Catalog No.
Product Name
Application
Product Information
Citations
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GABA-T Inhibitor
D-DABA is an enantiomeric form of L-DABA that acts as a weak inhibitor of GABA transaminase (GABA-T). Its inhibitory potency is approximately one-twentieth that of the L-isomer in reducing GABA uptake. This compound is useful in research applications involving GABA metabolism and neurotransmitter modulation. -
GABAA Receptor Antagonist
Golexanolone is a GABAA receptor antagonist that modulates steroid activity. This compound demonstrates significant effects on reducing peripheral inflammation and neuroinflammation, contributing to enhanced cognitive and motor functions in hyperammonemic rat models. Golexanolone serves as a valuable tool for investigating the mechanisms underlying neurological disorders and peripheral inflammation. -
GABAA receptor Positive Allosteric Modulator
Carbiphene is a positive allosteric modulator of the GABAA receptor. It inhibits [35S] TBPS binding while enhancing [3H] muscimol binding in rat forebrain membranes, targeting specific subsets of the GABAA receptor. This compound is valuable in research focused on schizophrenia and related neurological disorders. -
GABAA Receptor Positive Modulator
Androst-16-en-3-ol is a positive allosteric modulator of GABAA receptors, influencing neurotransmission in the central nervous system. This compound is known for its anxiolytic, antidepressant, and anticonvulsant properties, evidenced through behavioral studies in mice. Additionally, it serves as a pheromone, eliciting mating responses in estrous sows, and is present in human biological fluids such as urine and sweat. Its modulation of GABAA receptors positions Androst-16-en-3-ol as a significant reagent for investigating neuropharmacological mechanisms and exploring potential therapeutic applications. -
GABABR1 Receptor Agonist
(iodo-125)-CGP 71872 is a radiolabeled agonist of the GABABR1 receptor, featuring an azido group that allows for photoactivation. This compound is useful in studies aimed at characterizing GABAB receptors, facilitating investigations into their role in various neurological processes. Its specific targeting of GABAB receptors makes it a valuable tool for research in neuropharmacology and receptor signaling. -
GABA Receptor
Imagabalin is a compound that acts as a selective modulator of the GABA receptor, contributing to its potential in addressing neurological disorders. This reagent is instrumental in the study of conditions such as anxiety and epilepsy, where GABAergic signaling is disrupted. The synthesis of imagabalin not only produces the active compound but also characterizes key intermediates like 3-methylvaleryl chloride and 3-methylvaleric anhydride, providing valuable insights into the underlying reaction mechanisms in organic synthesis. -
GABA Receptor Ligand
Saripidem is a non-selective ligand for the ω modulatory sites of the GABA receptor. This compound exhibits anxiolytic and sedative properties by enhancing GABAergic neurotransmission. It is applicable in research focused on neuropharmacology, particularly in the study of anxiety, sleep disorders, and other neuropsychiatric conditions. -
GABA Receptor inverse agonist
Suritozole is an inverse agonist targeting the GABA receptor, specifically acting on benzodiazepine binding sites within GABAA ion channel complexes. This compound has demonstrated cognitive enhancement properties and is relevant in the investigation of neurodegenerative diseases. Research applications include studying the modulation of GABAergic neurotransmission and its implications in cognitive function and pathophysiology of neurological disorders. -
GABAAR Antagonist
GMQ is a competitive antagonist of the GABAergic receptor, primarily targeting the GABA(A) receptor subtypes α1β2, α1β2γ2, α4β2γ2, and α5β2γ2. This compound potently inhibits GABAAR activity, enhancing neuronal excitation by disrupting GABAergic transmission. Additionally, GMQ offers anti-histaminic effects within the enteric system, specifically inhibiting gastric acid secretion, making it valuable for research in neuropharmacology and gastrointestinal function. -
GABA Receptor Antagonist
GABAB receptor antagonist 3 is a potent inhibitor of the GABAB receptor, which plays a crucial role in neurotransmission and modulation of synaptic activity. This compound effectively blocks GABAB receptor signaling, making it valuable for studying the physiological and pathological roles of GABA in the central nervous system. Its applications include research into anxiety, epilepsy, and other neuropsychiatric disorders, providing insights into potential therapeutic interventions. -
GABAA Agonist
DS1 is a potent agonist of the GABAA receptor, enhancing its activity. This compound stimulates serum response element (SRE) and cAMP response element (CRE) promoters, leading to increased expression of luteinizing hormone beta (LHbeta) and follicle-stimulating hormone beta (FSHbeta) genes. DS1 is valuable for research applications focused on the modulation of GABAA receptor activity and its effects on hormone regulation. -
Tuclazepam
Tuclazepam is a benzodiazepine derivative primarily targeting the central nervous system to exert its anxiolytic and sedative effects. This compound is utilized in research focused on anxiety disorders and sleep-related studies due to its ability to modulate GABA receptor activity. Its significant calming properties make Tuclazepam an important reagent for investigating the neuropharmacological mechanisms underlying anxiety and sedation. -
GABAB Receptor Agonist
CGP47656 is a potent GABAB receptor agonist that selectively inhibits forskolin-stimulated adenylyl cyclase activity while enhancing noradrenaline-stimulated adenylyl cyclase activity. This compound is valuable for investigating the role of GABAB receptors in various neurological functions and diseases, offering potential insights into therapeutic strategies for brain function-related disorders. Its unique mechanism of action makes it a useful tool for researchers studying synaptic transmission and neuropharmacology. -
GABA Receptor Agonist
(R)-Baclofen hydrochloride is a selective agonist of the GABAB receptor. This compound is primarily utilized for its muscle relaxant properties and has been studied for its potential therapeutic effects in conditions such as spasticity and pain management. Its mechanism of action involves the modulation of neurotransmitter release, thereby influencing synaptic transmission and muscle tone. Research applications include neuroscience studies and investigations into GABAB receptor pathways. -
GABAB Receptor Antagonist
CGP 62349 is a selective GABAB receptor antagonist that exhibits oral bioactivity. This compound has been shown to enhance cognitive performance across various learning paradigms, making it a valuable tool in neuroscience research. Its application can provide insights into the modulation of cognitive processes and the therapeutic potential for cognitive impairments. -
GABA Antagonist
CGS-9895 is a GABA antagonist that functions by binding to the benzodiazepine site on GABA receptors. This compound selectively inhibits the activity of GABA, a major inhibitory neurotransmitter in the central nervous system. Its application in research includes studies on anxiety, depression, and seizure disorders, providing insights into the modulation of GABAergic signaling. -
GABAA receptors agonist
JY-XHe-053 is a selective agonist of GABAA receptors, particularly targeting those containing the α5 subunit, with an affinity of 0.7 nM. This compound demonstrates significant biological activity at GABAA receptors, particularly at the α2 and α3 subunits. Despite its potency, JY-XHe-053 exhibits minimal anti-anxiety activity, making it a valuable tool for investigating GABAA receptor function and the role of the α5 subunit in neurological research. -
GABAA Receptor Agonist
PF-0713 is a selective agonist of the GABAA receptor, which plays a crucial role in inhibitory neurotransmission within the central nervous system. This compound exhibits significant anxiolytic and anticonvulsant properties, making it valuable for research in neuropharmacology and potential therapeutic applications in anxiety disorders and epilepsy. PF-0713's mechanism of action can aid in understanding GABAA receptor modulation and its implications in various neurological conditions. -
GABAR RDL Antagonist
Chrodrimanin B is a potent antagonist of the GABA receptor RDL, primarily sourced from a fungal metabolite. It effectively inhibits GABA-mediated responses with an IC50 of 1.66 nM, demonstrating a peak current amplitude reduction at the RDL channel with an IC50 of 1.13 nM. This meroterpenoid compound exhibits significant insecticidal activity, making it a valuable tool in the study of insect neurobiology and potential pest control applications. -
GABAA Receptor Ligand
PNU-107484A is a selective GABAA receptor ligand with distinct activity across various α isoform subtypes. It functions as a positive allosteric modulator for the α1β2γ2 subtype, enhancing GABA-induced chloride currents, while exhibiting inhibitory effects on the α3β2γ2 and α6β2γ2 subtypes. The compound demonstrates half-maximal inhibitory concentrations of 3.1 μM for α1β2γ2, 4.2 μM for α3β2γ2, and 3.5 μM for α6β2γ2. PNU-107484A serves as a valuable tool for exploring the physiological implications of different GABAA receptor α isoform subtypes in research settings. -
GABA/nACh Receptor Inhibitor
APS3 is a potent inhibitor of GABA and nicotinic acetylcholine (nACh) receptors, showcasing a lethal concentration (LC50) of 7.2423 μg/mL against the pest Plutella xylostella. This compound is useful for studying neuropharmacological pathways and assessing the impact of receptor inhibition on insect behavior and survival. Applications include research in insect physiology and the development of pest management strategies. -
GABAA Receptor Antagonist
SKF 10810 is a GABAA receptor antagonist with an EC50 of 4.3 μM, demonstrating a notable capacity to inhibit GABAergic signaling. By disrupting GABA-mediated inhibition in reward pathways of the brain, SKF 10810 may have potential antidepressant effects. This compound serves as a valuable tool for research into neurological disorders and the mechanisms underlying mood regulation. -
GABA/GHBR Antagonist
NCS-382 is a potent antagonist of the GABA and GHBR receptors. It exhibits significant anticonvulsant and antisedative properties, making it a valuable reagent for studying neurological disorders. NCS-382 is primarily utilized in research related to hereditary nervous system diseases, providing insights into the mechanisms underlying these conditions. -
Benzodiazepine Agonist
Adinazolam mesylate is a triazolobenzodiazepine that functions as a benzodiazepine agonist. It exerts its biological activity by allosterically binding to peripheral-type benzodiazepine receptors, which modulate GABA receptor function. This compound demonstrates dual anxiolytic and antidepressant effects, making it a valuable tool in research focused on anxiety and depression-related pathways. -
Atagabalin Stereoisomer
iso-Atagabalin hydrochloride is a stereoisomer of Atagabalin, functioning primarily as a selective GABA (gamma-aminobutyric acid) receptor agonist. It is noted for its antianxiety effects, making it a valuable tool for research focused on anxiety disorders and related neurological conditions. This compound can aid in elucidating the mechanisms of GABAergic modulation in various biological contexts. -
GABA Receptor Modulator
SGE-516 is a neuroactive steroid functioning as a potent positive allosteric modulator of both synaptic and extra-synaptic GABAA receptors. This compound exhibits significant anticonvulsant activity, making it a valuable tool for research in neurological disorders, especially those related to GABAergic signaling. Its modulatory effects can provide insights into therapeutic strategies for epilepsy and other conditions characterized by altered GABA receptor function. -
GABA Aminotransferase Inhibitor
Gabaculine is a potent inhibitor of GABA aminotransferase, an enzyme responsible for the degradation of gamma-aminobutyric acid (GABA). This compound, derived from the microbial strain Streptomyces toyocaensis, effectively increases GABA levels, thereby modulating neurotransmission and exhibiting potential anxiolytic effects. Gabaculine is widely utilized in neurobiological research to study neurotransmitter dynamics and the role of GABA in various neurological disorders. -
GABAA Receptor Partial Agonist
ELB-139 is a GABAA receptor partial agonist known for its anxiolytic and anticonvulsant properties. This progesterone analogue modulates GABAA receptor activity, demonstrating significant effects on neurotransmitter levels, particularly enhancing extracellular serotonin (5-HT) in the striatum and medial prefrontal cortex of rodent models. ELB-139 holds potential for research applications related to anxiety disorders and seizure disorders. -
GABA Receptor
Epi-Aszonalenin A is a benzodiazepine fungal metabolite that targets the GABA receptor. It exhibits psychoactive properties, making it a valuable compound for studying the modulation of neurotransmission and its effects on behavior. This compound has potential applications in neuroscientific research related to anxiety, sedation, and other disorders associated with GABAergic signaling. -
GABA Receptor
Carburazepam is a benzodiazepine derivative that targets GABA receptors, enhancing the inhibitory neurotransmitter's effects within the central nervous system. Its primary biological activity includes anxiolytic and sedative properties, making it useful in research related to anxiety disorders and sleep disturbances. As a research reagent, Carburazepam provides valuable insight into the pharmacological mechanisms of benzodiazepines and their impact on neuronal signaling pathways. -
GABA Receptor
Suclofenide is an anticonvulsant compound that modulates GABA receptor activity, influencing GABA metabolism. It exhibits potential neuroprotective effects and has been utilized in research related to epilepsy and seizure disorders. Suclofenide serves as a valuable tool for investigating GABAergic signaling and its implications in various neurological conditions. -
GABA Receptor
CGP11952 is a triazolyl-benzophenone that acts as a positive allosteric modulator of the GABA receptor. This compound exhibits characteristics similar to benzodiazepines, contributing to its pharmacological profile. CGP11952 is primarily utilized in research to investigate GABAergic signaling and its implications in neurological disorders. -
GABA Receptor Agonist
Ro 41-3290 is a selective GABA receptor agonist, acting primarily as a partial agonist at the benzodiazepine site. This compound demonstrates potent biological activity in modulating GABAergic neurotransmission, making it valuable for research in the fields of neuropharmacology and anxiety disorders. Its mechanisms may provide insights into therapeutic approaches for conditions such as anxiety, insomnia, and seizure disorders. -
GABA Receptor Agonist
FG8119 is a novel benzodiazepine agonist that targets GABA receptors, enhancing their activity. This compound demonstrates significant anxiolytic and sedative effects, making it valuable for research in neuropharmacology and the study of anxiety disorders. FG8119 can be utilized to investigate the modulation of GABAergic neurotransmission and its implications in various neurological conditions. -
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. -
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. -
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. -
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. -
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. -
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.
