GABA Receptor Inhibitor

Phenelzine-d5 sulfate is the deuterium labeled Phenelzine sulfate (HY-B1018A). Phenelzine sulfate, an antidepressant agent, is an irreversible and orally active monoamine oxidase (MAO-A and MAO-B) inhibitor. Phenelzine sulfate inhibits GABA transaminase and primary amine oxidase (PrAO), and sequester reactive aldehydes. Phenelzine sulfate also inhibits LSD1 (Ki: 5.6 μM) and suppresses oxidative stress and lipogenesis. Phenelzine sulfate elevates neurotransmitters (serotonin, norepinephrine, dopamine). Phenelzine sulfate is studied in neurological, metabolic and cancer diseases for depression and anxiety disorders, stroke, spinal cord injury, traumatic brain injury, multiple sclerosis, Parkinson’s disease, Alzheimer’s disease, inflammatory pain, obesity and prostate cancer.

Caramboxin is a phenylalanine-like α-amino acid neurotoxin found in star fruit (Averrhoa carambola) with glutamatergic ionotropic action. Caramboxin activates NMDA, AMPA, and kainate receptors while inhibiting GABA binding to synaptic membranes, shifting the CNS toward an excitatory state and exerting neurotoxic effects linked to star fruit ingestion. Caramboxin can be used for research on neurotoxicity and as a reference standard for toxicological studies.

OV329 hydrochloride is a potent GABA aminotransferase inactivator. OV329 hydrochloride is a Vigabatrin (HY-15399) analogue. OV329 hydrochloride can increase brain GABA levels and block abnormal intracerebral hyperexcitability. OV329 hydrochloride exhibits anticonvulsant and antiepileptic activities. OV329 hydrochloride can be used for the research of neurological disease, such as seizure.

Anticonvulsant agent 2 is a potent and orally active anticonvulsant agent. Anticonvulsant agent 2 shows antiepileptic activity.

Afoxolaner (Standard) is the analytical standard of Afoxolaner. This product is intended for research and analytical applications. Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-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.

Cefepime (BMY-28142) (Standard) is the analytical standard of Cefepime. This product is intended for research and analytical applications. Cefepime is a broad-spectrum, blood-brain barrier-permeable cephalosporin antibiotic with hPON1 inhibitory activity, with an IC₅₀ of 21.115 mM and a K_i of 35.092 mM. Cefepime inhibits hPON1 via a non-competitive mechanism and blocks GABA_A receptors. Cefepime penetrates the outer membrane of Gram-negative bacteria, inhibits the growth of Gram-positive and Gram-negative bacteria, and does not induce the production of β-lactamase.

E2730 is a noncompetitive but selective inhibitor of gamma-aminobutyric acid (GABA) transporter 1 (GAT1) with orally available and antiepileptic activity. E2730-mediated GAT1 inhibition is positively correlated with environmental GABA levels and selectively inhibits GAT1-mediated GABA uptake. E2730 (5-50 mg/kg; po) in rat amygdala ignition model, and in mouse cornea ignition (5-50 mg/kg), drug resistance 6Hz-44mA has demonstrated in vivo efficacy in models of psychomotor epilepsy (5-50 mg/kg), fragile X syndrome (2.5-300 mg/kg), and Dravet syndrome (10 mg/kg, 20 mg/kg).

OV329 is a potent GABA aminotransferase inactivator. OV329 is a Vigabatrin (HY-15399) analogue. OV329 can increase brain GABA levels and block abnormal intracerebral hyperexcitability. OV329 exhibits anticonvulsant and antiepileptic activities. OV329 can be used for the research of neurological disease, such as seizure.

Cefepime (BMY-28142) hydrochloride is a broad-spectrum, blood-brain barrier-permeable cephalosporin antibiotic with hPON1 inhibitory activity, with an IC₅₀ of 21.115 mM and a K_i of 35.092 mM. Cefepime hydrochloride inhibits hPON1 via a non-competitive mechanism and blocks GABA_A receptors. Cefepime hydrochloride penetrates the outer membrane of Gram-negative bacteria, inhibits the growth of Gram-positive and Gram-negative bacteria, and does not induce the production of β-lactamase.

Cefepime (BMY-28142) chloride is a broad-spectrum, blood-brain barrier-permeable cephalosporin antibiotic with hPON1 inhibitory activity, with an IC₅₀ of 21.115 mM and a K_i of 35.092 mM. Cefepime chloride inhibits hPON1 via a non-competitive mechanism and blocks GABA_A receptors. Cefepime chloride penetrates the outer membrane of Gram-negative bacteria, inhibits the growth of Gram-positive and Gram-negative bacteria, and does not induce the production of β-lactamase.

TB-21007 is a selective and brain penetrant α5 subunit-containing GABAA receptor inverse agonist with K_is of 1.6 nM, 20 nM, 16 nM, and 20 nM for α5, α1, α2 and α3 subtypes, respectively. TB-21007 enhances cognition in rats.

Scoulerine ((-)-Scoulerine; Discretamine) hydrochloride is a multi-target inhibitor with anti-tumor and antioxidant activities. Scoulerine hydrochloride mainly targets the PI3K/Akt/mTOR signaling axis and α1D-adrenergic receptor, disrupts microtubule structure, and induces cell cycle arrest and apoptosis. Scoulerine hydrochloride effectively inhibits mitochondrial dehydrogenase activity, targets GABA receptors and BACE1, and suppresses the proliferation, migration, invasion, epithelial-mesenchymal transition and stem cell properties of cancer cells. Scoulerine hydrochloride also exhibits multiple pharmacological activities including anti-Plasmodium falciparum, antibacterial, antiemetic and antitussive effects, and regulates endoplasmic reticulum stress and mitochondrial function (modulates Bax, Bcl-2 and cytochrome c). Scoulerine hydrochloride is applicable to research related to leukemia, ovarian cancer, and colorectal cancer.

Flufiprole is a nonsystemic phenylpyrazole insecticide targeting the GABA receptor used in the rice field. Flufiprole is excellent in controlling a wide range of pests.

Tiagabine-d₅ (hydrochloride) is deuterium labeled Tiagabine (hydrochloride). Tiagabine hydrochloride (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease.

Ro19-4603 is a benzodiazepine inverse agonist. Ro19-4603 antagonizes ethanol (EtOH) intake in alcohol-preferring rats.

CPP-115 is a GABA transaminase inactivator with higher affinity and lower retinal toxicity than Vigabatrin (HY-15399). CPP-115 increases brain GABA levels by inhibiting GABA transaminase catabolism. CPP-115 can be used in the study of drug addiction and infantile spasms.

GABA-IN-2 (Compound 5) is a GABA inhibitor. GABA-IN-2 has larvicidal activity and insecticidal effect, with mortality rates of 87% at 50 mg/L.

BuChE-IN-9 (compound 22a) is a potent equine serum-derived BuChE (eqBuChE) inhibitor with an IC₅₀ of 173 nM. BuChE-IN-9 also inhibits human BACE1, Aβ aggregation, mouse GABA transporter 1 (mGAT1) and mGAT4. BuChE-IN-9 has significant antiamnesic properties.

Guvacine, an alkaloid found in the nut of Areca catechu, is a potent GABA uptakp inhibitor. Guvacine inhibits rat GAT-1, rat GAT-2 and rat GAT-3 with IC₅₀ values of 39 μM, 58 μM and 378 μM, respectively.

NNC 05-2090 is aGABA uptake inhibitor and inhibitor of the β-GABA transporter (BGT-1) (IC₅₀ sub>: 10.6 μM). NNC 05-2090 also inhibits mGAT2 with a K_i value of 1.4 μM. NNC 05-2090 has anticonvulsant activity and can be used in the study of epilepsy and neurological diseases.