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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, inhibitingGABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod .
TACA (trans-4-Aminocrotonic acid) is a potent agonist of GABAA and GABACreceptors (KD= 0.6 μM). TACA also is GABA uptake inhibitor and substrate for GABA-T. TACA produces late biphasic responses in the MPG neurons .
GABAreceptor Antagonist 1 (compound 7w) inhibitsPx RDL1 GABAR with an IC50 value of 7.08 nmol/L. GABAreceptor Antagonist 1 shows insecticide activity against P. xylostella, S. frugiperda, S. exigua, and S. litura, with LC50 of 0.09, 0.84, 0.87, and 0.68 mg/L respectively. GABAreceptor Antagonist 1 shows a medium toxicity to honeybee (48 h, ID50 = 2.22 μg/adult), and low toxicity to zebrafish (LC50: 42.4 mg/L) .
Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAAreceptor antagonist, which negatively modulates the action of GABA on GABAAreceptors. Picrotoxinin inhibits α1β2γ2L GABAAreceptor with an IC50 of 1.15 μM .
3-Hydroxyphenazepam is an active metabolite of Cinazepam. Cinazepam is a GABAA receptor agonist. 3-Hydroxyphenazepam can inhibit synaptosomal transporter-mediated [ 3H]GABA uptake .
Broflanilide is a potential insecticide and metabolized to Desmethyl-Broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin (RDL) GABAReceptor, and inhibitsS. litura RDL GABAR, with an IC50 value of 1.3 nM .
Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibitsGABAreceptor with IC50s of 30 nM and 1600 nM for cockroach and rat GABAreceptors, 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 .
FGIN 1-43 is an effective and specific ligand for the mitochondrial diazepam binding inhibitor (DBI) receptor (related to the production of neurosteroids). FGIN 1-43 enhances the transmission of GABA by inducing the production of neurosteroids, which can be used for research on anti-anxiety .
Fipronil (Standard) is the analytical standard of Fipronil. This product is intended for research and analytical applications. Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibitsGABAreceptor with IC50s of 30 nM and 1600 nM for cockroach and rat GABAreceptors, 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 .
Lesogaberan (AZD-3355) is a potent and selective GABABreceptor agonist with an EC50 of 8.6 nM for human recombinant GABABreceptors. The affinity (Kis) of Lesogaberan for rat GABAB and GABAAreceptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABABreceptor agonist with an EC50 of 8.6 nM for human recombinant GABABreceptor. The affinity (Kis) of Lesogaberan hydrochloride for rat GABAB and GABAAreceptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
Lesogaberan (AZD-3355) napadisylate is a potent and selective GABABreceptor agonist with an EC50 of 8.6 nM for human recombinant GABABreceptors. The affinity (Kis) of Lesogaberan napadisylate for rat GABAB and GABAAreceptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
Fipronil sulfone is the major metabolite of Fipronil.Fipronil sulfone selectively inhibitsGABAreceptor with IC50 of 175 nM (assayed by displacement of 4′-ethynyl-4-n-[2,3-3H2]- propylbicycloorthobenzoate ([3H]EBOB) from the noncompetitive blocker site).
BL-1020 mesylate is the mesylate salt form of BL-1020. BL-1020 mesylate is an antipsychotic agent. BL-1020 mesylate is inhibitor for dopamine receptor and serotonin receptor (5-HT receptor), with Ki of 0.066, 0.062 and 0.21 nM, for D2L, D2S and 5-HT2A receptors, respectively. BL-1020 mesylate is agonist for GABAAreceptor with Ki of 3.74 μM, and enhances the GABA release. BL-1020 mesylate exhibits high affinity with histamine receptor (Ki is 0.47 nM). BL-1020 mesylate reduces Amphetamine-induced hyperactivity, with lower catalepsy and sedation. BL-1020 mesylate is blood-brain barrier penetrate .
Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABAreceptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
GABAreceptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory neurotransmitter in the vertebrate central nervous system. There are two classes of GABAreceptors: GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors), whereas GABAB receptors are G protein-coupled receptors (also known asmetabotropic receptors). GABAreceptors are significant drug targets in the treatment of neuropsychiatric disorders such as epilepsy, insomnia, and anxiety, as well as in anesthesia in surgical operations.
MCE offers a unique collection of 139 GABAreceptorsinhibitors and activators, which is an efficient tool for neuropsychiatric disorders drugs discovery.
Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAAreceptor antagonist, which negatively modulates the action of GABA on GABAAreceptors. Picrotoxinin inhibits α1β2γ2L GABAAreceptor with an IC50 of 1.15 μM .
DBI, a versatile protein, binds medium- and long-chain acyl-CoA esters, indicating a potential intracellular carrier role. It also displaces diazepam from the benzodiazepine recognition site on the GABA type A receptor. This dual functionality suggests DBI may act as a neuropeptide, modulating GABA receptor activity. Remarkably, DBI functions as a monomer in these interactions. DBI Protein, Human (103a.a, His) is the recombinant human-derived DBI protein, expressed by E. coli , with N-6*His labeled tag. The total length of DBI Protein, Human (103a.a, His) is 103 a.a., with molecular weight of ~14 kDa.
Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABAreceptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
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