Catalog No.
Product Name
Application
Product Information
Citations
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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. -
S-enantiomer of Padsevonil
(S)-Padsevonil is the S-enantiomer of Padsevonil, a potent antiepileptic agent that selectively targets presynaptic and postsynaptic sites. This compound exhibits a high affinity for synaptic vesicular protein 2 (SV2), enhancing neurotransmitter release. Additionally, (S)-Padsevonil functions as a positive allosteric modulator and partial agonist of GABA receptors, demonstrating significant activity against α1 and α5 subtypes. Its efficacy has been established in various rodent models, making it a valuable tool for research into epilepsy and related neurological disorders. -
GABA Antagonist
Pipazethate, a pyridobenzothiazine derivative, functions primarily as a GABA antagonist. It exhibits significant antitussive properties, making it a valuable reagent in the study of cough suppression. Research applications include investigations into the mechanisms of cough reflex modulation and potential therapeutic strategies for cough-related disorders. -
GABAA Receptors
(1S,3R)-3-Aminocyclopentane carboxylic acid is a selective modulator of GABAA receptors. This compound exhibits significant activity in enhancing GABAergic neurotransmission, making it valuable for studies focused on anxiolytic and sedative effects. Its unique structure allows for exploration in the context of neurological disorders and potential therapeutic applications in modulating inhibitory synaptic transmission. -
GABAA Receptor Agonist
MRK-623 is a potent GABAA receptor agonist with high affinity, exhibiting Ki values of 0.85 nM, 3.7 nM, 4.0 nM, and 0.53 nM for the α1, α2, α3, and α5 subtypes, respectively. This compound demonstrates significant anxiolytic effects, making it a valuable tool for research in anxiety disorders and related neurological studies. Its oral bioactivity further enhances its utility in pharmacological investigations. -
GABA Receptor Inhibitor
Sandaracopimaric acid is a diterpenoid that functions as a GABA receptor inhibitor. It exhibits significant anti-inflammatory properties and has been shown to reduce the contraction of phenylephrine-induced pulmonary arteries, with an EC50 value of 43.93 μM. This compound is useful for research applications in studying the modulation of GABAergic signaling and its effects on vascular tone. -
GABA Receptors Modulator
Delta3,5-cholestadien-7-one is an oxysterol that functions as a negative allosteric modulator of GABAA receptors. It effectively reduces GABA-induced currents in HEK cells expressing GABAA receptor subunits α1β1γ2 and α4β3γ2, with IC50 values of 1.5 µM and 1 µM, respectively. Additionally, Delta3,5-cholestadien-7-one attenuates GABA-induced depolarization in both peptidergic and non-peptidergic nociceptors, C-LTMRs, and cold thermosensors in isolated mouse dorsal root ganglion neurons, making it valuable for research on pain perception and sensory signaling. -
GABA Receptor Mimetic
Pregabalinum naproxencarbilum acts as a GABA receptor mimetic, exhibiting analgesic properties. This compound provides effective modulation of both inflammatory and neuropathic pain signaling pathways, making it a valuable tool for research focused on pain management and neurological disorders. Its unique mechanism supports investigations into nonopioid pain relief options. -
GABA Aminotransferase Inactivator
OV329 is a potent inactivator of GABA aminotransferase, functioning as an analogue of Vigabatrin. This compound effectively elevates brain GABA levels and mitigates abnormal intracerebral hyperexcitability. OV329 demonstrates significant anticonvulsant and antiepileptic properties, making it a valuable tool for the investigation of neurological disorders, including seizures. -
GABA receptor agonist
Arbaclofen placarbil is a transported proagent of the active R-isomer of baclofen, functioning primarily as a GABA receptor agonist. It exhibits significant biological activity by modulating GABAB receptor signaling, which is implicated in various neurological processes. This compound is utilized in research applications focused on neuromodulation, pain management, and the study of spasticity disorders. Its unique mechanism enhances the potential for therapeutic exploration in conditions related to GABAergic dysfunction. -
Stable Isotope
Acamprosate-d3 calcium is a deuterium-labeled form of Acamprosate calcium, a compound that acts as a GABA receptor agonist and modulates glutamatergic systems. This stable isotope is utilized in research to study the pharmacokinetics and dynamics of Acamprosate in various biological systems. Its unique labeling allows for precise tracking and analysis in metabolic studies and drug interaction investigations. -
Stable Isotope
Acamprosate-d6 calcium is a stable isotope-labeled form of Acamprosate calcium, functioning primarily as a GABA receptor agonist and modulating glutamatergic neurotransmission. This compound is crucial for research into alcohol dependence and withdrawal, as it helps investigate the biochemical pathways involved in these processes. The stable isotope labeling enhances the sensitivity and accuracy of analytical techniques, making it valuable for various pharmacological studies. -
GABAA Receptor Modulator
SB-205384 is a selective modulator of the GABAA receptor, influencing the dynamics of GABAA-activated currents. It primarily enhances the decay half-life of responses following agonist removal, making it a valuable tool for studying synaptic transmission and neuropharmacology. This compound is pertinent for research focused on the modulation of inhibitory neurotransmission and related neurological disorders. -
GABAA Receptor Inverse Agonist
TB-21007 is a potent inverse agonist targeting the α5 subunit of the GABAA receptor, exhibiting Ki values of 1.6 nM, 20 nM, 16 nM, and 20 nM for the α5, α1, α2, and α3 subtypes, respectively. This compound demonstrates significant brain penetration and is shown to enhance cognitive function in preclinical models, making it a valuable tool for research into cognitive disorders and neuropharmacology. Its selective action on α5-containing GABAA receptors positions it as a promising candidate for investigations into memory and learning. -
GABA Receptor Antagonist
SCH 50911 hydrochloride is a selective, orally-active antagonist of the γ-Aminobutyric acid B (GABA(B)) receptor, exhibiting competitive binding with an IC50 value of 1.1 μM. This compound effectively antagonizes GABA(B) autoreceptors, leading to an increase in electrically-stimulated 3H overflow at an IC50 of 3 μM. SCH 50911 hydrochloride is utilized in research applications related to neuropharmacology, particularly in studying the modulation of synaptic transmission and the role of GABA(B) receptors in various neurological disorders. -
GABA Receptor
ZK-91296 is a selective GABA receptor agonist known for its anxiolytic properties. This compound effectively reduces anxiety in animal models without inducing sedation, distinguishing it from traditional anxiolytics. ZK-91296 may selectively interact with specific benzodiazepine receptor subtypes, making it a valuable tool for research in anxiety disorders and the pharmacological investigation of GABAergic systems. -
Phenylpyrazole Insecticide
Flufiprole is a nonsystemic phenylpyrazole insecticide that targets the GABA receptor, disrupting neurotransmission in target pests. It demonstrates potent biological activity against a variety of insect species, making it effective for integrated pest management, particularly in rice fields. Flufiprole's mechanism of action offers a valuable tool for researchers studying pest control and insecticide efficacy. -
GABA Receptor
EF-1502 is a selective inhibitor of GABA transporters, specifically targeting GAT1 and BGT1. This compound demonstrates significant anti-epileptic activity, especially when combined with Tiagabine, enhancing seizure suppression. In contrast, co-administration with THIP resulted in reduced efficacy and dyskinesia, indicating a distinct mechanism of action. EF-1502 thus serves as a valuable tool for research into GABAergic modulation and its implications in epilepsy treatment strategies. -
GABA Transaminase Inactivator
CPP-115 is a GABA transaminase inactivator that selectively inhibits the enzyme, leading to increased GABA levels in the brain. This compound exhibits a higher affinity and reduced retinal toxicity compared to traditional options. CPP-115 is particularly useful in the investigation of drug addiction mechanisms and the treatment of infantile spasms, making it a valuable tool for neurological research applications. -
GABAB Antagonist
CGP36216 hydrochloride is a selective antagonist of the GABAB receptor, exhibiting a Ki value of 0.3 μM. This compound effectively inhibits presynaptic GABA signaling, making it a useful tool for investigating the role of GABAB receptors in anxiety and trauma-related disorders. Research applications include studying synaptic transmission and evaluating therapeutic strategies for related neurological conditions. -
GABA A Receptor Modulator
Necopidem is a GABA A receptor modulator that exhibits anxiolytic properties. This compound is utilized in research focused on neurological disorders, particularly anxiety-related conditions. Its mechanism of action enhances GABAergic transmission, making it a valuable tool for investigating the pathophysiology of anxiety and the development of novel therapeutic strategies. -
GABA Receptor
Flutazolam is a potent compound that primarily targets the GABA-A receptor, acting on benzodiazepine sites. It exhibits anxiolytic and sedative effects, making it useful in the study of anxiety disorders and other related conditions. This compound is valuable in biochemical research aimed at understanding the mechanisms of anxiety modulation and receptor interaction. -
GABA Receptor
Chlormethiazole (edisylate) is an allosteric modulator of GABAA receptors, functioning primarily as a sedative-hypnotic agent. Its mechanism enhances the inhibitory effects of GABA, contributing to its anxiolytic and anticonvulsant properties. This compound is widely utilized in research exploring neuropharmacology and the modulation of anxiety and sleep disorders. -
GABA Receptor Modulator
Inidascamine is a GABA receptor modulator that influences cholinergic and glutamatergic pathways. It exhibits potential biological activity relevant to the study of schizophrenia and related neuropsychiatric disorders. This compound serves as an important tool in research investigating the regulatory mechanisms of neurotransmitter receptors and their impact on cognitive function and behavior. -
GABAB Receptor Antagonist
GABAB receptor antagonist 2 is a selective antagonist of the GABAB receptor, inhibiting its function to modulate neurotransmission. This compound exhibits properties that may disrupt GABAergic signaling pathways and can be utilized in research focused on studying neurological disorders and synaptic plasticity. Its application extends to investigating the role of GABAB receptors in various physiological and pathophysiological processes. -
GABA Receptor Agonist
2'MeO6MF is a positive allosteric modulator targeting GABA receptors, specifically at the α2β1γ2L and all α1-containing GABAA receptors. This compound demonstrates direct agonistic activity on α2β2/3 and α2β2/3γ2L GABAA receptors, exhibiting anxiolytic effects and psychomotor stabilization. Additionally, 2'MeO6MF provides neuroprotective benefits, enhances functional recovery, and reduces stroke-induced inflammation, making it a valuable tool in neurological research applications. -
GABAA Antagonist
(+)-Bicuculline methochloride is a potent antagonist of the GABAA receptor, modulating inhibitory neurotransmission in the central nervous system. This compound alters neuronal membrane properties and firing patterns, leading to a reduction in Apamin-sensitive afterhyperpolarization. By inhibiting apamin-sensitive Ca2+-activated K+ currents, (+)-Bicuculline methochloride enhances burst firing, making it a valuable tool for studying synaptic transmission and neuronal excitability in various research applications. -
GABA Receptor Agonist
T-2000 (DMMDPB) is an orally active GABA receptor agonist that exhibits potent anticonvulsant properties. This compound enhances GABAergic transmission, making it a valuable tool for research into epilepsy and other neuropsychiatric disorders. T-2000 may also serve as a model for studying the therapeutic potential of GABA receptor modulation in various neurological conditions. -
Insecticidal Agent
GABA-IN-2 is a GABA receptor inhibitor that exhibits notable larvicidal activity. This compound demonstrates insecticidal effects, achieving mortality rates of 87% at a concentration of 50 mg/L. It is primarily utilized in research applications focused on pest control and the study of insect neurobiology. -
GABA Uptakp Inhibitor
Guvacine, a GABA uptake inhibitor derived from the nut of Areca catechu, selectively targets GABA transporters. It demonstrates potent inhibition of rat GAT-1, GAT-2, and GAT-3, with IC50 values of 39 μM, 58 μM, and 378 μM, respectively. This compound is instrumental in studies investigating GABAergic signaling and its implications in neurological research. Guvacine's properties make it a valuable tool for exploring therapeutic approaches for disorders linked to altered GABA uptake. -
GABA/mGAT2 Inhibitor
NNC 05-2090 is a GABA uptake inhibitor that primarily targets the β-GABA transporter (BGT-1) with an IC50 of approximately 10.6 μM, and exhibits potent inhibition of mGAT2 with a Ki value of 1.4 μM. This compound demonstrates anticonvulsant activity, making it a valuable tool for investigating epilepsy and other neurological conditions. Its effectiveness in modulating GABA transport provides insights into potential therapeutic strategies for neurological disorders. -
Anxiolytic Agent
Suriclone is a GABA receptor agonist that functions primarily as an anxiolytic agent. Exhibiting high affinity for benzodiazepine receptors, Suriclone effectively reduces anxiety-related behaviors. Its oral bioavailability makes it suitable for studies investigating the anxiolytic effects of GABA modulation in various biological contexts.
