Catalog No.
Product Name
Application
Product Information
Citations
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GABA-AT Inhibitor
GABA-AT-IN-1 is a potent inhibitor of γ-aminobutyric acid aminotransferase (GABA-AT), leading to a significant increase in GABA levels in the brain. This compound effectively crosses the blood-brain barrier, making it a valuable tool for research in anticonvulsant therapies. GABA-AT-IN-1 may be utilized in studies aimed at understanding GABAergic modulation in neurological disorders. -
GABAA Receptor Modulator.
DOV51892 is a GABAA receptor modulator that specifically targets receptors containing the α1 subunit. It exhibits non-sedative anti-anxiety effects, making it a valuable tool for studying anxiety-related pathways. This compound is suitable for in-depth research on the functional roles of GABAA receptors in various biological contexts. -
GABA(A) Receptor Antagonist
Refisolone is a selective antagonist of the GABAA receptor, effectively inhibiting its activity. This compound plays a crucial role in research related to anxiety, sedation, and other neurological disorders by modulating inhibitory neurotransmission. Refisolone is valuable for studying the physiological and pharmacological effects of GABAA receptor modulation in various experimental models. -
GABAA Receptor Modulator
GMA-839 is a selective modulator of the γ-aminobutyric acid A receptor (GABAA) with an IC50 value of 230 nM. This compound demonstrates potent anxiolytic-like activity, exhibiting significant dose-dependent effects in various animal models, with an effective oral dosage of 1.6 mg/kg. Notably, GMA-839 has been shown to enhance punished responding in both squirrel monkeys and pigeons. These characteristics position GMA-839 as a valuable tool for research into anxiolytic drug development. -
GABAA Receptor Antagonist
GABAA receptor agent 2 TFA is a potent GABAA receptor antagonist that exhibits an IC50 of 24 nM in human α1β2γ2 GABAA-expressing tsA201 cells and a Ki of 28 nM in rat GABAA receptors. This compound selectively inhibits GABAA receptor activity without affecting four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3). It serves as a valuable tool for studying GABAA receptor-mediated pathways and exploring therapeutic interventions in neurological disorders. -
GABAA Receptor PAM
Brallobarbitone is a positive allosteric modulator of the GABAA receptor, enhancing its activity and potentiating inhibitory neurotransmission. This compound has been utilized in research focusing on β-cell dysfunction, providing insights into its role in glucose homeostasis and potential therapeutic strategies for diabetes. Its modulation of GABAA receptor activity may offer further understanding of neuroendocrine interactions and their implications in metabolic disorders. -
GABAA Receptors PAM
U-89843A is a positive allosteric modulator (PAM) of GABAA receptors. It enhances GABA-induced chloride ion currents specifically in the α1β2γ2, α3β2γ2, and α6β2γ2 subtypes. U-89843A exhibits notable antioxidant and sedative effects, making it a valuable tool for research into neurological and psychiatric disorders. -
RDLac Homo-Oligomers Antagonist
Isohyenanchin is an antagonist of RDLac homo-oligomers, demonstrating its potential in modulating synaptic activity. Additionally, it exhibits weak antagonistic properties against ionotropic GABA receptors. This compound may serve as a valuable tool for research into the pathways and mechanisms involving GABAergic signaling and RDLac-related functions in neurological studies. -
GABAB Receptor Modulator
BHF177 is a positive modulator of GABAB receptors, acting to attenuate the interaction between nicotine and the dopaminergic system in the brain. This modulation reduces the addictive properties associated with nicotine consumption. BHF177 is primarily utilized in research focused on smoking cessation and addiction therapies. -
GABA Receptor Agonist
Timelotem is a GABA receptor agonist belonging to the class of 1,2-cyclo1,4-benzodiazepines. It exhibits significant antipsychotic properties while providing sedative, anti-anxiety, and anti-convulsant effects through the enhancement of gamma-aminobutyric acid (GABA) activity. This compound is valuable for research applications related to schizophrenia and various other mental disorders. -
GABA Receptor Agonist
(S)-Baclofen hydrochloride is a selective GABAB receptor agonist that effectively crosses the blood-brain barrier and demonstrates oral bioactivity, with an IC50 of 1.77 μM for GABAB receptors and 1564 μM for GABAA receptors. This compound is primarily utilized in research focused on muscle disorders, including spasticity, providing insights into therapeutic strategies for modulating muscle tone and motor function. -
GABA Receptor Antagonist
(S)-3C4HPG is a GABA receptor antagonist that plays a crucial role in modulating neuronal excitability and synaptic transmission. This compound exhibits key biological activity in the study of neurological disorders, making it valuable for research applications focused on understanding the mechanisms of GABAergic signaling. -
GABA receptors Ligand
(-)-JM-1232 is a ligand for GABA A receptors that binds to the benzodiazepine binding site, leading to pronounced analgesic effects. This compound has shown significant efficacy in preclinical models, with CI50 values of 2.96 mg/kg for acute thermal stimuli, 3.06 mg/kg for mechanically induced pain, and 2.27 mg/kg for visceral pain. The potent analgesic properties of (-)-JM-1232 make it a valuable tool for research focused on pain mechanisms and the development of analgesic therapies. -
γ-GABAAR Antagonist
GABAA receptor agent 5 is a selective antagonist of the γ-GABAAR, exhibiting a high binding affinity with a Ki value of 0.020 µM. This compound demonstrates effective γ-GABAAR antagonistic activity while maintaining low cellular membrane permeability. It serves as a valuable tool for research investigating the roles of γ-GABAAR in neurological disorders and synaptic transmission studies. -
GABAA Receptor Modulator
GABAA receptor modulator-12 is a potent modulator of the GABAA receptor, specifically inhibiting anesthetic-induced desensitization of the GABAA α3β3γ2 subtype with an IC50 of 0.2 μM. This compound is effective in research applications related to central nervous system disorders, contributing valuable insights into neuropharmacology and therapeutic interventions. -
GABA Antagonist
Pipazethate hydrochloride is a potent GABA antagonist that demonstrates significant antitussive activity. This compound is utilized in research focusing on cough suppression mechanisms and provides valuable insights into the development of therapeutic interventions for related respiratory conditions. Its pharmacological properties make it a suitable candidate for studies exploring the modulation of GABAergic neurotransmission. -
GABAB Agonist
SKF 97541 is a potent and selective agonist of the GABAB receptor, which plays a crucial role in mediating inhibitory neurotransmission. This compound has demonstrated antiepileptic activity, making it a valuable tool for research in epilepsy models and investigations into GABAB receptor modulation. Its ability to induce hyperpolarization highlights its potential for studying synaptic transmission and neuroprotection in various neurological disorders. -
GABA Receptor Modulator
(Rac)-Acetoxyvalerenic acid is a derivative of valerenic acid serving as a GABA (A) receptor modulator, known for its potential sedative and sleep-enhancing properties. This compound demonstrates altered permeability across the blood-brain barrier relative to diazepam, suggesting that its transport mechanism may involve an unidentified pathway rather than conventional passive diffusion. Research applications include the investigation of sleep disorders and the exploration of novel sedative agents. -
GABAA1 Receptor Modulator
GABAA receptor agent 7 is a potent positive modulator of the GABAA1 receptor. It exhibits anticonvulsant activity both in vitro and in vivo while demonstrating low neurotoxicity. This compound is a valuable tool for research into epilepsy and related neurological disorders. -
GABA Receptor Antagonist
(-)-Securinine nitrate is an alkaloid that functions as a GABAA receptor antagonist. It plays a crucial role in modulating neurotransmission and has been utilized in research to study its effects on neurological pathways. This compound serves as a valuable tool for investigating the pharmacological potential of GABAergic signaling in various biological contexts. -
GABAA agonist
Anxiolytic/Nonsedative Agent-1 is a potent GABAA receptor agonist demonstrating selective affinity for various benzodiazepine receptors in bovine brain membranes, with inhibition constants (Kis) of 14, 121, and 239 nM for α1β2γ2, α2β2γ2, and α5β3γ2 subtypes, respectively. This compound exhibits selective efficacy for the α2 subunit in vitro and displays anxioselective effects in vivo, making it a valuable tool for research into anxiety-related disorders and potential therapeutics. -
GABA Receptor
AHN-683 is a potent ligand for the GABA receptor, specifically acting on the peripheral benzodiazepine receptor (BDR). This compound modulates GABAergic signaling, which plays a critical role in nervous system function. AHN-683 can be utilized in research applications aimed at understanding anxiety, neurodegeneration, and the therapeutic potential of benzodiazepine derivatives. -
GABAA agonist
Org20599 is a positive allosteric modulator and, at elevated concentrations, a direct agonist of the GABAA receptor, exhibiting an EC50 of 1.1 μM. This compound enhances GABAA receptor activity, contributing to the modulation of inhibitory neurotransmission. Org20599 is utilized in research exploring the effects of GABAergic signaling on various neurological conditions and for the investigation of anxiolytic and anticonvulsant properties. -
GABA Receptor Inhibitor
Tiagabine hydrochloride hydrate is a potent and selective inhibitor of GABA uptake, primarily targeting the GABA receptor. It demonstrates significant anticonvulsant activity, with IC50 values of 67 nM in synaptosomes, 446 nM in neurons, and 182 nM in glial cells for [3H]GABA uptake. This compound is widely utilized in research focused on epilepsy and related neurological disorders. -
GABA Receptor Modulator
Clazolam is a GABA receptor modulator that primarily influences the activity of gamma-aminobutyric acid (GABA) receptors. It exhibits significant biological activity in the central nervous system, making it valuable for research in neurological diseases and pharmacological studies related to anxiety and sleep disorders. Its modulatory effects on GABA receptors provide insightful avenues for exploring therapeutic interventions in neuropsychiatric conditions. -
GABA Receptor Ligand
Nitrazolam is a benzodiazepine compound that functions as a GABA receptor ligand. It may exert central nervous system depressant properties, including sedation, hypnosis, anxiolytic, and anticonvulsant effects. This compound is relevant for research applications focused on disorders associated with GABAergic dysfunction and the pharmacological exploration of benzodiazepine-related mechanisms. -
GABAAR Inhibitor
Org 21465 is a selective inhibitor of the GABA A receptor (GABA A R). It exhibits significant analgesic properties without inducing cardiovascular or respiratory depression, making it a valuable compound for pain research. This compound can be utilized in studies concerning the modulation of GABAergic neurotransmission and its effects on pain mechanisms in vivo. -
GABA Receptor Agonist
CGP44532 is a selective GABAB receptor agonist, exhibiting a geometric mean pEC50 value of 5.63 μM. It plays a crucial role in modulating inhibitory neurotransmission in the central nervous system. This compound is primarily utilized in research applications focusing on neuropharmacology and the exploration of GABAergic signaling pathways. -
GABA Receptor
COR627 is a positive allosteric modulator of the GABA receptor, designed to enhance GABAergic activity. It increases the affinity for GABA(B) receptors, as demonstrated through its effects on both GABA and baclofen stimulation in rat cortical membranes. In vivo studies indicate that COR627 can amplify the sedative and hypnotic effects of baclofen, even at doses that are otherwise ineffective without pretreatment, making it a valuable tool for research in neuropharmacology and psychotropic drug studies. -
GABAergic Antidepressant Drug
Fengabine is a GABAergic antidepressant that primarily targets GABA receptors to modulate neurotransmitter activity. It exhibits potent antidepressant properties, making it a valuable compound for investigating the pathophysiology of depression and the mechanisms underlying mood disorders. Research applications include studies on synaptic transmission, neural plasticity, and behavioral assessments in depression models. -
γ-GABAAR Antagonist
GABAA receptor agent 6 is a potent antagonist of the γ-GABAAR, exhibiting an inhibition constant (Ki) of 0.56 µM. This compound demonstrates significant γ-GABAAR antagonistic activity while maintaining low permeability across cellular membranes. It is suitable for research applications involving the investigation of GABAergic signaling and the modulation of inhibitory neurotransmission in various biological systems. -
Stable Isotope
γ-Aminobutyric acid-4,4-d2 is a deuterated form of γ-aminobutyric acid (GABA), a principal inhibitory neurotransmitter in the mammalian brain. This compound selectively binds to ionotropic GABA receptors (GABAA) and metabotropic receptors (GABAB), modulating synaptic transmission and neuronal excitability. The stable isotope labeling allows for advanced metabolic studies and tracing applications in neuropharmacology and neuroscience research. -
GABAA Receptor PAM
Xilmenolone is a positive allosteric modulator of the GABAA receptor, enhancing its activity and facilitating neurotransmission. This compound exhibits notable anxiolytic and sedative properties, making it a valuable tool in neuropharmacological research. Xilmenolone can be utilized to study the modulation of GABAergic signaling and its implications in various neurological disorders. -
GABA Receptor
Sch 50910 is a GABA(B) receptor antagonist that exhibits inhibitory effects on GABA(B) autoreceptors. At a concentration of 100 μM, Sch 50910 does not influence electrically stimulated neurotransmitter release. Its activity profile suggests limited utility in investigations focused on GABA(B) receptor function, making it a potential tool for exploring the complex dynamics of GABAergic signaling pathways. -
GABAA Receptor Modulator
Loreclezole hydrochloride is a selective modulator of the GABAA receptor, acting as a positive allosteric modulator for receptors containing the β2 or β3 subunits. This compound demonstrates significant antiepileptic activity, making it a valuable tool for researching epilepsy and related neurological disorders. Its capacity to enhance GABAergic transmission positions it as a potential therapeutic candidate in the development of treatments for seizure disorders and anxiety. -
GABA Receptor Agonist
Nerisopam is a potent agonist of the gamma-aminobutyric acid (GABA) receptor, demonstrating notable anxiolytic and antipsychotic properties. This orally active homophthalazine induces rapid expression of Fos-like immunoreactivity in key regions of the rat striatum, specifically the rostral, dorsomedial, and lateral areas. Researchers can utilize Nerisopam in studies focused on the modulation of anxiety and psychotic disorders, providing insights into GABAergic mechanisms and their implications in neuropsychiatric conditions. -
GABA Receptor
COR628 is a positive allosteric modulator of GABA(B) receptors, enhancing GABA-induced GTPγS stimulation. It demonstrates significant activity in vitro and has shown efficacy in mouse models by potentiating sedation and hypnosis induced by baclofen, leading to reduced onset time and prolonged loss of righting reflex. Additionally, COR628 exhibits a cytotoxic effect comparable to or greater than that of other known modulators, making it a valuable tool for research on GABAergic signaling and its implications in neurological studies. -
GABA Receptor Antagonist
CGP46381 is an orally active GABA receptor antagonist, exhibiting an IC50 of 4.9 μM. It effectively inhibits neuronal depression induced by the application of baclofen. This compound is useful for research applications involving the modulation of GABAB receptor activity and its effects on neuronal signaling. -
Peptide Ligand for GABARAP
K1 peptide is a high-affinity ligand for GABAA receptor-associated protein (GABARAP). It plays a crucial role in mediating protein interactions involved in cellular processes such as autophagy and synaptic transmission. K1 peptide is valuable for research applications focused on GABARAP function and its implications in neurobiology and cellular signaling pathways. -
nAChR/GABA Receptor Modulator
Spinosyn J functions as a non-competitive modulator of nicotinic acetylcholine receptors (nAChR) and γ-aminobutyric acid (GABA) receptors. It exhibits significant insecticidal activity, making it a valuable compound for the study of agricultural pests. This property positions Spinosyn J as a useful tool in entomological research and pest management strategies. -
GABAA Receptor Inverse Agonist
Terbequinil is a potent inverse agonist of the Gamma-aminobutyric acid A (GABAA) receptor, exhibiting significant oral bioavailability. This compound is valuable for investigations into the modulation of GABAA receptor activity and its implications in various nervous system disorders. Its ability to inhibit receptor signaling makes it a useful tool in exploring therapeutic approaches to conditions influenced by GABAA receptor dysfunction. -
Insecticide
Leporin A is an insecticide that primarily targets GABA receptors and sodium channels, disrupting neurotransmission in insects. This mechanism leads to paralysis and mortality, making Leporin A a potent agent for agricultural pest control. It is utilized in research focused on insect physiology and pest management strategies. -
GABA Receptor
CGP55845 is a potent and selective antagonist of the GABAB receptor, effectively blocking agonist binding. With an IC50 value of 5 nM, it demonstrates significant inhibition of GABA and glutamate release. The compound exhibits a high affinity for the GABAB receptor, with an apparent Kd of 30 nM. CGP55845 is comparable in potency to 100 μM CGP 35348 for reversing the inhibitory effects of (R)-(-)-baclofen, making it a valuable tool for research into GABAergic signaling and related physiological functions. -
GABAA Agonist
Org 20599 methanesulfonate is a selective agonist of the GABAA receptor, exhibiting an EC50 value of 1.1 μM. This compound plays a significant role in modulating inhibitory neurotransmission and is valuable for studying neurological disorders and related mechanisms. Its potent activity provides insights into the therapeutic potential of GABAA receptor modulation in various neurological contexts. -
GABA Receptor
AZD 3043 is a positive allosteric modulator of GABA(A) receptors, demonstrating sedative and hypnotic activity. This compound enhances GABA(A) receptor-mediated chloride currents in vitro and produces hypnotic effects along with electroencephalographic inhibitory activity in vivo. Its unique esterase-dependent metabolic pathway results in a short duration of action, allowing for rapid clearance, which may offer potential clinical applications in managing sleep disorders. -
GABAB Receptor Agonist
3-Aminopropylphosphinic acid (3-APPA) is a phosphonic analog of gamma-aminobutyric acid (GABA) that acts as a potent and selective agonist of the GABAB receptor. Its primary mechanism involves enhancing GABAB receptor signaling, which is crucial for modulating inhibitory neurotransmission in the central nervous system. 3-APPA is valuable for research applications focused on neurological disorders, synaptic transmission, and the pharmacological functions of GABAB receptors. -
GABAA Receptors PAM
U-89843A hydrochloride is a positive allosteric modulator (PAM) of GABAA receptors. It enhances GABA-induced chloride currents across the α1β2γ2, α3β2γ2, and α6β2γ2 subtypes, contributing to its biological activity. This compound also exhibits antioxidant and sedative effects, making it a valuable tool for research into neurological disorders and the modulation of inhibitory neurotransmission. -
Anti-anxiety Agent
HDZI 2,4OH is an effective anti-anxiety agent that operates primarily through GABA receptor modulation. This compound demonstrates a significant ability to penetrate the blood-brain barrier, making it suitable for neuropharmacological studies. Furthermore, HDZI 2,4OH exhibits low toxicity in zebrafish, allowing for safer in vivo investigations. It is a valuable reagent for research on neurological disorders, particularly anxiety disorders. -
GABA A Receptor Agonist
L-663581 is a partial agonist specifically targeting the GABA A receptor through the benzodiazepine receptor. This compound exhibits notable anxiolytic and sedative properties, making it valuable for research into neurological conditions and potential therapeutic applications for anxiety disorders. Its modulation of GABAergic neurotransmission provides insights into the mechanisms of action for anxiolytic agents. -
GABA A Agonist
Desalkylgidazepam is a metabolite of Gidazepam and functions as a GABA A receptor agonist. This benzodiazepine compound has been shown to enhance GABAergic transmission, making it useful in studies related to anxious behavior and neuropharmacology. Its ability to interact with the translocator protein (TSPO) further expands its potential applications in research on neuroprotective effects and psychiatric disorders.
