GABA Receptor Inhibitor

HIE-124 is a potent ultra-short acting hypnotic that exhibits a rapid onset of action and a shorter duration of action with no acute tolerance or noticeable side effects. HIE-124 is promising for research of preanesthetic medication and anesthesia inducer.

Deschloro-Zopiclone is an impurity of Zopiclone. Zopiclone is the first non-benzodiazepine compound, which can enhance the activity of inhibitory neurotransmitter gamma amino butyric acid in the brain.

3-Ethyl-3-methylthiolan-2-one is an antiepileptic agent that inhibits GABA_A receptors.

HDZI 2,4OH exerts significant anti anxiety activity through GABA receptors. HDZI 2,4OH can penetrate the blood-brain barrier. HDZI 2,4OH exhibits low toxicity in zebrafish. HDZI 2,4OH can be used for research on neurological disorders such as anxiety disorders.

GABA-AT-IN-2 (compound 11g) is a GABA aminotransferase (GABA-AT) inhibitor with an IC₅₀ of 19.8 μM. GABA-AT-IN-2 demonstrates notable antianxiety effects in mice. GABA-AT-IN-2 can be used for anxiety-related neurotic disorders research.

LU-32-176B, a GABA transporter 1(GAT1) selective inhibitor, is found to exert a synergistic anticonvulsant action with GAT2 transport inhibitor EF1502. LU-32-176B inhibits neurons, astrocytes and mGAT1 with the IC₅₀ values of 2μM, 1μM, 4μM, respectively.

mGAT3/4-IN-1 (compound 19b) is a potent mGAT3/mGAT4 inhibitor, with pIC₅₀ values of 5.31 and 5.24, respectively. mGAT3/4-IN-1 exhibits a significant tactile allodynia reduction in diabetic neuropathic mice.

Thiazesim hydrochloride is a CNS-penetrant GABAA receptor inhibitor, exerting anticonvulsant and antidepressant effects. Thiazesim hydrochloride depresses amygdala output, disrupts conditioned avoidance response in rats. Thiazesim hydrochloride can be used for the research of depression and epilepsy.

CHF-2993 is an orally active anticonvulsant. CHF-2993 antagonizes Bicuculline (HY-N0219)- and Picrotoxin (HY-101391)-induced tonic convulsions in mice, shows no activity against Pentylenetetrazole-induced clonic convulsions in mice, and partially reduces Veratridine (HY-N6691)-induced aspartate efflux in rat cortical synaptosomes. CHF-2993 can be used in the research of epilepsy.

GABAA receptor agent 8 (compoud 5e) is a potent GABAA receptor positive modulator. GABAA receptor agent 8 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 8 has the potential for the research of epilepsy.

CI-966 is a potent, selective, orally active and brain-penetrant inhibitor of the GABA transporter GAT-1, with IC₅₀s of 0.26 μM and 1.2 μM for hGAT-1, rGAT-1, respectively. CI-966 shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 exhibits anticonvulsant and neuroprotective activities.

AA29504 is a ethyl carbamate with γ-aminobutyric acid (GABAA(HY-L120) receptor activity. AA29504 inhibits the delivery of the neurotransmitter gamma-aminobutyric acid in the central nervous system. AA29504 can be used to research anxiety, insomnia and other neuropsychiatric diseases .

GABA-IN-1 (Compound 6) is a GABA inhibitor. GABA-IN-1 has larvicidal activity and insecticidal effect, with mortality rates of 93% at 50 mg/L.

CP-457920 (Compound 21) is a GABA receptor inhibitor (K_i ≈ 1 ng/mL). CP-457920 can be used in research on neurological diseases such as Alzheimer's disease.

TETS-4-Methylaniline (compound 2k) is a hapten. TETS-4-Methylaniline conjugates to the carrier protein via using either diazotization or glutaraldehyde methods.

DPNI-GABA is a nitroindoline cage compound that inhibits GABA(A) receptors and reduces GABA-evoked peak responses with an IC₅₀ value of 0.5 mM.

Tiagabine-d₄ hydrochloride is deuterated labeled Tiagabine hydrochloride (HY-B0696A). 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.

Transcription factor-IN-1 (Compound 4e) is an inhibitor for transcription factor. Transcription factor-IN-1 exhibits anticonvulsant activity by antagonism with pentylenetetrazole (PTZ) (ED₅₀ =34.5 mg/kg). Transcription factor-IN-1 exhibits antidepressant effects in rat models.

mNLS-CPP-WSTF is a nuclear localization signal (NLS)-cell-penetrating peptide based on the mouse WSTF sequence. mNLS-CPP-WSTF significantly inhibits the GABARAP-WSTF interaction, WSTF degradation and inflammatory gene expression. mNLS-CPP-WSTF effectively attenuates chronic inflammation, liver fibrosis and cartilage damage in metabolic-dysfunction-associated steatohepatitis (MASH) and osteoarthritis (OA) mice model. mNLS-CPP-WSTF is promising for research of chronic inflammatory diseases such as MASH and OA.

Leptophos oxon, a metabolite of leptophos, is a GABA_A receptor chloride channel inhibitor with an IC₅₀ values of 89.6 μM. Leptophos oxon inhibits GABA-induced chloride influx, binds to GABA_A receptor-associated TBPS sites, and inhibits TBPS binding to voltage-dependent chloride channels. Leptophos oxon is a insecticide. Leptophos oxon can be used for the research of neurological disease.