Catalog No.
Product Name
Application
Product Information
Citations
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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. -
GABA-AT Inhibitor
GABA-AT-IN-1 is a potent inhibitor of γ-aminobutyric acid aminotransferase (GABA-AT), leading to a significant increase in GABA levels in the brain. This compound effectively crosses the blood-brain barrier, making it a valuable tool for research in anticonvulsant therapies. GABA-AT-IN-1 may be utilized in studies aimed at understanding GABAergic modulation in neurological disorders. -
GABAA Receptor Modulator.
DOV51892 is a GABAA receptor modulator that specifically targets receptors containing the α1 subunit. It exhibits non-sedative anti-anxiety effects, making it a valuable tool for studying anxiety-related pathways. This compound is suitable for in-depth research on the functional roles of GABAA receptors in various biological contexts. -
GABA(A) Receptor Antagonist
Refisolone is a selective antagonist of the GABAA receptor, effectively inhibiting its activity. This compound plays a crucial role in research related to anxiety, sedation, and other neurological disorders by modulating inhibitory neurotransmission. Refisolone is valuable for studying the physiological and pharmacological effects of GABAA receptor modulation in various experimental models. -
GABAA Receptor Modulator
GMA-839 is a selective modulator of the γ-aminobutyric acid A receptor (GABAA) with an IC50 value of 230 nM. This compound demonstrates potent anxiolytic-like activity, exhibiting significant dose-dependent effects in various animal models, with an effective oral dosage of 1.6 mg/kg. Notably, GMA-839 has been shown to enhance punished responding in both squirrel monkeys and pigeons. These characteristics position GMA-839 as a valuable tool for research into anxiolytic drug development. -
GABAA Receptor Antagonist
GABAA receptor agent 2 TFA is a potent GABAA receptor antagonist that exhibits an IC50 of 24 nM in human α1β2γ2 GABAA-expressing tsA201 cells and a Ki of 28 nM in rat GABAA receptors. This compound selectively inhibits GABAA receptor activity without affecting four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3). It serves as a valuable tool for studying GABAA receptor-mediated pathways and exploring therapeutic interventions in neurological disorders. -
GABAA Receptor PAM
Brallobarbitone is a positive allosteric modulator of the GABAA receptor, enhancing its activity and potentiating inhibitory neurotransmission. This compound has been utilized in research focusing on β-cell dysfunction, providing insights into its role in glucose homeostasis and potential therapeutic strategies for diabetes. Its modulation of GABAA receptor activity may offer further understanding of neuroendocrine interactions and their implications in metabolic disorders. -
GABAA Receptors PAM
U-89843A is a positive allosteric modulator (PAM) of GABAA receptors. It enhances GABA-induced chloride ion currents specifically in the α1β2γ2, α3β2γ2, and α6β2γ2 subtypes. U-89843A exhibits notable antioxidant and sedative effects, making it a valuable tool for research into neurological and psychiatric disorders. -
RDLac Homo-Oligomers Antagonist
Isohyenanchin is an antagonist of RDLac homo-oligomers, demonstrating its potential in modulating synaptic activity. Additionally, it exhibits weak antagonistic properties against ionotropic GABA receptors. This compound may serve as a valuable tool for research into the pathways and mechanisms involving GABAergic signaling and RDLac-related functions in neurological studies. -
GABAB Receptor Modulator
BHF177 is a positive modulator of GABAB receptors, acting to attenuate the interaction between nicotine and the dopaminergic system in the brain. This modulation reduces the addictive properties associated with nicotine consumption. BHF177 is primarily utilized in research focused on smoking cessation and addiction therapies. -
GABA Receptor Agonist
Timelotem is a GABA receptor agonist belonging to the class of 1,2-cyclo1,4-benzodiazepines. It exhibits significant antipsychotic properties while providing sedative, anti-anxiety, and anti-convulsant effects through the enhancement of gamma-aminobutyric acid (GABA) activity. This compound is valuable for research applications related to schizophrenia and various other mental disorders. -
GABA Receptor Agonist
(S)-Baclofen hydrochloride is a selective GABAB receptor agonist that effectively crosses the blood-brain barrier and demonstrates oral bioactivity, with an IC50 of 1.77 μM for GABAB receptors and 1564 μM for GABAA receptors. This compound is primarily utilized in research focused on muscle disorders, including spasticity, providing insights into therapeutic strategies for modulating muscle tone and motor function. -
GABA Receptor Antagonist
(S)-3C4HPG is a GABA receptor antagonist that plays a crucial role in modulating neuronal excitability and synaptic transmission. This compound exhibits key biological activity in the study of neurological disorders, making it valuable for research applications focused on understanding the mechanisms of GABAergic signaling. -
GABA receptors Ligand
(-)-JM-1232 is a ligand for GABA A receptors that binds to the benzodiazepine binding site, leading to pronounced analgesic effects. This compound has shown significant efficacy in preclinical models, with CI50 values of 2.96 mg/kg for acute thermal stimuli, 3.06 mg/kg for mechanically induced pain, and 2.27 mg/kg for visceral pain. The potent analgesic properties of (-)-JM-1232 make it a valuable tool for research focused on pain mechanisms and the development of analgesic therapies. -
γ-GABAAR Antagonist
GABAA receptor agent 5 is a selective antagonist of the γ-GABAAR, exhibiting a high binding affinity with a Ki value of 0.020 µM. This compound demonstrates effective γ-GABAAR antagonistic activity while maintaining low cellular membrane permeability. It serves as a valuable tool for research investigating the roles of γ-GABAAR in neurological disorders and synaptic transmission studies. -
GABAA Receptor Modulator
GABAA receptor modulator-12 is a potent modulator of the GABAA receptor, specifically inhibiting anesthetic-induced desensitization of the GABAA α3β3γ2 subtype with an IC50 of 0.2 μM. This compound is effective in research applications related to central nervous system disorders, contributing valuable insights into neuropharmacology and therapeutic interventions. -
GABA Antagonist
Pipazethate hydrochloride is a potent GABA antagonist that demonstrates significant antitussive activity. This compound is utilized in research focusing on cough suppression mechanisms and provides valuable insights into the development of therapeutic interventions for related respiratory conditions. Its pharmacological properties make it a suitable candidate for studies exploring the modulation of GABAergic neurotransmission. -
GABAB Agonist
SKF 97541 is a potent and selective agonist of the GABAB receptor, which plays a crucial role in mediating inhibitory neurotransmission. This compound has demonstrated antiepileptic activity, making it a valuable tool for research in epilepsy models and investigations into GABAB receptor modulation. Its ability to induce hyperpolarization highlights its potential for studying synaptic transmission and neuroprotection in various neurological disorders. -
GABA Receptor Modulator
(Rac)-Acetoxyvalerenic acid is a derivative of valerenic acid serving as a GABA (A) receptor modulator, known for its potential sedative and sleep-enhancing properties. This compound demonstrates altered permeability across the blood-brain barrier relative to diazepam, suggesting that its transport mechanism may involve an unidentified pathway rather than conventional passive diffusion. Research applications include the investigation of sleep disorders and the exploration of novel sedative agents.
