cl cotransporter (NKCC). Furosemide sodium is a subtype-selective antagonist of gamma-aminobutyric acid type A (GABAA) receptor.
Nat Commun, 2024, 15(1):7342
Ren Fail, 2022, 44(1):1345-1355
S9065 Songorine Songorine, a ubiquitous alkaloid in the genus Aconitum, is a novel antagonist of the GABAA receptor in rat brain and has antiarrhythmic, antinociceptive, anti-inflammatory, regenerative and CNS-modulating properties.