Catalog No.
Product Name
Application
Product Information
Citations
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δ-GABAA Receptor Positive Allosteric Modulator
DS2 is a selective positive allosteric modulator of the δ-GABAA receptor. This compound specifically enhances GABAergic responses mediated by the α4β3δ receptor while exhibiting minimal activity at α4β3γ2 and α1β3γ2 receptors. DS2 demonstrates significant analgesic properties and holds potential for research in sleep disorders, making it a valuable tool in neuropharmacology studies. -
GABAA Modulator
L-838417 is a selective partial agonist targeting the α2, α3, and α5 subtypes of the GABAA receptor while functioning as an antagonist at the α1 subtype. With binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM, and 2183 nM for various receptor subtypes, L-838417 exhibits significant anti-anxiety effects. This reagent is valuable for research on anxiety disorders and the modulation of GABAergic neurotransmission. -
GABAA Receptor Modulator
Tracazolate hydrochloride is a potent modulator of the GABAA receptor, specifically exhibiting selectivity towards the β3 subunit. It enhances GABAA receptor activity, demonstrating effective potentiation in α1β1γ2s (EC50=13.2 μM) and α1β3γ2 (EC50=1.5 μM) configurations. With its significant anxiolytic and anticonvulsant properties, Tracazolate hydrochloride serves as a valuable tool for research in neurological and psychiatric disorders, elucidating the role of GABAA receptor modulation in therapeutic contexts. -
GABAA Receptor PAM
α-Androstenol (5α-Androst-16-en-3α-ol) is a steroid pheromone that acts as a positive allosteric modulator of GABAA receptors, enhancing GABA-activated currents in primary mouse cerebellar granule cells with an EC50 of 0.4 μM. It exhibits anxiolytic-like, antidepressant-like, and anticonvulsant effects in murine models. This compound can be utilized in research focused on the mechanisms underlying seizures and related neurological disorders. -
GABA Receptor
ATPCA hydrochloride is a selective inhibitor targeting the GABA transporters BGT1, GAT1, and GAT3. It is utilized in biochemical studies to investigate GABAergic signaling and transport mechanisms. This compound plays a significant role in understanding the physiological and pathological processes related to GABA modulation, making it a valuable tool in neuropharmacology and drug discovery research. -
GABAA Receptor Agonist
ZK 93423 is a potent agonist of the GABAA receptor, belonging to the benzodiazepine class. It is characterized by its ability to enhance inhibitory neurotransmission, leading to sedative and anxiolytic effects. This compound is used in research to investigate the pharmacological profiles of GABAA receptor modulation and its potential therapeutic applications in anxiety and sleep disorders. -
GABA Receptor Agonist
3-Aminopropylphosphonic acid is a phosphonic acid analogue of gamma-aminobutyric acid (GABA) that functions as a GABAB receptor agonist. This compound exhibits significant biological activity by modulating neurotransmission through GABAB receptor activation. It is widely utilized in research focusing on neuropharmacology, particularly in studies related to anxiety, epilepsy, and other neurological disorders. -
GABA Receptor Activator
Cirsimaritin is a GABA receptor activator that exhibits weak binding to the benzodiazepine site on GABAA receptors. It demonstrates notable antidepressant, anxiolytic, and antinociceptive activities, making it a valuable tool for research in neuropharmacology. Its potential applications include the exploration of anxiety disorders, depression, and pain management pathways. -
GABA Uptake Inhibitor
Arecaidine hydrochloride is a pyridine alkaloid that acts as a potent GABA uptake inhibitor. By functioning as a substrate for the H+-coupled amino acid transporter 1 (PAT1, SLC36A1), it competitively inhibits the uptake of L-proline. This compound is valuable for research into GABAergic signaling and neuropharmacology, aiding in the exploration of neurological disorders and potential therapeutic interventions. -
Benzodiazepine Tranquilizer
Gidazepam is a benzodiazepine tranquilizer that acts as an agonist of GABA receptor channels (GABA RCs). It demonstrates significant anxiolytic and sedative properties, making it a valuable tool for studying anxiety disorders and neuropharmacology. Research applications include exploration of the mechanisms underlying GABAergic signaling and the development of therapeutic strategies for anxiety-related conditions. -
GABA Receptor Antagonist
6,2'-Dihydroxyflavone functions as a GABAA receptor antagonist, effectively inhibiting receptor activity. This compound exhibits potential neuroprotective effects and is being investigated for its role in neurological research, particularly in the context of anxiety, depression, and seizure disorders. Its unique structure and properties make it a valuable tool for studies exploring GABAergic signaling pathways. -
GABAB Receptor PAM
CGP13501 is a positive allosteric modulator of the GABAB receptor, enhancing its activity while facilitating gamma-aminobutyric acid (GABA) signaling. This compound serves as a structural analogue of propofol and is useful in research exploring the modulation of GABAB receptor-mediated pathways. CGP13501 may aid in studies related to neurotransmission, anxiety, and other central nervous system disorders. -
GABAB Agonist
(R)-4-Amino-3-hydroxybutyric acid is a GABAB receptor agonist that plays a significant role in modulating neurotransmission. Its interaction with GABAB receptors makes it a valuable tool for studying various neurological disorders and potential therapeutic pathways. This compound is instrumental in advancing research on the pharmacological aspects of the central nervous system. -
GABAC Receptor Antagonist
TPMPA is a selective antagonist of the GABAC receptor, exhibiting a binding affinity of KB = 2.1 μM. It does not significantly interact with GABAA or GABAB receptors, with binding constants of KB = 320 μM and EC50 = 500 μM, respectively. This compound is valuable in research focused on modulating orientation selectivity in ganglion cells, making it an important tool for exploring neural signaling mechanisms. -
GABA Aminotransferase Activator
3-Methyl-GABA is a potent GABA aminotransferase activator that enhances the activity of L-glutamic acid decarboxylase (GAD). This compound fits into the binding pocket of the GABAA receptor (GABAaR), facilitating the modulation of GABAergic signaling. 3-Methyl-GABA demonstrates anticonvulsant properties, making it a valuable reagent for research in neuropharmacology and the study of seizure disorders. -
GABA Uptake Inhibitor
Spinacine ((S)-Spinacine) functions as a GABA uptake inhibitor, increasing synaptic GABA availability by inhibiting its reuptake in cortical neuronal tissues. This compound effectively modulates reflex responses in isolated spinal cord preparations and decreases motor activity, as well as reducing exploratory behaviors in conflict situations, such as approaching water dispensers. Additionally, Spinacine elevates pain sensitivity thresholds when administered via subarachnoidal injection, making it valuable for research in neuropharmacology and pain modulation studies. -
GABAA Receptor Agonist
6-Aminonicotinic acid is a selective GABAA receptor agonist with a Ki value of 4.4 nM, demonstrating its potential for modulating neurotransmission. This compound exhibits diverse biological activities, including inhibition of protein synthesis and functioning as a vitamin B3 agonist. Additionally, it may play a role as a modulating agent in chemotherapy, making it a valuable tool for research in neuropharmacology and cancer therapeutics. -
GABA Uptake Inhibitor
CI-966 hydrochloride is a selective GABA uptake inhibitor targeting the GABA transporter GAT-1. With IC50 values of 0.26 μM for human GAT-1 and 1.2 μM for rat GAT-1, it demonstrates over 200-fold selectivity compared to GAT-2, GAT-3, and BGT-3. This compound possesses anticonvulsant and neuroprotective properties, making it a valuable tool in neurological research and potential therapeutic applications. -
GABA Receptor Modulator
7-Keto-DHEA is a modulator of the GABA receptor that has shown efficacy in reducing ethanol intake in rodent models. This compound is primarily investigated for its potential applications in studying alcohol dependence disorders, making it a valuable tool for research in addiction and neuropharmacology. -
GABA Receptor Antagonist
Pivagabine is a GABA receptor antagonist that acts as a hydrophobic derivative of 4-aminobutyric acid, exhibiting significant neuromodulatory properties. This compound effectively crosses the blood-brain barrier in rodent models, demonstrating its potential for central nervous system research. Pivagabine antagonizes the neuroactive effects triggered by foot shock, influencing GABAA receptor function and modulating corticotropin-releasing factor (CRF) concentrations in the rat brain, thus making it a valuable tool in studies related to stress responses and anxiety. -
Metabolite of Fipronil
Fipronil sulfone is a primary metabolite of the insecticide Fipronil, acting as a selective antagonist of GABA receptors. With an IC50 value of 175 nM, it effectively inhibits GABA receptor-mediated neurotransmission by displacing [3H]EBOB from its noncompetitive blocker site. This compound is important for research into neurotoxicology and the study of insect neurobiology. -
GABAA Receptor Ligand
Difludiazepam is a benzodiazepine derivative that acts as a ligand for the GABAA receptor, exhibiting an IC50 value of 4.1 nM. By binding to an allosteric site on the GABAA receptor, Difludiazepam enhances the receptor's responsiveness to GABA, thereby decreasing neuronal excitability. This compounds structural features include halogenated groups situated at the ortho position of its phenyl ring, making it a valuable tool for research focused on neurological function and disorders. -
GABAA PAM
PZ-II-029 is a GABAA positive allosteric modulator that selectively binds with high affinity to the α6β3γ2 receptor subtype. This compound exhibits significant biological activity in promoting anxiolytic and anti-migraine effects. It serves as a valuable tool for research into the neuropharmacology of anxiety disorders and migraine pathophysiology. -
GABA Analogue
1-Phenyl-2-pyrrolidinone is a phenyl analogue of gamma-aminobutyric acid (GABA) that exhibits sedative properties. It has been shown to reduce exploratory behavior in animal models, including rats at doses of 50-100 mg/kg (i.v.), and to inhibit emotional responses in dogs and cats. Additionally, 1-Phenyl-2-pyrrolidinone decreases pressor responses to emotional stress while not affecting the baroreceptor reflexes, making it a valuable tool for research on GABAergic signaling and emotional regulation. -
GABA Uptake Inhibitor
Guvacine hydrobromide is a potent GABA uptake inhibitor that specifically targets rat GABA transporters GAT-1, GAT-2, and GAT-3 with IC50 values of 39 μM, 58 μM, and 378 μM, respectively. This compound is derived from the nut of Areca catechu and plays a significant role in modulating GABAergic neurotransmission. Guvacine hydrobromide is particularly valuable for research applications focused on neuropharmacology and the exploration of GABA-related pathways in various physiological and pathological conditions. -
Anti-anxiety agent
Temgicoluril is an orally active anti-anxiety agent that targets GABA receptors to enhance GABAergic neurotransmission. Its primary mechanism involves modulating the inhibitory effects of GABA, leading to anxiolytic and potential antidepressant effects. This compound is valuable in research focused on anxiety disorders and the neurochemical pathways that influence mood regulation. -
GABAB PAM
COR659 is a potent positive allosteric modulator of GABAB receptors. It has been shown to effectively reduce self-administration of alcohol and chocolate in rat models, indicating its potential utility in studying addiction and reward behavior. This compound is valuable for researchers investigating the modulation of GABAB receptor activity and its implications in substance use disorders. -
GABA Antagonist
Anisatin, a non-competitive GABA antagonist, is derived from the seeds of Illicium anisatum. It effectively suppresses GABA-induced currents in a concentration-dependent manner, exhibiting an EC50 of approximately 1.10 μM. Anisatin is primarily utilized in research applications exploring GABAergic pathways and the modulation of neurotransmission. -
GABAA Receptor Agonist
TP003 is a non-selective agonist at the benzodiazepine site of the GABAA receptor, exhibiting EC50 values of 20.3 nM for α1β2γ2, 10.6 nM for α2β3γ2, 3.24 nM for α3β3γ2, and 5.64 nM for α5β2γ2. This compound demonstrates significant anxiolytic activity primarily through interaction with the α2 GABAA receptor subtype. TP003 is valuable for research into anxiety disorders and other neuropharmacological applications, providing insights into GABAA receptor-mediated anxiolysis. -
GABA Uptake Inhibitor
Arecaidine hydrobromide is a pyridine alkaloid that functions as a potent GABA uptake inhibitor. It acts as a substrate for the H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits the uptake of L-proline. This compound is utilized in research exploring GABAergic signaling and transport mechanisms, providing insights into neurological conditions and potential therapeutic strategies. -
GABA Receptor Activator
N-Arachidonyl-GABA is a novel lipoamino acid that acts as a GABA receptor activator. It has been identified in bovine brain and exhibits significant analgesic activity. This compound is valuable for research on pain modulation and GABAergic signaling pathways in various physiological contexts. -
GABAA Receptor Antagonist
Epiallopregnanolone (5α,3β-THDOC) is a neurosteroid that acts as an antagonist at GABAA receptors while enhancing NMDA receptor activity. This compound plays a significant role in modulating neurotransmission and has potential applications in neuropharmacology research, particularly in studies exploring anxiety, depression, and neurodegenerative disorders. Its unique mechanism of action makes it a valuable tool for understanding the complexities of synaptic transmission and receptor interactions in the central nervous system. -
GABA Receptor
CGS 8216 is a non-benzodiazepine ligand targeting the GABA receptor, exhibiting high affinity and specificity for rat forebrain membranes. This compound effectively inhibits 3H-flunitrazepam binding to rat synaptosomal membranes, demonstrating potent blocking of 3H-FLU labeling of brain benzodiazepine receptors in vivo, comparable to Diazepam. CGS 8216 is valuable for studying GABAergic signaling and the pharmacological properties of benzodiazepine receptors in neural research applications. -
GABAA Agonist
Cinazepam is a partial agonist of the GABAA receptor and belongs to the benzodiazepine class. It exhibits anxiolytic and sedative effects, making it a valuable tool in the study of sleep disorders and anxiety-related conditions. Research utilizing Cinazepam can provide insights into the modulation of GABAergic signaling and its implications for therapeutic applications. -
nAChR antagonist
Waglerin-1 is a 22-amino acid peptide that acts as a competitive antagonist of the muscle nicotinic acetylcholine receptor (nAChR). It effectively inhibits nAChR-mediated signaling, making it a valuable tool for studying neuromuscular transmission and muscle physiology. This peptide is utilized in various research applications, including the investigation of synaptic mechanisms and the development of therapeutic strategies for neuromuscular disorders. -
GABA Receptor Antagonist
NCS-382 sodium is a potent antagonist of the GABA receptor, exhibiting both anti-sedative and anti-hypnotic activities. This compound is valuable for research applications focused on neurological diseases, enabling investigations into the modulation of GABAergic neurotransmission and its implications for various neurological disorders. -
GABA Receptor Agonist
Thiomuscimol is a potent GABAA receptor agonist, with an IC50 value of 19 nM. This compound serves as a valuable tool for researchers investigating GABA binding sites by acting as a photoaffinity label for the purification and identification of components within the GABAA receptor complex. It is particularly useful in studies focused on neuropharmacology and the mechanisms of synaptic transmission. -
GABA Receptor Agonist
Ocinaplon is a partial agonist of the GABAA receptor, specifically functioning as a positive allosteric modulator with notable efficacy at the α1 subunit. This compound demonstrates potential anxiolytic effects, making it valuable for research in anxiety disorders and related neurological conditions. Its mechanism of action offers insight into therapeutic strategies targeting GABAergic pathways. -
GABAA Agonist
Pagoclone is a selective partial agonist of the GABA(A) receptor. It exhibits anxiolytic properties, making it relevant for research into the modulation of anxiety and panic disorders. Its unique profile allows for the investigation of GABAergic mechanisms in neurological research and pharmacological studies. -
GABA Receptor
(+)-Nipecotic acid is a GABA transport inhibitor that targets the GABA receptor, contributing to its potential antidepressant and anxiolytic effects. By increasing the concentration of GABA in the synaptic cleft, it enhances inhibitory neurotransmission. Research involving (+)-Nipecotic acid may offer insights for the development of novel therapeutic compounds aimed at treating psychiatric disorders. -
GABA Transaminase Inhibitor
γ-Acetylenic GABA serves as an irreversible inhibitor of GABA-transaminase, effectively elevating GABA levels in the rat brain. It is utilized in research to investigate the modulation of GABAergic neurotransmission. Additionally, γ-Acetylenic GABA features an alkyne group, making it suitable for click chemistry applications, particularly copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing substrates. -
GABA Transaminase Inhibitor
L-DABA hydrobromide is a GABA transaminase inhibitor, known for its ability to modulate gamma-aminobutyric acid (GABA) levels. With an IC50 greater than 500 μM, it demonstrates weak inhibition of this enzyme. Additionally, L-DABA has shown antitumor activity in both in vivo and in vitro studies, making it a valuable compound for research in cancer biology and neurochemical signaling. -
GABAAα3 Agonist
NS-2710 is a potent GABAAα3 receptor agonist, exhibiting a binding affinity with a Ki value of 9.2 nM. This compound is primarily utilized in research focused on anxiety disorders, investigating the role of GABAAα3 activation in modulating neurobehavioral responses. Its strong efficacy and selective targeting make it a valuable tool for pharmacological studies in the field of neurobiology. -
AChE Inhibitor/GABAA Receptor Antagonist
Bis(7)-tacrine dihydrochloride is a dimeric inhibitor of acetylcholinesterase (AChE) and a potent antagonist of GABAA receptors. This compound exhibits neuroprotective properties by preventing glutamate-induced neuronal apoptosis through NMDA receptor blockade. Bis(7)-tacrine dihydrochloride is valuable for research applications related to Alzheimer's disease and other neurological disorders. -
GABA(A) Receptor Inhibitor
MIDD0301 is a potent inhibitor of the γ-aminobutyric acid type A (GABA(A)) receptor, demonstrating significant biological activity as an anti-asthmatic agent. This compound effectively relaxes histamine-contracted airway smooth muscle in both guinea pigs and humans, making it relevant for research into bronchoconstrictive diseases. Furthermore, MIDD0301 has shown immunotoxicological safety in mice, exhibiting no adverse effects on lymphocyte, monocyte, or granulocyte populations with repeated dosing. -
GABA Receptor Activator
RuBi-GABA is a ruthenium-based caged GABA compound that targets GABA receptors. Upon excitation with visible light wavelengths, RuBi-GABA undergoes photocleavage, effectively releasing GABA. This compound facilitates GABA receptor-mediated currents, making it an invaluable tool for research applications in neuropharmacology and photophysiology to study synaptic transmission and neuronal activity. -
GABAA Receptor Agonist
ZAPA sulfate is a low-affinity agonist of the GABAA receptor. It effectively induces membrane hyperpolarization in Ascaris muscle cells, exhibiting an EC50 of 10.3 μM. This compound is valuable for research in neuropharmacology, particularly in studying the mechanisms of GABAergic signaling and its effects on muscle cell function. -
Benzodiazepine Agonist
Adinazolam is a triazolobenzodiazepine that functions as a benzodiazepine agonist. It binds to peripheral-type benzodiazepine receptors, which modulate GABA receptor activity through an allosteric mechanism. This compound exhibits both anxiolytic and antidepressant properties, making it valuable for research in anxiety and depression-related studies. -
GABAB Receptor Agonist
Lesogaberan is a potent and selective agonist of the GABAB receptor, exhibiting an EC50 of 8.6 nM for human recombinant GABAB receptors. This compound shows high affinity for rat GABAB receptors with a Ki value of 5.1 nM, while demonstrating a lower affinity for GABAA receptors at 1.4 μM. Lesogaberan is primarily utilized in research to investigate its effects on transient lower esophageal sphincter relaxation through its peripheral action, making it a valuable tool in studies related to gastrointestinal function and pharmacology. -
GABAA Receptor Ligand
GABAA receptor agent 1 is a high-affinity ligand that specifically targets the GABAA receptor. This compound exhibits potent anticonvulsant activity, making it valuable for research in epilepsy and seizure disorders. Its mechanism of action involves modulating neurotransmission, thereby influencing anxiety and various neurobehavioral conditions.
