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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 .
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 .
Droperidol (Dehydrobenzperidol) is a butyrophenone pamine-2receptor antagonist that inhibits the activation of GABA(A) and neuronal nicotinic receptors (nAChR), with IC50 values of 12.6 nM and 5.8 μM. Droperidol has anesthetic and sedative properties .
Sch 50910 is a GABA(B) receptor antagonist with some activity in inhibitingGABA(B) autoreceptors. Sch 50910 had no effect on electrically stimulated release at a concentration of 100 μM. The activity of Sch 50910 suggests that it may not have a significant role in studies of GABA(B) receptor function .
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) .
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, inhibitingGABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod .
Profadol (CI-572) hydrochloride is a potent analgesic agent. Profadol is a µ-opioid receptor (MOR) agonist. Profadol hydrochloride activates the γ-aminobutyric acid (GABA) receptors and inhibits the N-methyl-D-aspartate (NMDA) receptor. Profadol increases the mRNA and protein expression of MOR .
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 .
Picrotoxinin (Standard) is the analytical standard of Picrotoxinin. This product is intended for research and analytical applications. Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC50 of 1.15 μM .
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 .
CGP55845 is a potent and selective GABAB receptor antagonist with activity that blocks agonist binding. The IC50 value of CGP55845 is 5 nM, indicating that it exhibits significant activity in inhibitingGABA and glutamate release. The apparent Kd of CGP55845 when forming a complex with the GABAB receptor is 30 nM, indicating its high affinity for this receptor. CGP55845 is as potent as 100 μM CGP 35348 in relieving the inhibitory effect of (R)-(-)-baclofen .
Broflanilide (Standard) is the analytical standard of Broflanilide. This product is intended for research and analytical applications. Broflanilide is a potential insecticide and metabolized to Desmethyl-Broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin (RDL) GABAReceptor, and inhibits S. litura RDL GABAR, with an IC50 value of 1.3 nM .
Emamectin B1a (L-656,748) is a semisynthetic derivative of avermectin B1a that binds to GABAreceptors (Ki=17.6 nM in rat brain membranes) and enhances GABA responses. Emamectin B1a acitivates GABAA receptorsα1β1γ2, α1β2γ2, and α1β3γ2 with IC50s of 57, 210, and 49.8 nM, respectively. Emamectin B1a also binds to glycine receptors, inhibiting glycine receptors with an IC50=218 nM in rat spinal cord. Emamectin B1a (1.067 ng/mL) caused 90% mortality of S. exigua larvae in foliar spray bioassays and topical application, making it more toxic than avermectin B1.
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).
(S)-Laudanosine is an alkaloid that can be found in poppies and is the S-enantiomer of Laudanosine. Laudanosine acts on the central nervous system and cardiovascular system, inhibiting low-affinity GABAreceptors with an IC50 value of 10 μM, and can cause seizures, hypotension, and bradycardia. Additionally, Laudanosine exerts analgesic effects by competitively binding to the opioid Mu-1 receptor (Ki = 2.7 μM) .
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 sulfone (Standard) is the analytical standard of Fipronil sulfone. This product is intended for research and analytical applications. 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).
CLH304a (compound 14) is a specific and noncompetitive GABABreceptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABABreceptor .
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.
6-Hydroxyflavone is an orally effective flavonoid compound. 6-Hydroxyflavone can inhibit LPS (HY-D1056) -induced NO production and has anti-inflammatory effects. 6-Hydroxyflavone promotes osteoblast differentiation by activating AKT, ERK 1/2 and JNK signaling pathways. 6-Hydroxyflavone has an inhibitory effect on bovine hemoglobin (BHb) glycosylation. 6-Hydroxyflavone has a kidney protective effect. In addition, 6-Hydroxyflavone enhances GABA-induced current through the Benzodiazepine sites of γ-aminobutyric acid (GABAA) receptors. 6-Hydroxyflavone shows a clear preference for α2 - and α3 - subtypes, which play an anti-anxiety role .
PNU-107484A is a GABAAreceptor ligand that exhibits target activity mechanisms dependent on α isoforms. In the α1β2γ2 subtype, PNU-107484A acts as a positive allosteric modulator, enhancing GABA-induced Cl - currents, while it inhibits the currents in the α3β2γ2 and α6β2γ2 subtypes. The half-maximal concentrations for the α1β2γ2, α3β2γ2, and α6β2γ2 subtypes are 3.1, 4.2, and 3.5 μM, respectively. PNU-107484A can be used as a probe to investigate the physiological roles of different α isoform subtypes .
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 152 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 .
(S)-Laudanosine is an alkaloid that can be found in poppies and is the S-enantiomer of Laudanosine. Laudanosine acts on the central nervous system and cardiovascular system, inhibiting low-affinity GABAreceptors with an IC50 value of 10 μM, and can cause seizures, hypotension, and bradycardia. Additionally, Laudanosine exerts analgesic effects by competitively binding to the opioid Mu-1 receptor (Ki = 2.7 μM) .
6-Hydroxyflavone is an orally effective flavonoid compound. 6-Hydroxyflavone can inhibit LPS (HY-D1056) -induced NO production and has anti-inflammatory effects. 6-Hydroxyflavone promotes osteoblast differentiation by activating AKT, ERK 1/2 and JNK signaling pathways. 6-Hydroxyflavone has an inhibitory effect on bovine hemoglobin (BHb) glycosylation. 6-Hydroxyflavone has a kidney protective effect. In addition, 6-Hydroxyflavone enhances GABA-induced current through the Benzodiazepine sites of γ-aminobutyric acid (GABAA) receptors. 6-Hydroxyflavone shows a clear preference for α2 - and α3 - subtypes, which play an anti-anxiety role .
Picrotoxinin (Standard) is the analytical standard of Picrotoxinin. This product is intended for research and analytical applications. Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor 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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