GABA Receptor Antagonist

GABA Receptor Antagonists (96):

Cat. No.	Product Name	Effect	Purity

HY-N0219

Bicuculline	Antagonist	99.97%
Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABA_A receptor antagonist (IC₅₀=2 μM). Bicuculline also blocks Ca²⁺ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice.

HY-B0135

Furosemide	Antagonist	99.90%
Furosemide is a potent and orally active inhibitor of Na⁺/K⁺/2Cl^- (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide is also a GABA_A receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.

HY-121116

CGS 8216	Antagonist
CGS 8216, a benzodiazepine receptor antagonist, inhibits ³H-flunitrazepam (³H-FLU) binding to rat synaptosomal membranes in vitro at subnanomolar concentrations.

HY-103533

Gabazine	Antagonist	99.05%
Gabazine is a selective and competitive antagonist of GABA_A receptor, with an IC₅₀ of ~0.2 μM for GABA receptor.

HY-B0009

Flumazenil	Antagonist	99.97%
Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.

HY-103531

CGP52432	Antagonist	98.16%
CGP52432 is a GABA_B receptor antagonist, with an IC₅₀ of 85 nM.

HY-100813

Saclofen	Antagonist	99.87%
Saclofen is an orally available competitive GABA_B receptor antagonist with an IC₅₀ of 7.8 μM, but it has a weaker antagonistic effect on GABA_B1b and GABA_B2 heterodimer recombinant receptors. Saclofen can inhibit the binding of baclofen (HY-B007) to rat cerebellar membranes and block the phase shifts in circadian rhythms caused by baclofen. Saclofen has also shown anti-inflammatory and analgesic effects in rats.

HY-10232

THIP	Antagonist	99.93%
THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC₅₀ value of 13 µM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders.

HY-N2079

(-)-Securinine	Antagonist	99.93%
(-)-Securinine is plant-derived alkaloid and also a GABA_A receptor antagonist.

HY-108689

Broflanilide	Antagonist	99.36%
Broflanilide is a potential insecticide and metabolized to Desmethyl-Broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin (RDL) GABA Receptor, and inhibits S. litura RDL GABAR, with an IC₅₀ value of 1.3 nM.

HY-103530

CGP35348	Antagonist	≥98.0%
CGP 35348?is a selective, brain penetrant, centrally active GABAB receptor antagonist with an EC₅₀ of 34 μM.?CGP 35348 shows affinity for the GABAB receptor only. CGP 35348 has a potential to improve neuromuscular coordination and spatial learning in albino mouse following neonatal brain damage.

HY-116564

Lotilaner	Antagonist	99.84%
Lotilaner is a parasiticide, acts as a potent non-competitive antagonist of insects GABACl receptors, with an IC₅₀ of 23.84 nM for Drosophila melanogaster GABA receptor. No effect on a dog GABAA receptor.

HY-Y0313

p-Hydroxybenzaldehyde	Antagonist	99.98%
p-Hydroxybenzaldehyde is a one of the major components in vanilla aroma, with antagonistic effect on GABA_A receptor of the α₁β₂γ₂S subtype at high concentrations.

HY-B1494

Picrotoxinin	Antagonist	99.82%
Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABA_A receptor antagonist, which negatively modulates the action of GABA on GABA_A receptors. Picrotoxinin inhibits α₁β₂γ_2L GABA_A receptor with an IC₅₀ of 1.15 μM.

HY-120051

Afizagabar	Antagonist	98.40%
Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC₅₀ of 585 nM for α5β2γ2 and a K_i of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy.

HY-B0355

Ginkgolide A	Antagonist	≥98.0%
Ginkgolide A (BN-52020) is an extract from in Ginkgo biloba and a g-aminobutyric acid (GABA) antagonist.

HY-103516

CGP55845 hydrochloride	Antagonist	≥99.0%
CGP55845 hydrochloride is a potent and selective GABAB receptor antagonist with an IC₅₀ of 6 nM. CGP55845 hydrochloride can be used for neurological research.

HY-B0135A

Furosemide sodium	Antagonist	99.89%
Furosemide sodium is a potent and orally active inhibitor of Na⁺/K⁺/2Cl^- (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide sodium is also a GABA_A receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide sodium acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.

HY-B0822

Fipronil	Antagonist	98.98%
Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits GABA receptor with IC₅₀s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes.

HY-100370

MRK-016	Antagonist	99.71%
MRK-016 is a selective, orally bioavailable inverse agonist of GABA_A α5 receptor, with an EC₅₀ of 3 nM for GABA_A α5, and K_is of 0.83, 0.85, 0.77?and 1.4?nM for human?GABA_A?α1β3γ2, GABA_A?α2β3γ2, GABA_A?α3β3γ2, and GABA_A?α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.

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