GABA Receptor Inhibitor

CI-966 hydrochloride 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 hydrochloride shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 hydrochloride exhibits anticonvulsant and neuroprotective activities.

Riluzole (Standard) is the analytical standard of Riluzole. This product is intended for research and analytical applications. Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na⁺ channel blocker which can also inhibit GABA uptake with an IC₅₀ of 43 μM.

Harmane hydrochloride is a benzodiazepine receptor inhibitor (IC₅₀=7 μM), with IC₅₀ values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane hydrochloride inhibits the I1 imidazoline receptor (IC₅₀ = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane hydrochloride inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane hydrochloride can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).

Cefepime-d₃ (BMY-28142-d₃) sulfate is deuterium labeled Cefepime sulfate. Cefepime sulfate 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 sulfate inhibits hPON1 via a non-competitive mechanism and blocks GABA_A receptors. Cefepime sulfate 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.

BGT1-IN-1 (compound 9) is a potent BGT1 inhibitor with IC₅₀ value of 13.9, 58.3 µM for hBGT1, GAT3, respectively. BGT1-IN-1 shows no cytotoxic. BGT1-IN-1 shows neuroprotective activity.

Fluorothyl (Bis (2,2,2-trifluoroethyl) ether; Flurothyl) is a GABAA receptor modulator and epileptogenic agent. Fluorothyl induces generalized epilepsy in mice. Fluorothyl is used for epilepsy research.

Waglerin-1, a 22-amino acid peptide, is a competitive antagonist of the muscle nicotinic receptor (nAChR).

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

Temgicoluril (Tetramethylglycoluril) is an orally active antianxiety and antidepressant. Temgicoluril acts on GABA receptors to enhance GABA neurotransmission.

mNLS-CPP-WSTF TFA is the trifluoroacetate salt of mNLS-CPP-WSTF (HY-P11208). 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.

RuBi-Glutamate hexafluorophosphate sodium is a neuronal activator. RuBi-Glutamate hexafluorophosphate sodium photocleaves to release glutamate upon one- or two-photon excitation, activating glutamate receptors in cortical pyramidal neurons. RuBi-Glutamate hexafluorophosphate sodium reduces peak amplitude of evoked GABAergic inhibitory postsynaptic currents in its caged form. RuBi-Glutamate hexafluorophosphate sodium can be used for the research of Huntington's disease.

Sandaracopimaric acid is a diterpenoid with anti-inflammatory effect. Sandaracopimaric acid reduces the contraction of phenylephrine-induced pulmonary arteries with an EC₅₀ of 43.93 μM.

Cefepime-d₈ (BMY-28142-d₈) sulfate is deuterium labeled Cefepime sulfate. Cefepime sulfate 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 sulfate inhibits hPON1 via a non-competitive mechanism and blocks GABA_A receptors. Cefepime sulfate 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) Dihydrochloride Monohydrate (Standard) is the analytical standard of Cefepime Dihydrochloride Monohydrate. This product is intended for research and analytical applications. Cefepime Dihydrochloride Monohydrate 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 Dihydrochloride Monohydrate inhibits hPON1 via a non-competitive mechanism and blocks GABA_A receptors. Cefepime Dihydrochloride Monohydrate 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.

Arecaidine hydrobromide is a GABA transport system inhibitor. Arecaidine hydrobromide inhibits the proliferation of oral mucosal fibroblasts, increases the secretion of IL-6, TGF-β and TNF-α in cells, downregulates the expression of PPAR-γ and PCK1 in cells, and upregulates the expression of TGF-β1. Arecaidine hydrobromide inhibits the uptake of γ-aminobutyric acid and β-alanine by the central nervous system of cats. Arecaidine hydrobromide inhibits hPAT1-mediated L-[³H]proline uptake in cells. Arecaidine hydrobromide can be used in research related to neurological diseases.

6-Hydroxyflavanone is a compound that can be isolated from the Muntingia calabura leaves. 6-Hydroxyflavanone targets cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX), and opioid and GABA-A receptors that has anti-inflammatory and anti-neuropathic pain potential. 6-Hydroxyflavanone can be used for the research of diabetes.

Harman-¹³C₂,¹⁵N is ¹³C and ¹⁵N labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC₅₀=7 μM), with IC₅₀ values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC₅₀ values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC₅₀=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).

γ-Acetylenic GABA (4-Aminohex-5-ynoic acid) is an irreversible inhibitor of GABA-transaminase. γ-Acetylenic GABA can increase the concentration of GABA in rat brain. γ-Acetylenic GABA is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

U93631 is a GABAA receptor inhibitor targeting the picrotoxin (HY-101391) site, which exhibits higher inhibitory potency in receptors lacking α subunits. U93631 blocks GABA-induced chloride currents, exerts a mild initial stimulatory effect on activated currents, but its activity decreases in β2T246F mutant receptors. U93631 can serve as a ligand for the convulsant site of GABAA receptors in relevant studies.

L-DABA (L-2,4-Diaminobutyric acid) hydrobromide is a week GABA transaminase inhibitor with an IC₅₀ of larger than 500 μM; exhibits antitumor activity in vivo and in vitro.