Catalog No.
Product Name
Application
Product Information
Citations
- 6-Hydroxyflavone is an orally active flavonoid with diverse pharmacological properties. It exhibits anti-inflammatory activity by inhibiting lipopolysaccharide (LPS)-induced nitric oxide (NO) production and also promotes osteoblast differentiation through activation of the AKT, ERK1/2, and JNK signaling pathways, supporting its role in bone health. Additionally, 6-Hydroxyflavone inhibits the glycosylation of bovine hemoglobin (BHb), suggesting potential in managing glycation-related complications. It demonstrates kidney-protective effects and modulates GABAergic neurotransmission by enhancing GABA-induced currents via the benzodiazepine binding sites on GABAA receptors
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GABAB Receptor Negative Allosteric Modulator
CLH304a (compound 14) is a selective and noncompetitive negative allosteric modulator (NAM) of the GABA$_B$ receptor. It specifically targets the heptahelical domain of the GB2 subunit, inhibiting receptor activity with inverse agonist properties. CLH304a reduces GABA-induced inositol trisphosphate (IP₃) production with an IC₅₀ of 37.9 μM and does not affect other Class C GPCRs, including mGluR1, mGluR2, and mGluR5, indicating high selectivity. Additionally, CLH304a inhibits Baclofen-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABA$_B$ receptors, further supporting its function as a negative modulator. This compound is a valuable tool for investigating GABA$_B$ receptor function and holds potential for therapeutic research in neurological disorders involving GABAergic signaling dysregulation. -
Stable Isotope
Primidone-d5 is a deuterium-labeled analog of Primidone, primarily known for its inhibitory action on the transient receptor potential melastatin 3 (TRPM3) channel, with an IC50 value of 0.6 μM. This reagent also inhibits receptor-interacting protein (RIP) kinase and voltage-gated sodium channels, while acting as an antagonist at the GABA receptor. Primidone-d5 is valuable for research in pain management and seizure disorders, enabling studies focused on its analgesic and anticonvulsant properties. -
GABAA Receptor Agonist
Cipepofol is a positive allosteric modulator and direct agonist of the GABAA receptor. This compound demonstrates significant central nervous system inhibition and promotes sleep, offering potential applications in anesthesia and sleep research. Additionally, Cipepofol activates the Sirtuin1 (Sirt1)/Nrf2 pathway, providing cardioprotective effects against isoproterenol-induced myocardial infarction by reducing oxidative stress, inflammatory responses, and cardiomyocyte apoptosis. -
GABA Receptor Modulator
α-Thujone is a monoterpene that acts as a reversible modulator of the GABA type A receptor, with an IC50 of 21 μM for inhibiting GABA-induced currents. This compound demonstrates significant anti-tumor activity by inducing reactive oxygen species (ROS) accumulation, as well as promoting cell apoptosis and autophagy. Additionally, α-Thujone exhibits antinociceptive, insecticidal, and anthelmintic properties, while being capable of crossing the blood-brain barrier, making it valuable for various biological research applications. -
GABAB Receptor Negative Allosteric Modulator
(E/Z)-CLH304a is a negative allosteric modulator of the GABAB receptor, consisting of a mixture of (E)-CLH304a and (Z)-CLH304a. This compound selectively inhibits the GABAB receptor and noncompetitively modulates its activity. Research has demonstrated that (E)-CLH304a is effective in blocking Baclofen-induced ERK1/2 phosphorylation in HEK293 cells that overexpress GABAB receptors, making it a valuable tool for studies investigating GABAB receptor signaling pathways and their implications in neurological disorders. -
GABA(A) Receptor Antagonist/σ1 Receptor Agonist
Dehydroepiandrosterone sulfate (DHEA sulfate) functions as a GABA(A) receptor antagonist and a σ1 receptor agonist. This neurosteroid, primarily secreted by the adrenal gland, is capable of partially penetrating the blood-brain barrier. It inhibits GABA(A) receptor-mediated chloride influx while enhancing NMDA receptor activity via σ1 receptor interaction, displaying anti-inflammatory and antidepressant properties. DHEA sulfate is relevant for research in neuroprotection, depression, post-traumatic stress disorder (PTSD), and Alzheimer’s disease, and may serve as a biomarker for cardiovascular disease mortality due to its correlation with mortality rates. -
GABA(A) Receptor Antagonist/σ1 Receptor Agonist
Dehydroepiandrosterone sulfate sodium (DHEA sulfate) primarily acts as a non-competitive GABA(A) receptor antagonist and σ1 receptor agonist. This neurosteroid, predominantly secreted by the adrenal gland, has demonstrated significant biological activities, including enhancing NMDA receptor function and exerting anti-inflammatory and antidepressant effects. DHEA sulfate sodium can penetrate the blood-brain barrier, making it valuable in research applications related to neuroprotection, neurite growth regulation, and neuropsychiatric disorders such as depression, post-traumatic stress disorder (PTSD), and Alzheimer's disease. Additionally, it may serve as a biomarker for cardiovascular disease mortality, with its levels inversely correlated with mortality rates. -
GABAA/BZ Receptor Agonist
(E)-3,4,5-Trimethoxycinnamic acid is a potent GABAA/BZ receptor agonist characterized by multiple methoxy substitutions on its cinnamic acid structure. This compound demonstrates significant biological activity, including anticonvulsant and sedative effects, making it a valuable tool in research related to insomnia, headaches, and epilepsy. Additionally, (E)-3,4,5-Trimethoxycinnamic acid exhibits favorable binding affinity to the 5-HT2C and 5-HT1A receptors, with IC50 values of 2.5 and 7.6 μM, respectively, supporting its potential in neuropharmacological studies. -
GABAA Activator
Valerenic acid is a sesquiterpenoid that acts as a positive allosteric modulator of GABAA receptors, particularly enhancing the function of receptors containing the β3 subunit. Its anxiolytic properties are primarily mediated through this modulation. Additionally, Valerenic acid serves as a partial agonist at the 5-HT5a receptor and exhibits significant antioxidant activity, making it valuable in research related to anxiety disorders and oxidative stress. -
GABAB Receptor Positive allosteric modulator
ADX71441 is an orally active positive allosteric modulator of the GABAB receptor, capable of crossing the blood-brain barrier. With an EC50 of 96 nM, it enhances the effect of endogenous GABA, while also functionally inhibiting adenosine transporters and the 5-HT2B receptor. ADX71441 demonstrates a range of biological activities, including anxiolytic, analgesic, muscle relaxant, and hypothermic effects. Additionally, it reduces acute locomotor activity, decreases the voluntary intake of alcohol and saccharin, mitigates stress-induced neuronal activation, and exhibits anti-hyperalgesic properties, making it a valuable tool for research in neuropharmacology and related fields. -
GABA Receptor Activator
2'-O-Methylisoliquiritigenin is a GABA receptor activator that enhances neurotransmitter activity across various pathways, including serotonin (5-HT), norepinephrine (NE), dopamine (DA), and GABA. Isolated from the Arachis species, this compound plays a significant role in modulating nervous system functions and offers valuable insights for research applications related to neurochemistry and pharmacology. Its selective influence on neurotransmitter pathways makes it a useful tool for studying neuropharmacological mechanisms. -
GABA transport system Inhibitor
Arecaidine is a potent inhibitor of the GABA transport system, impacting neurotransmitter uptake and signaling. It has been shown to inhibit the proliferation of oral mucosal fibroblasts, while also regulating cytokine secretion, specifically increasing IL-6, TGF-β, and TNF-α levels, and altering the expression of PPAR-γ and PCK1. Additionally, Arecaidine inhibits hPAT1-mediated proline uptake, making it a valuable tool for research into neurological diseases and related mechanisms. -
Anti-tumor Agent
Scoulerine hydrochloride is a multi-target inhibitor primarily acting as an anti-tumor agent. It disrupts the PI3K/Akt/mTOR signaling pathway and α1D-adrenergic receptors, leading to microtubule destabilization, cell cycle arrest, and apoptosis in cancer cells. This compound also inhibits mitochondrial dehydrogenase activity and demonstrates effects on GABA receptors and BACE1, suppressing tumor cell proliferation, migration, invasion, and stem cell-like properties. Additionally, Scoulerine hydrochloride exhibits pharmacological activities against Plasmodium falciparum, as well as antibacterial, antiemetic, and antitussive properties, while also influencing endoplasmic reticulum stress and mitochondrial function. It is particularly relevant in studies focused on leukemia, ovarian cancer, and colorectal cancer. -
GABAA Receptor Modulator
6-Methoxyflavanone is a flavonoid compound that acts as a positive allosteric modulator of GABAA receptors, specifically enhancing the activity of human recombinant α1β2γ2L and α2β2γ2L subtypes. This compound is capable of crossing the blood-brain barrier and demonstrates key biological activities including anti-anxiety effects, analgesic properties, and relief from neuropathic pain. Additionally, 6-Methoxyflavanone exhibits inhibitory activity towards bitter receptor hTAS2R39 and hTAS2R14, providing a reversible antagonistic effect. Its unique profile makes it a valuable tool for research in neuroscience and pharmacology. -
Alkaloid
(S)-Laudanosine is an alkaloid with a primary action on the central nervous system and cardiovascular system. It inhibits low-affinity GABA receptors, exhibiting an IC50 value of 10 μM and has the potential to induce seizures, hypotension, and bradycardia. Additionally, (S)-Laudanosine demonstrates analgesic properties through competitive binding to the opioid Mu-1 receptor, with a binding affinity characterized by a Ki value of 2.7 μM. This compound is valuable for research into neurological and cardiovascular functions. -
LTD4/PAF Receptor Antagonist
CP-96021 is a potent antagonist of the leukotriene D4 (LTD4) receptor (Ki = 34 μM) and the platelet activating factor (PAF) receptor (Ki = 37 μM). This compound effectively targets two key inflammatory mediators, making it valuable in research on inflammation-related pathologies. With a high specificity profile, CP-96021 demonstrates negligible activity against various receptors, including dopamine, adenosine, and GABA receptors, suggesting minimal off-target effects. This reagent can be employed in studies investigating the pathogenesis of inflammatory diseases, such as asthma. -
Drug Metabolite Control
4-Hydroxypentanoate sodium is an active metabolite of gamma-Valerolactone, functioning primarily as a sedative. Its primary mechanism involves modulation of GABA receptors, leading to enhanced inhibitory neurotransmission. This compound is utilized in pharmacological research to study drug metabolism and to evaluate sedative effects in various experimental models. -
Drug Metabolite Control
7-Bromo-5-(2-fluorophenyl)-1,3-dihydro-3-hydroxy-2H-1,4-benzodiazepin-2-one is a primary metabolite of Flubromazepam, acting on the central nervous system through modulation of GABA receptors. This compound exhibits potential anxiolytic and sedative properties, making it relevant for studies on drug metabolism and pharmacokinetics. Its application is beneficial in research focused on benzodiazepine derivatives and their metabolic pathways. -
GABA/Glutamate-gated Chloride Channel Potentiator
4''-Oxoavermectin B1a is a potent modulator of GABA (γ-aminobutyric acid) and glutamate-gated chloride channels, exhibiting significant insecticidal and acaricidal properties. This compound demonstrates efficacy in disrupting neurological processes in target pests, making it a valuable tool for research in agricultural pest management. Its application contributes to understanding the mechanisms of action in pest control strategies. -
GABAA Receptor Chloride channel Inhibitor
Leptophos oxon is a potent GABAA receptor chloride channel inhibitor, exhibiting an IC50 value of 89.6 μM. This compound effectively inhibits GABA-induced chloride influx through binding to the TBPS sites associated with GABAA receptors, as well as inhibiting TBPS binding to voltage-dependent chloride channels. Leptophos oxon is primarily utilized in studies related to neurological diseases and functions as an insecticide, making it relevant for research in both neurobiology and pest management. -
Stable Isotope
γ-Aminobutyric acid-d6 is a deuterium-labeled form of γ-Aminobutyric acid, a crucial inhibitory neurotransmitter in the mammalian central nervous system. This compound primarily targets ionotropic GABA receptors (GABAA) and metabotropic receptors (GABAB), playing a significant role in regulating neuronal excitability. It is useful in research applications focused on neurotransmitter dynamics, GABAergic signaling, and metabolic studies involving stable isotopes. -
GABA(A) Receptors Blocker
Bicuculline methiodide is a potent blocker of GABA(A) receptors, serving to inhibit GABA-mediated neurotransmission. By altering membrane properties and firing patterns, it effectively reduces Apamin-sensitive afterhyperpolarization, enhancing neuronal excitability. This compound is valuable for research applications focused on understanding the role of GABA(A) receptors in synaptic transmission and studying neuronal firing behaviors in various neurological models. -
GABAB Receptor Antagonist
Saclofen is a competitive antagonist of the GABAB receptor, exhibiting an IC50 value of 7.8 μM. It demonstrates weak antagonistic activity towards the GABAB1b and GABAB2 heterodimeric receptors. Saclofen effectively inhibits Baclofen binding to rat cerebellar membranes and blocks Baclofen-induced circadian phase shifts. Additionally, it has shown anti-inflammatory and analgesic effects in preclinical models. This makes Saclofen a valuable tool for investigating GABAB receptor functions and related biological processes. -
GABAB Receptor Antagonist
CGP35348 is a selective GABAB receptor antagonist exhibiting a central nervous system penetration with an EC50 of 34 μM. This compound specifically targets the GABAB receptor, demonstrating potential to enhance neuromuscular coordination and spatial learning in animal models, particularly following neonatal brain injury. Its unique mechanism offers a valuable tool for researching the effects of GABAB receptor modulation on cognitive functions and motor behavior. -
GABAB Receptor Antagonist
CGP55845 hydrochloride is a potent and selective antagonist of the GABAB receptor, exhibiting an IC50 of 6 nM. This compound is valuable in neurological research, providing insights into GABAergic signaling pathways and their implications in various neurological disorders. Researchers use CGP55845 hydrochloride to investigate the role of GABAB receptors in synaptic transmission and neuronal excitability. -
GABA Receptor
17β-Estradiol sulfate sodium is a neuroactive steroid that acts as a modulator of the GABA receptor. This compound exhibits significant biological activity by influencing neurotransmission and neuroprotection, making it useful in research related to neuropharmacology and hormone signaling. Its applications include studying the effects of estrogens on the central nervous system and investigating potential therapeutic targets for neurological disorders. -
GABAA Receptor Modulator
AZD7325 is a potent and orally active partial positive allosteric modulator (PAM) of the GABAA receptor, specifically targeting the α2 and α3 subtypes (Ki=0.3 nM and 1.3 nM, respectively), while exhibiting reduced antagonistic activity at the α1 and α5 subtypes. It serves as a valuable tool for research applications related to anxiety disorders and Dravet syndrome. Additionally, AZD7325 acts as a moderate inducer of CYP1A2 and a potent inducer of CYP3A4 in vitro, making it relevant for studies on drug metabolism and interactions. -
GABA Receptor Activator
Alpha-Asarone (α-Asarone) acts as a GABA receptor activator, demonstrating significant antidepressant-like activity in preclinical mouse models. This compound is of interest in neuropharmacology research for its potential effects on mood regulation and anxiety disorders. Its mechanism may provide insights into novel therapeutic approaches for treating depression and related conditions. -
GABA Receptor Inhibitor
Aminoxyacetic acid acts as an inhibitor of the GABA receptor by targeting the GABA-degrading enzyme GABA-T. Its primary mechanism disrupts the metabolism of gamma-aminobutyric acid, leading to increased GABA levels. This compound is valuable for research studies investigating GABAergic signaling, neuropharmacology, and the modulation of neurotransmitter dynamics in various models of neurological disorders. -
GABAA Agonist
Clomethiazole is a potent, orally active GABAA agonist that enhances inhibitory neurotransmission within the central nervous system. This compound exhibits anticonvulsant properties, making it particularly relevant for the treatment of convulsive status epilepticus. Additionally, Clomethiazole has been shown to inhibit cytochrome P450 isoforms CYP2A6 and CYP2E1 in human liver microsomes, which may impact metabolic pathways relevant to drug interactions in pharmacological studies. -
GABAA Receptor Antagonist
Bicuculline (methochloride) is a selective antagonist of the GABAA receptor, exhibiting an IC50 value of 3 μM. This compound is known to induce clonic-tonic convulsions in mammals and is also capable of blocking Ca2+-activated potassium channels. Bicuculline (methochloride) is utilized in research focused on epilepsy and related psychiatric disorders, providing valuable insights into neuronal excitability and inhibitory transmission. -
GABA Receptor Antagonist
L-Allylglycine is an amino acid derivative that acts as a GABA receptor antagonist through the inhibition of glutamate decarboxylase (GAD), consequently reducing GABA biosynthesis in the brain. This compound exhibits convulsant activity, making it a valuable tool in neurological research. L-Allylglycine is utilized to study the roles of GABAergic signaling in various physiological and pathological conditions. -
GABAA PAM
Darigabat is a selective positive allosteric modulator (PAM) targeting GABAA receptors, specifically the α2, α3, and α5 subtypes. This compound exhibits high affinity for GABAA receptors with K_i values of 2.9 nM for α2 and 21 nM for α3, while demonstrating significantly lower affinity for α4 and α6 subunits. Darigabat effectively penetrates the blood-brain barrier and possesses anxiolytic properties, indicating its potential use in treating conditions such as anxiety and epilepsy. -
GABA Uptake Inhibitor
Nipecotic acid is a potent inhibitor of GABA uptake in neurons and glial cells, significantly impacting GABAergic neurotransmission. This compound has also been shown to directly activate GABAA-like chloride channels, with an effective concentration (EC50) of approximately 300 μM. Its biological activity makes nipecotic acid valuable for research applications focused on GABAergic signaling and associated neurological processes. -
Stable Isotope
γ-Aminobutyric acid-d2 is a deuterium-labeled form of γ-Aminobutyric acid, a critical inhibitory neurotransmitter in the mammalian central nervous system. It functions by binding to both ionotropic GABA receptors (GABAA) and metabotropic GABA receptors (GABAB), playing a vital role in neuronal signaling and modulation. This stable isotope is particularly useful in research applications involving metabolic tracing, pharmacokinetics, and the study of neurochemical pathways. -
GABA Receptor Antagonist
CGP 54626 hydrochloride is a potent and selective antagonist of the GABAB receptor, exhibiting an IC50 value of 4 nM. This compound is valuable in research aimed at elucidating the role of GABAB receptors in various neurological signaling pathways. Its use can enhance the understanding of GABAB receptor-mediated mechanisms in both normal physiology and pathological conditions. -
GABABR Agonist
Baclofen hydrochloride is a selective agonist of the metabotropic GABAB receptor (GABABR). This lipophilic derivative of γ-aminobutyric acid (GABA) mimics GABA's action, inducing presynaptic inhibition and facilitating muscle relaxation. With its ability to penetrate the blood-brain barrier effectively, Baclofen hydrochloride is valuable for research applications focused on muscle spasticity and neurological disorders. -
GABA Agonist
Piperidine-4-sulfonic acid is a potent GABA agonist targeting GABA receptors, exhibiting an IC50 of 0.034 μM for the inhibition of H-GABA binding. This compound is valuable in research applications involving neuropharmacology and the study of GABAergic neurotransmission, providing insights into potential therapeutic strategies for neurological disorders. -
α5-GABAAR Antagonist
Afizagabar (S44819) is a selective antagonist of the GABA-binding site at the α5-GABA receptor subtype, displaying an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. This compound has been shown to enhance synaptic plasticity within the hippocampus, thus demonstrating potential pro-cognitive effects. Afizagabar serves as a valuable tool for research focused on cognitive enhancement and the modulation of GABAergic signaling pathways. -
GABA Receptor Activator
Kavain is a kavalactone derived from Piper methysticum, primarily acting as a GABA receptor activator. This compound has demonstrated anxiolytic effects in both animal and human studies. Its ability to positively modulate the gamma-aminobutyric acid type A (GABAA) receptor makes it relevant for research into anxiety disorders and related neurological conditions. -
GABA/mGAT2 Inhibitor
NNC 05-2090 hydrochloride is a potent inhibitor of GABA uptake, specifically targeting the β-GABA transporter (BGT-1) with an IC50 value of 10.6 μM, and exhibiting inhibitory activity against mGAT2 with a Ki of 1.4 μM. This compound demonstrates anticonvulsant properties, making it valuable for research in epilepsy and other neurological disorders. Its unique mechanism allows for exploration of GABAergic signaling pathways and therapeutic interventions in related conditions. -
GABAB Receptor Antagonist
Phaclofen is a selective GABAB receptor antagonist primarily acting on both central and peripheral systems. This compound is instrumental for research into the physiological roles of baclofen-sensitive and bicuculline-insensitive GABA receptors. Its diverse applications in neuropharmacology make it valuable for studies aimed at understanding GABAergic signaling and related physiological processes. -
GABAA PAM
(2S)-6-Prenylnaringenin is a potent positive allosteric modulator of the GABAA receptor, specifically targeting the α+β binding interface. It demonstrates significant biological activity within the forebrain, enhancing inhibitory neurotransmission. This compound is valuable for research applications focused on neuroscience, particularly in the study of anxiety, neuroprotection, and the modulation of synaptic transmission. -
GABA Transaminase Inhibitor
γ-Acetylenic GABA hydrochloride is an irreversible inhibitor of GABA transaminase, effectively increasing GABA levels in the brain. This compound is utilized in studies investigating the modulation of neurotransmitter systems and has applications in neuropharmacology. Additionally, γ-Acetylenic GABA hydrochloride serves as a click chemistry reagent, featuring an alkyne functional group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules. -
GABAA Receptor Inhibitor
FG 7142 is a non-selective inverse agonist of the GABAA receptor, exhibiting high affinity for the α1 subunit (Ki = 91 nM). It effectively modulates GABA-induced chloride flux at GABAA receptors containing the α1 subunit (EC50 = 137 nM). Additionally, FG 7142 has been shown to enhance tyrosine hydroxylation and upregulate β-adrenoceptors in the mouse cerebral cortex, making it valuable for research in neuropharmacology and the study of anxiety-related disorders. -
GABA Receptor Modulator
TPA-023B is an orally active partial agonist at the GABAA receptor α2 and α3 subtypes, with affinities of 0.73 nM and 2 nM, respectively, while acting as an antagonist at the α1 subtype with a Ki of 1.8 nM. This compound exhibits non-sedating anxiolytic-like properties, making it a valuable tool for research into anxiety disorders and GABAergic signaling. Its selective modulation of specific GABA receptor subtypes allows for nuanced studies on neuropharmacological effects. -
GABAA Receptor Agonist
Isonipecotic acid is a GABAA receptor partial agonist that modulates inhibitory neurotransmission in the central nervous system. Its biological activity includes the potential to enhance GABAergic signaling, making it a valuable tool for studying anxiety, seizure disorders, and other neurophysiological processes. This compound is applicable in research focused on developing therapeutic strategies for CNS-related conditions. -
GABA Receptor Antagonist
L-Allylglycine hydrochloride is an amino acid derivative that acts as a GABA receptor antagonist by inhibiting glutamate decarboxylase (GAD), thereby reducing GABA biosynthesis in the brain. This compound exhibits convulsant activity, making it a valuable tool for investigating the role of GABA in neurological disorders and for studying excitatory-inhibitory balance in neural circuits. Its applications extend to pharmacological research focused on seizures and related neurotransmission studies.
