Catalog No.
Product Name
Application
Product Information
Citations
- Propofol is a hypnotic alkylphenol derivative. Propofol is a General Anesthetic. Propofol is a short-acting medication that results in a decreased level of consciousness and lack of memory for events. Formulated for intravenous induction of sedation and hypnosis during anesthesia, propofol facilitates inhibitory neurotransmission mediated by gamma-aminobutyric acid (GABA).
- Daphne Chun-Che Chien, .et al. , Sci Transl Med, 2024, May 8;16(746):eadk8198 PMID: 38718132
- Chenghao Jin, .et al. , Immun Inflamm Dis, 2023, Aug;11(8):e952 PMID: 37647434
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GABAA antagonist
(+)-Bicuculline is a classical GABAA antagonist.- Maryam Adenike Salaudeen, .et al. , J Pharmacy and Drug Innovations, 2022, 3(4)
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GABA(A) receptor agonist
Muscimol hydrobromide is a potent but toxic structural analog of g-aminobutyric acid (GABA), with a zwitterionic structure.- Shi, Mengting, .et al. , Acupuncture and Herbal Medicine, 2025, 5(2):p 217-228
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HIV-1 production Inhibitor
Baicalin is a known prolyl endopeptidase inhibitor and affects the GABA receptors.- Shoichi Ozawa, .et al. , Sci Rep, 2019, 9: 15464 PMID: 31664047
- Chlormezanone (Trancopal), a non-benzodiazepine that is used in the management of anxiety. It has been suggested for use in the treatment of muscle spasm. Chlormezanone binds to central benzodiazepine receptors which interact allosterically with GABA receptors. This potentiates the effects of the inhibitory neurotransmitter GABA, increasing the inhibition of the ascending reticular activating system and blocking the cortical and limbic arousal that occurs following stimulation of the reticular pathways.
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Dihydropyrimidinase Inhibitor
Dihydromyricetin (Ampelopsin (flavanol); Ampeloptin) is a natural antioxidant with good prospects. -
Benzodiazepine antagonist
Flumazenil, an imidazobenzodiazepine derivative, antagonizes the actions of benzodiazepines on the central nervous system. Flumazenil competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex. Flumazenil is a weak partial agonist in some animal models of activity, but has little or no agonist activity in humans. - Furosemide is a non-competitive antagonist at GABAA receptors with ~ 100-fold greater selectivity for α6-containing receptors than α1-containing receptors.
- Nefiracetam is cognitive enhancer. It activates L/N-type calcium channels, cholinergic, monoaminergic and GABAergic systems.
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GABA uptake inhibitor
SKF 89976A hydrochloride is a potent inhibitor of GABA uptake with IC50 of 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively. -
partial benzodiazepine receptor agonist
Pipequaline hydrochloride (PK-8165 hydrochloride) is a partial benzodiazepine receptor agonist with anxiolytic activity. -
GABAA receptors agonist
Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a selective agonist at GABAA receptors that contain α4-δ subunits, and has anxiolytic and sedative effects. -
Benzodiazepine inverse agonist
DMCM (hydrochloride) is Benzodiazepine inverse agonist that displays anxiogenic and potent convulsant activity. -
GABAB receptor positive allosteric modulator
SSD114 hydrochloride is a novel GABAB receptor positive allosteric modulator. -
GABA-A modulator
Imidazenil is a GABA-A modulator that blocks the sedative effects without lowering the convulsion threshold. -
nervoussystem toxicant
Emamectin Benzoate (MK-244) is an orally active nervoussystem toxicant by binding g-aminobutyric (GABA) receptor in insects. - 4-Acetamidobutanoic acid (N-acetyl GABA) is a γ-aminobutyric acid (GABA) derivative.
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GABA receptor agonist
Isoguvacine hydrochloride is a GABA receptor agonist. - Piperazine Citrate is an organic compound that consists of a six-membered ring, containting two nitrogen atoms at opposite positions in the ring; first introduced in 1953 as an Anthelmintic.
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chemoprotective agent
Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation. -
GABAAα5 modulator
Basmisanil is a highly selective GABAAα5 negative allosteric modulator. -
GABAA receptor partial agonist
CP-409092 hydrochloride is a partial agonist of GABAA receptor, with anti-anxiety activity. -
benzodiazepine receptor inverse agonist
Ro 19-4603 is a benzodiazepine receptor inverse agonist. -
GABA receptor antagonist
Gabazine free base is a specific GABA receptor antagonist. Does not affect GABA-transaminase or glutamate-decarboxylase activitites. -
pyrazolopyridine anxiolytic
Tracazolate is a pyrazolopyridine anxiolytic known to interact with gamma-aminobutyric acid (GABA)(A) receptors, adenosine receptors, and phosphodiesterases. -
modulator of the GABAA receptor complex
GABAA Modulator I is novel modulator of the GABAA receptor complex, and in particular for combating anxiety and related diseases. -
Stable Isotope
Primidone-d5 is a deuterium-labeled analog of Primidone, primarily known for its inhibitory action on the transient receptor potential melastatin 3 (TRPM3) channel, with an IC50 value of 0.6 μM. This reagent also inhibits receptor-interacting protein (RIP) kinase and voltage-gated sodium channels, while acting as an antagonist at the GABA receptor. Primidone-d5 is valuable for research in pain management and seizure disorders, enabling studies focused on its analgesic and anticonvulsant properties. - 6-Hydroxyflavone is an orally active flavonoid with diverse pharmacological properties. It exhibits anti-inflammatory activity by inhibiting lipopolysaccharide (LPS)-induced nitric oxide (NO) production and also promotes osteoblast differentiation through activation of the AKT, ERK1/2, and JNK signaling pathways, supporting its role in bone health. Additionally, 6-Hydroxyflavone inhibits the glycosylation of bovine hemoglobin (BHb), suggesting potential in managing glycation-related complications. It demonstrates kidney-protective effects and modulates GABAergic neurotransmission by enhancing GABA-induced currents via the benzodiazepine binding sites on GABAA receptors
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GABAB Receptor Negative Allosteric Modulator
CLH304a (compound 14) is a selective and noncompetitive negative allosteric modulator (NAM) of the GABA$_B$ receptor. It specifically targets the heptahelical domain of the GB2 subunit, inhibiting receptor activity with inverse agonist properties. CLH304a reduces GABA-induced inositol trisphosphate (IP₃) production with an IC₅₀ of 37.9 μM and does not affect other Class C GPCRs, including mGluR1, mGluR2, and mGluR5, indicating high selectivity. Additionally, CLH304a inhibits Baclofen-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABA$_B$ receptors, further supporting its function as a negative modulator. This compound is a valuable tool for investigating GABA$_B$ receptor function and holds potential for therapeutic research in neurological disorders involving GABAergic signaling dysregulation. -
Benzodiazepine receptor agonist
Pipequaline (PK 8165) is a partial benzodiazepine receptor agonist with anxiolytic activity. -
GABA transport inhibitor
(S)-SNAP5114 is a selective GABA transport inhibitor, with IC50 values of 5 μM and 21 μM for hGAT-3 and rGAT-2, respectively. (S)-SNAP5114 is an anticonvulsant drug.
