Catalog No.
Product Name
Application
Product Information
Citations
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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. -
GABA Receptor Ligand
GABA-A Receptor Ligand-1 is a selective ligand for the GABA-A receptor, exhibiting a pKi of 7.27. This compound demonstrates significant neuroprotective effects, reducing mitochondrial dysfunction and promoting both neurite outgrowth and neuronal regeneration. Research applications include studies on ischemic stroke models in rats, highlighting its potential for therapeutic interventions in neurodegenerative conditions. -
GABA-AT Inhibitor
GABA-AT-IN-2 is an inhibitor of GABA aminotransferase (GABA-AT) with an IC50 of 19.8 μM. This compound has demonstrated significant antianxiety effects in preclinical models, making it a valuable tool for investigating anxiety-related neurotic disorders. Its application in research may provide insights into therapeutic strategies for managing anxiety. -
GABA Receptor Agonist
Propanidid is a γ-aminobutyric acid type A (GABAA) receptor agonist known for its short-acting properties as a non-barbiturate general anesthetic. This compound exhibits significant analgesic effects and can effectively lower arterial pressure. Propanidid is utilized in research applications focusing on pain management, sedation, and the modulation of vascular tone. -
GABAA PAM
LI-633 is a selective and orally active positive allosteric modulator (PAM) of the GABAA receptor, exhibiting a Ki value of 21 nM. This compound effectively potentiates GABA-induced inward currents, with EC50 values ranging from 8 nM for the α5β2γ2 subtype to 128 nM for α3β2γ2. Additionally, LI-633 enhances muscimol-induced GABAergic currents in rat dorsal root ganglion neurons, displaying an EC50 of 70.4 nM. This reagent is valuable for investigating mechanisms of visceral pain. -
GABAB Receptor Agonist
Lesogaberan napadisylate is a potent and selective agonist of the GABAB receptor, exhibiting an EC50 of 8.6 nM for human recombinant receptors. It demonstrates strong affinity for rat GABAB and GABAA receptors, with Kis values of 5.1 nM and 1.4 μM, respectively. This compound effectively inhibits transient lower esophageal sphincter relaxation, making it relevant for research into gastrointestinal disorders and neuromodulation. -
GABAA Positive Allosteric Modulator
Brexanolone caprilcerbate is a potent positive allosteric modulator of the GABAA receptor. This compound enhances GABAergic neurotransmission, promoting anxiolytic and sedative effects. It is primarily utilized in research focusing on mood disorders, epilepsy, and sleep regulation. -
Potassium Channel Opener
Flupirtine hydrochloride is a potassium channel opener (Kv7 activator) recognized for its analgesic and neuroprotective properties. This compound acts as a non-opioid analgesic while also antagonizing NMDA receptors and activating GABA receptors. Flupirtine hydrochloride enhances neuronal stability by reducing oxidative stress and calcium influx, thereby protecting neurons from excitotoxicity and ischemia. It is applicable in research focused on conditions such as focal cerebral ischemia, pain management, Alzheimer’s disease, and multiple sclerosis. -
GABAA Agonist
CP-615003 is a potent partial agonist of the GABAA receptor, exhibiting subtype-selectivity with a Ki value of 1.1 μM. This compound is converted into the active metabolite CP-900725 through oxidative deamination, which also shows affinity for the GABAA receptor. Additionally, CP-615003 is a substrate of P-glycoprotein, which may restrict its central nervous system penetration. It is primarily used in research related to CNS disorders and functions of the GABAA receptor. -
GABAergic System Modulator
Sodium bromide is a GABAergic system modulator that effectively reduces and blocks epileptiform discharges by enhancing inhibitory GABAergic functions. This compound increases the amplitude of inhibitory postsynaptic currents and paired-pulse inhibition, leading to pronounced anticonvulsant effects. Additionally, sodium bromide induces stimulation-induced extracellular alkalosis while sparing baseline pH levels and subsequent acidosis processes. It demonstrates species-specific pharmacokinetic characteristics and competes with chloride for renal tubular reabsorption, making it useful as a marker for extracellular fluid volume in research focused on epilepsy and related neurological conditions. -
GABA(A) Receptors Antagonist
Etbicyphat (Trimethylopropane phosphate) is a potent competitive antagonist of GABA(A) receptors. This compound is known to induce epileptiform activity in hippocampal CA1 neurons, making it an important tool for studying GABAergic signaling and its role in neuronal excitability. Etbicyphat also demonstrates binding affinity for GABA(A)-benzodiazepine receptors, facilitating research into neurological disorders and potential therapeutic interventions. -
GABA-mimetic Prodrug
Cholesteryl γ-aminobutyrate is a GABA-mimetic prodrug that targets GABA receptors in the central nervous system. It effectively inhibits orthodromically-evoked discharges in pyramidal cells located in the CA1 region of the hippocampus. This compound demonstrates dose-dependent suppression of locomotor activity in rodents and has been shown to inhibit Bicuculline-induced seizures in mice. Cholesteryl γ-aminobutyrate is valuable for research into CNS disorders associated with dysfunctional GABAergic signaling. -
GABA Receptor Agonist
5α-Androstan-3α-ol is a potent agonist of the γ-aminobutyric acid (GABA) receptor, influencing neurochemical signaling pathways. This compound has been shown to inhibit the transcriptional activity of the orphan nuclear receptor CAR (constitutive androstane receptor) by promoting its dissociation from coactivator proteins. 5α-Androstan-3α-ol is suitable for investigating nuclear receptor-mediated processes related to hormone metabolism and drug detoxification mechanisms in various biological systems. -
GABAB Receptor Antagonist
CGP36216 is a selective antagonist of the GABAB receptor, exhibiting a binding affinity with a Ki value of 0.3 μM. This compound is valuable in the study of anxiety and trauma-related disorders, allowing researchers to explore the roles of GABAB receptor modulation in these conditions. Its specificity makes it an important tool for investigating the therapeutic potential of GABAB receptor antagonism in various neuropsychiatric research applications. -
GABAA Receptor Agonist
Lorotomidate is a GABAA receptor agonist known for its anesthetic properties, exhibiting an ED50 of 2 mg/kg intravenously in KM mice, while demonstrating an LD50 of 46.5 mg/kg in the same model. This compound’s unique profile includes the ability to maintain corticosteroid secretion, which highlights its safety and efficacy. Lorotomidate is utilized in research to explore anesthetic mechanisms and neuro pharmacology, contributing to studies aimed at understanding GABAA receptor modulation. -
GABA Receptor Modulator
GABAA receptor agent 2 is a GABA receptor modulator that serves as a valuable tool for investigating the structure and orthosteric ligand binding of GABA(A) receptors. This compound aids in elucidating the binding mechanisms of orthosteric ligands, contributing to a deeper understanding of receptor functionality. The development of binding mode hypotheses through structure-activity relationships with homologous series of orthosteric GABA(A)R antagonists further enhances its application in pharmacological research. -
GABA Receptor Agonist
Divaplon is a GABA receptor agonist, exhibiting EC50 values of 31 nM for α3β2γ2 and 2 nM for α5β2γ2 subtypes. This compound demonstrates significant anxiolytic activity, making it valuable for research applications focusing on anxiety disorders and their underlying neurobiological mechanisms. Divaplon serves as a useful tool for studying GABAergic signaling and its effects on anxiety-related behaviors. -
GABAA1 Receptor Modulator
GABAA Receptor Agent 8 is a potent positive modulator of the GABAA1 receptor. It exhibits significant anticonvulsant activity both in vitro and in vivo, demonstrating low levels of neurotoxicity. This compound holds promise for research applications in the field of epilepsy and related neurological disorders. -
GABA Uptake Inhibitor
CI-966 is a highly selective, orally active inhibitor of the GABA transporter GAT-1, with exceptional brain penetration. It displays IC50 values of 0.26 μM for human GAT-1 and 1.2 μM for rat GAT-1, demonstrating over 200-fold selectivity against GAT-2, GAT-3, and BGT-3. CI-966 is recognized for its anticonvulsant and neuroprotective properties, making it a valuable tool for neuropharmacological research.
