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Catalog No.
Product Name
Application
Product Information
Citations
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Dihydropyrimidinase Inhibitor
Dihydromyricetin (Ampelopsin (flavanol); Ampeloptin) is a natural antioxidant with good prospects. -
GABA uptake inhibitor
SKF 89976A hydrochloride is a potent inhibitor of GABA uptake with IC50 of 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively. -
GABA transport inhibitor
(S)-SNAP5114 is a selective GABA transport inhibitor, with IC50 values of 5 μM and 21 μM for hGAT-3 and rGAT-2, respectively. (S)-SNAP5114 is an anticonvulsant drug. -
GABA uptake inhibitor
Guvacine hydrochloride inhibits GABA uptake (IC50 values are 14, 58, 119 and 1870 uM for hGABA T-1, rGABA T-2, hGABA T-3 and hBGT-1 respectively). -
GABA-transaminase inhibitor
Vigabatrin is a structural analog of the inhibitory neurotransmitter ??-aminobutyric acid (GABA) that irreversibly inhibits the catabolism of GABA by GABA transaminase. -
GABA reuptake inhibitor
Tiagabine is an anti-convulsive medication. The medication is also utilized in the treatment of panic disorder, as are a few other anticonvulsants. -
GABA transport system Inhibitor
Arecaidine is a potent inhibitor of the GABA transport system, impacting neurotransmitter uptake and signaling. It has been shown to inhibit the proliferation of oral mucosal fibroblasts, while also regulating cytokine secretion, specifically increasing IL-6, TGF-β, and TNF-α levels, and altering the expression of PPAR-γ and PCK1. Additionally, Arecaidine inhibits hPAT1-mediated proline uptake, making it a valuable tool for research into neurological diseases and related mechanisms. -
GABAA Receptor Chloride channel Inhibitor
Leptophos oxon is a potent GABAA receptor chloride channel inhibitor, exhibiting an IC50 value of 89.6 μM. This compound effectively inhibits GABA-induced chloride influx through binding to the TBPS sites associated with GABAA receptors, as well as inhibiting TBPS binding to voltage-dependent chloride channels. Leptophos oxon is primarily utilized in studies related to neurological diseases and functions as an insecticide, making it relevant for research in both neurobiology and pest management. -
GABA Receptor Inhibitor
Aminoxyacetic acid acts as an inhibitor of the GABA receptor by targeting the GABA-degrading enzyme GABA-T. Its primary mechanism disrupts the metabolism of gamma-aminobutyric acid, leading to increased GABA levels. This compound is valuable for research studies investigating GABAergic signaling, neuropharmacology, and the modulation of neurotransmitter dynamics in various models of neurological disorders. -
GABA Uptake Inhibitor
Nipecotic acid is a potent inhibitor of GABA uptake in neurons and glial cells, significantly impacting GABAergic neurotransmission. This compound has also been shown to directly activate GABAA-like chloride channels, with an effective concentration (EC50) of approximately 300 μM. Its biological activity makes nipecotic acid valuable for research applications focused on GABAergic signaling and associated neurological processes. -
GABA/mGAT2 Inhibitor
NNC 05-2090 hydrochloride is a potent inhibitor of GABA uptake, specifically targeting the β-GABA transporter (BGT-1) with an IC50 value of 10.6 μM, and exhibiting inhibitory activity against mGAT2 with a Ki of 1.4 μM. This compound demonstrates anticonvulsant properties, making it valuable for research in epilepsy and other neurological disorders. Its unique mechanism allows for exploration of GABAergic signaling pathways and therapeutic interventions in related conditions. -
GABA Transaminase Inhibitor
γ-Acetylenic GABA hydrochloride is an irreversible inhibitor of GABA transaminase, effectively increasing GABA levels in the brain. This compound is utilized in studies investigating the modulation of neurotransmitter systems and has applications in neuropharmacology. Additionally, γ-Acetylenic GABA hydrochloride serves as a click chemistry reagent, featuring an alkyne functional group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules. -
GABAA Receptor Inhibitor
FG 7142 is a non-selective inverse agonist of the GABAA receptor, exhibiting high affinity for the α1 subunit (Ki = 91 nM). It effectively modulates GABA-induced chloride flux at GABAA receptors containing the α1 subunit (EC50 = 137 nM). Additionally, FG 7142 has been shown to enhance tyrosine hydroxylation and upregulate β-adrenoceptors in the mouse cerebral cortex, making it valuable for research in neuropharmacology and the study of anxiety-related disorders. -
β1-containing GABAA Inhibitor
SCS (Salicylidene salicylhydrazide) is a selective allosteric inhibitor of β1-containing GABAA receptors, exhibiting a potency with an IC50 of 32 nM against the α2β1γ1θ subtype as determined by VIPR measurement. In addition to its inhibitory effects, SCS demonstrates metal ion chelation properties. This compound is valuable for research applications investigating GABAA receptor modulation and the role of metal ions in neuropharmacology. -
GABA Inhibitor
DL-Gabaculine hydrochloride is an irreversible inhibitor of bacterial pyridoxal phosphate-linked γ-aminobutyric acid-α-ketoglutaric acid transaminase, with a Ki of 2.86 μM. This neurotoxin effectively disrupts GABA metabolism, leading to increased levels of γ-aminobutyric acid in biological systems. It is utilized primarily in research applications focused on neuropharmacology and the study of neurotransmitter regulation. -
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. -
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. -
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 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. -
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 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. -
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 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 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. -
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. -
GABA Receptor Inhibitor
Tiagabine hydrochloride hydrate is a potent and selective inhibitor of GABA uptake, primarily targeting the GABA receptor. It demonstrates significant anticonvulsant activity, with IC50 values of 67 nM in synaptosomes, 446 nM in neurons, and 182 nM in glial cells for [3H]GABA uptake. This compound is widely utilized in research focused on epilepsy and related neurological disorders. -
GABAAR Inhibitor
Org 21465 is a selective inhibitor of the GABA A receptor (GABA A R). It exhibits significant analgesic properties without inducing cardiovascular or respiratory depression, making it a valuable compound for pain research. This compound can be utilized in studies concerning the modulation of GABAergic neurotransmission and its effects on pain mechanisms in vivo. -
GABA-AT Inhibitor
GABA-AT-IN-2 is an inhibitor of GABA aminotransferase (GABA-AT) with an IC50 of 19.8 μM. This compound has demonstrated significant antianxiety effects in preclinical models, making it a valuable tool for investigating anxiety-related neurotic disorders. Its application in research may provide insights into therapeutic strategies for managing anxiety. -
GABA Uptake Inhibitor
CI-966 is a highly selective, orally active inhibitor of the GABA transporter GAT-1, with exceptional brain penetration. It displays IC50 values of 0.26 μM for human GAT-1 and 1.2 μM for rat GAT-1, demonstrating over 200-fold selectivity against GAT-2, GAT-3, and BGT-3. CI-966 is recognized for its anticonvulsant and neuroprotective properties, making it a valuable tool for neuropharmacological research. -
GABAA Inhibitor
AA29504 is an ethyl carbamate that functions as a GABAA receptor inhibitor. It effectively blocks the transmission of gamma-aminobutyric acid (GABA), a key neurotransmitter in the central nervous system, leading to its potential applications in the study of anxiety, insomnia, and other neuropsychiatric disorders. This compound serves as an important tool for researchers investigating GABAA receptor-mediated pathways and their role in various neurological conditions. -
GABA Receptor Inhibitor
CP-457920 is a potent GABA receptor inhibitor with a Ki value of approximately 1 ng/mL. This compound is primarily utilized in neurological research, particularly for studying pathways and mechanisms underlying diseases such as Alzheimer's disease. Its inhibitory action on GABA receptors makes it a valuable tool for investigating neuropharmacological processes and potential therapeutic interventions. -
GABA Receptor Inhibitor
DPNI-GABA is a nitroindoline derivative that selectively inhibits GABA(A) receptors, significantly decreasing GABA-evoked peak responses with an IC50 value of 0.5 mM. This compound serves as a valuable tool for researching the role of GABAergic signaling in various physiological and pathological processes, contributing to studies of neuronal excitability and synaptic transmission. Its inhibition of GABA(A) receptors makes it essential for elucidating mechanisms of action in neuropharmacology and related fields. -
GABA Receptor Inhibitor
SKF 89976A is a selective GABA transporter (GAT-1) inhibitor, displaying an IC50 of 0.28 μM for GAT-1 and significantly higher IC50 values of 137.34 μM and 202.8 μM for GAT-2 and GAT-3, respectively, in CHO cells. This compound is primarily utilized in neurological research focusing on the modulation of GABA neurotransmission. Its specificity for GAT-1 makes it a valuable tool for studying GABAergic signaling and related disorders. -
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. -
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. -
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.
