Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
GABA Aminotransferase Inactivator
OV329 hydrochloride is a potent inactivator of GABA aminotransferase, an enzyme responsible for the degradation of GABA in the brain. By inhibiting this enzyme, OV329 hydrochloride effectively increases GABA levels, helping to mitigate abnormal intracerebral hyperexcitability. This compound demonstrates significant anticonvulsant and antiepileptic properties, making it a valuable tool for research into neurological disorders, particularly in the study of seizures. -
GABA Analogue
3-Amino-3-phenylpropionic acid is a structural analogue of GABA designed to interact with GABA receptors. This compound exhibits inhibitory properties against baclofen-induced gastric acid secretion, making it a valuable tool in gastrointestinal research. Its ability to modulate gastric function supports its use in studies focused on GABAergic signaling and related therapeutic applications. -
Zolpidem Precursor
Zolpidic acid serves as a crucial precursor in the synthesis of zolpidem, a widely utilized sedative-hypnotic agent. Its primary mechanism involves the modulation of GABA receptors, enhancing inhibitory neurotransmission in the central nervous system. This compound is essential for research applications focused on developing and studying sleep disorders and related pharmacological interventions. -
Anti-anxiety Agent
Triflubazam is an anti-anxiety agent that acts by modulating GABA receptors, leading to enhanced inhibitory neurotransmission. It exhibits significant anxiolytic properties and has potential applications in the study of sleep disorders and anxiety-related conditions. This compound is valuable for research aimed at elucidating the mechanisms underlying anxiety and developing therapeutic interventions. -
Midazolam Precursor
2-Amino-5-chloro-2'-fluorobenzophenone serves as a key precursor in the synthesis of Midazolam, a potent benzodiazepine. This compound is essential for the production of various derivatives used in pharmacological research and clinical applications. Its structure enables the exploration of interactions with GABA receptors, facilitating studies on sedative and anxiolytic effects. -
Gabapentinoid Compound
4-Fluoro phenibut hydrochloride is a Gabapentinoid compound that functions as a GABA analog, structurally resembling established nootropics. This compound has been shown to exhibit anxiolytic and nootropic effects, making it a valuable tool for research into cognitive enhancement and anxiety disorders. Its unique properties make it suitable for studying GABA receptor activity and related neurological pathways. -
GABA-Nortriptyline
BL-1021 free base is a conjugate of GABA and Nortriptyline, designed to target GABA receptors. This compound exhibits analgesic properties, making it beneficial in the treatment of pain. Its unique mechanism can support research into pain management and neuropharmacology. -
Capsaicinoid Analog
Nordihydrocapsaicin is a capsacinoid analog known for its pungent properties and oral bioactivity. This compound exhibits potential anti-cancer activities and is derived from both fresh and processed peppers. It may induce a burning sensation upon consumption, making it relevant for research in pain mechanisms and anti-tumor effects. -
Anesthesia Agent
Desflurane is a volatile anesthetic agent that functions primarily by enhancing the inhibitory effects of gamma-aminobutyric acid (GABA) at the GABA receptor, resulting in dose-dependent anesthesia. It is utilized in both surgical and diagnostic procedures requiring general anesthesia, offering rapid onset and recovery profiles. Additionally, desflurane is notable for its minimal metabolism, making it a valuable option in procedures requiring quick emergence from anesthesia. Its properties also make it suitable for studying the effects of anesthetics on neuronal activity. -
GABA(A) Agonist
Panadiplon is a partial agonist of the GABA(A) receptor, specifically targeting the 5GABA(A) subtype with notable selectivity over the 1GABA(A) subtype. This compound demonstrates significant anxiolytic properties and is employed in research applications related to anxiety disorders and other neuropharmacological studies. Its selective action makes Panadiplon a valuable tool for investigating the role of GABA(A) receptor subtypes in the central nervous system. -
GABAA/NMDA Receptor Modulator
Creatinine acts as a GABAA and NMDA receptor modulator, demonstrating antioxidant properties and metabolic regulation. It is produced through the non-enzymatic conversion of creatine and phosphocreatine in muscle, making its serum levels an important biomarker for renal function, muscle mass, and clinical outcomes. Creatinine is utilized in evaluating perioperative renal risk and has applications in research on neurodegenerative diseases, psychiatric disorders, acute and chronic kidney injury, and renal failure. Additionally, it can induce specific Cryptococcus species to produce creatinine deiminase, highlighting its role in metabolic studies. -
GABAR Antagonist
Songorine is a blood-brain barrier-permeable diterpenoid alkaloid that acts as a GABAA receptor antagonist. It exhibits notable anti-cancer, anti-arrhythmic, and anti-inflammatory properties, making it a compound of interest in several therapeutic areas. Research indicates its potential application in the treatment of epithelial ovarian cancer (EOC), underscoring its relevance in oncology studies. -
GABA Receptor Activator
6'''-Feruloylspinosin is a flavonoid that acts as a GABA receptor activator. Isolated from the seeds of Ziziphus jujuba, it is capable of crossing the blood-brain barrier and enhancing the expression of GABAAα1, GABAAα5, and GABABR1 mRNA in rat hippocampal neurons. This compound is valuable for research focused on neurological disorders and the modulation of GABAergic signaling pathways. -
GABAA Receptor Antagonist
Thiocolchicoside is a competitive antagonist of the γ-aminobutyric acid type A (GABAA) receptor, and acts as a glycine receptor agonist within the central nervous system. This semisynthetic sulfur derivative of colchicoside exhibits muscle relaxant properties, along with significant anti-inflammatory and analgesic effects. Thiocolchicoside is valuable in research for its potential applications in studying neuromuscular relaxation and pain management. -
Drug Derivative
Bornyval is a chemical derivative of valerian, primarily targeting the modulation of GABA receptors. It exhibits sedative and anxiolytic properties, making it valuable for research applications focused on neuropharmacology and the study of sleep disorders. Bornyval can facilitate the investigation of potential therapeutic strategies for anxiety and related conditions. -
Anticonvulsant Agent
CHF-2993 is an orally active anticonvulsant agent that functions primarily through the antagonism of GABA receptor modulators, specifically Bicuculline and Picrotoxin, to inhibit tonic convulsions in murine models. It shows no effect on Pentylenetetrazole-induced clonic convulsions but partially decreases Veratridine-induced aspartate efflux in rat cortical synaptosomes. CHF-2993 serves as a valuable tool in the investigation of epilepsy and related neurological disorders.
