Catalog No.
Product Name
Application
Product Information
Citations
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GABA Receptors PAM
3α,21-Dihydroxy-5α-pregnan-20-one is a positive allosteric modulator of GABAA receptors. This endogenous neurosteroid enhances the neuronal response to low levels of GABA, particularly at the α4β1δ subtype of GABAA receptors. It is pertinent in research applications related to neuropharmacology and the study of GABAergic signaling pathways. -
GABA Receptor
Rilmazafone hydrochloride is a selective ligand for the GABA receptor, specifically acting on the benzodiazepine site. This compound exhibits significant anxiolytic and sedative effects, making it valuable for research in neuropharmacology and the study of anxiety disorders. Its ability to modulate GABAergic neurotransmission renders it a useful tool for elucidating the mechanisms underlying anxiety and sleep regulation. -
GABA Receptor Activator
Homocarnosine TFA is a dipeptide comprised of γ-aminobutyric acid (GABA) and histidine, primarily found in the brain. As a GABA receptor activator, it functions as an inhibitory neuromodulator, demonstrating anticonvulsant properties. Additionally, Homocarnosine TFA exhibits antioxidant and anti-inflammatory activities, aids in the prevention of DNA damage, and inhibits the formation of advanced glycation end-products, making it relevant for various neurological research applications. -
GABAB Agonist
Phenibut hydrochloride is a GABA-B receptor agonist that exhibits anxiolytic and nootropic properties. By mimicking the action of GABA, it primarily influences GABAB receptor activity, thereby enhancing cognitive function and reducing anxiety. This compound is utilized in research focusing on neurological disorders, cognitive enhancement, and the study of anxiety mechanisms. -
GABAB Receptor Agonist
Lesogaberan hydrochloride acts as a potent and selective agonist for the GABAB receptor, exhibiting an EC50 of 8.6 nM for human recombinant GABAB receptors. It demonstrates high affinity for the rat GABAB and GABAA receptors, with Kis values of 5.1 nM and 1.4 μM, respectively. This compound is known to inhibit transient lower esophageal sphincter relaxation, making it a valuable tool in research related to gastrointestinal motility and related disorders. -
GABA Receptors Agonist
TACA, or trans-4-Aminocrotonic acid, is a potent agonist of GABAA and GABAC receptors, exhibiting a dissociation constant (KD) of 0.6 μM. Additionally, TACA acts as a GABA uptake inhibitor and serves as a substrate for GABA-transaminase (GABA-T). Its unique properties allow for the production of late biphasic responses in MPG neurons, making it valuable for research into GABAergic signaling and pharmacological interventions targeting these receptors. -
GABAA Antagonist
(-)-Bicuculline (methobromide) is a potent antagonist of the GABAA receptor. By inhibiting GABAA receptor activity, it modifies neuronal membrane properties and alters firing patterns. Furthermore, (-)-Bicuculline (methobromide) attenuates Apamin-sensitive afterhyperpolarization, facilitating burst firing by suppressing the small conductance Ca2+-activated K+ current. This compound is valuable for research applications in neurophysiology and the study of synaptic transmission. -
GABA Receptor Agonist
Progabide is a gamma-aminobutyric acid (GABA) receptor agonist that enhances GABAergic neurotransmission. It exhibits significant anxiolytic and anticonvulsant properties, making it valuable in neuroscience research. Progabide is commonly used to study the role of GABA in neurological disorders and to explore therapeutic interventions for epilepsy and anxiety-related conditions. -
GABA(A) Receptor Agonist
MK-0343 is an orally bioavailable partial agonist selective for the GABA(A) receptor subtype. This compound exhibits anxiolytic properties without sedation, making it a valuable tool for neurological research. MK-0343 is utilized in studies involving anxiety disorders and the modulation of neurotransmitter systems, contributing to the understanding of therapeutic approaches for related conditions. -
GABA Receptor Agonist
3,4,5-Trimethoxycinnamic acid is a phenylpropanoid known to act as a GABA receptor agonist. This compound has demonstrated anti-stress effects and is capable of prolonging sleep duration in animal models. Furthermore, 3,4,5-Trimethoxycinnamic acid increases the expression of GAD65 and the γ-subunit of the GABAA receptor, with no significant impact on the levels of α- and β-subunits. This makes it a valuable reagent for research into sleep regulation and stress response mechanisms. -
GABAA α5 Receptor PAM
Alogabat is a positive allosteric modulator (PAM) of the GABAA α5 receptor, specifically targeting the α5β3γ2 subunit with a Ki of 8.7 nM. It enhances the expression of this receptor subtype in oocytes, increasing levels by 1.97-fold. Alogabat is useful in research into cognitive impairment linked to various central nervous system disorders, including Alzheimer's disease, schizophrenia, and dementia. Its role in modulating GABAA receptors makes it relevant for studying conditions such as mild cognitive impairment and age-related cognitive decline, as well as elucidating mechanisms underlying neuropsychiatric disorders. -
GABA(A) Receptor Modulator
MRK-898 is an orally active modulator of the GABA(A) receptor, selectively binding to the α1, α2, α3, and α5 subunits with Ki values of 1.2 nM, 1.0 nM, 0.73 nM, and 0.50 nM, respectively. This compound is significant for distinguishing between the sedative effects mediated by α1-containing receptors and the anxiolytic properties associated with α2- and/or α3-containing subtypes. MRK-898 is valuable for research investigating the therapeutic potential for anxiety and sleep disorders through GABAergic modulation. -
GABA Receptor Activator
6-Methylflavone is an activator of GABAA receptors, specifically targeting the α1β2γ2L and α1β2 subtypes. This compound demonstrates anxiolytic and sedative properties, making it of interest in neuropharmacological research. Its applications include studies on neuronal signaling and the modulation of inhibitory neurotransmission, contributing to the understanding of GABAergic system functions. -
GABABR PAM
GS39783 is a positive allosteric modulator (PAM) of the GABAB receptor (GABABR). This compound enhances GABABR signaling, making it a valuable tool for studying the neuropharmacological mechanisms underlying nicotine addiction. Its application in research may contribute to the understanding of GABAergic modulation in addiction-related behaviors and potential therapeutic strategies. -
GABAA Receptor PMA
Tetrahydrodeoxycorticosterone is a neurosteroid that functions as a potent positive allosteric modulator of the GABAA receptor. This compound exhibits significant neuroinhibitory properties, making it a valuable tool for research focused on the modulation of neuronal excitability and investigation of neuropharmacological mechanisms. Its application includes studies on anxiety, depression, and other conditions associated with GABAergic dysfunction. -
GABAA receptor Modulator
Selank is a GABAA receptor modulator known for its anxiolytic properties. It allosterically influences the binding of GABA to GABAA receptors, thereby modulating the affinity of endogenous ligands. This compound effectively reduces anxiety levels and mitigates stress-induced exacerbation of anxiety, demonstrating a synergistic effect when combined with diazepam. Selank is suitable for research applications focused on anxiety disorders and related therapeutic interventions. -
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. -
GABAB Agonist
Phenibut (β-Phenyl-GABA) is a potent GABAB receptor agonist. It exerts anxiolytic effects and enhances cognitive function, making it valuable in research focused on anxiety disorders and cognitive enhancement. This compound is widely utilized in studies investigating the modulation of GABAergic signaling and its implications for neurological health. -
δ-GABAA Receptor Positive Allosteric Modulator
DS2 is a selective positive allosteric modulator of the δ-GABAA receptor. This compound specifically enhances GABAergic responses mediated by the α4β3δ receptor while exhibiting minimal activity at α4β3γ2 and α1β3γ2 receptors. DS2 demonstrates significant analgesic properties and holds potential for research in sleep disorders, making it a valuable tool in neuropharmacology studies. -
GABAA Modulator
L-838417 is a selective partial agonist targeting the α2, α3, and α5 subtypes of the GABAA receptor while functioning as an antagonist at the α1 subtype. With binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM, and 2183 nM for various receptor subtypes, L-838417 exhibits significant anti-anxiety effects. This reagent is valuable for research on anxiety disorders and the modulation of GABAergic neurotransmission. -
GABAA Receptor Modulator
Tracazolate hydrochloride is a potent modulator of the GABAA receptor, specifically exhibiting selectivity towards the β3 subunit. It enhances GABAA receptor activity, demonstrating effective potentiation in α1β1γ2s (EC50=13.2 μM) and α1β3γ2 (EC50=1.5 μM) configurations. With its significant anxiolytic and anticonvulsant properties, Tracazolate hydrochloride serves as a valuable tool for research in neurological and psychiatric disorders, elucidating the role of GABAA receptor modulation in therapeutic contexts. -
GABAA Receptor PAM
α-Androstenol (5α-Androst-16-en-3α-ol) is a steroid pheromone that acts as a positive allosteric modulator of GABAA receptors, enhancing GABA-activated currents in primary mouse cerebellar granule cells with an EC50 of 0.4 μM. It exhibits anxiolytic-like, antidepressant-like, and anticonvulsant effects in murine models. This compound can be utilized in research focused on the mechanisms underlying seizures and related neurological disorders. -
GABA Receptor
ATPCA hydrochloride is a selective inhibitor targeting the GABA transporters BGT1, GAT1, and GAT3. It is utilized in biochemical studies to investigate GABAergic signaling and transport mechanisms. This compound plays a significant role in understanding the physiological and pathological processes related to GABA modulation, making it a valuable tool in neuropharmacology and drug discovery research. -
GABAA Receptor Agonist
ZK 93423 is a potent agonist of the GABAA receptor, belonging to the benzodiazepine class. It is characterized by its ability to enhance inhibitory neurotransmission, leading to sedative and anxiolytic effects. This compound is used in research to investigate the pharmacological profiles of GABAA receptor modulation and its potential therapeutic applications in anxiety and sleep disorders. -
GABA Receptor Agonist
3-Aminopropylphosphonic acid is a phosphonic acid analogue of gamma-aminobutyric acid (GABA) that functions as a GABAB receptor agonist. This compound exhibits significant biological activity by modulating neurotransmission through GABAB receptor activation. It is widely utilized in research focusing on neuropharmacology, particularly in studies related to anxiety, epilepsy, and other neurological disorders. -
GABA Receptor Activator
Cirsimaritin is a GABA receptor activator that exhibits weak binding to the benzodiazepine site on GABAA receptors. It demonstrates notable antidepressant, anxiolytic, and antinociceptive activities, making it a valuable tool for research in neuropharmacology. Its potential applications include the exploration of anxiety disorders, depression, and pain management pathways. -
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. -
Benzodiazepine Tranquilizer
Gidazepam is a benzodiazepine tranquilizer that acts as an agonist of GABA receptor channels (GABA RCs). It demonstrates significant anxiolytic and sedative properties, making it a valuable tool for studying anxiety disorders and neuropharmacology. Research applications include exploration of the mechanisms underlying GABAergic signaling and the development of therapeutic strategies for anxiety-related conditions. -
GABA Receptor Antagonist
6,2'-Dihydroxyflavone functions as a GABAA receptor antagonist, effectively inhibiting receptor activity. This compound exhibits potential neuroprotective effects and is being investigated for its role in neurological research, particularly in the context of anxiety, depression, and seizure disorders. Its unique structure and properties make it a valuable tool for studies exploring GABAergic signaling pathways. -
GABAB Receptor PAM
CGP13501 is a positive allosteric modulator of the GABAB receptor, enhancing its activity while facilitating gamma-aminobutyric acid (GABA) signaling. This compound serves as a structural analogue of propofol and is useful in research exploring the modulation of GABAB receptor-mediated pathways. CGP13501 may aid in studies related to neurotransmission, anxiety, and other central nervous system disorders. -
GABAB Agonist
(R)-4-Amino-3-hydroxybutyric acid is a GABAB receptor agonist that plays a significant role in modulating neurotransmission. Its interaction with GABAB receptors makes it a valuable tool for studying various neurological disorders and potential therapeutic pathways. This compound is instrumental in advancing research on the pharmacological aspects of the central nervous system. -
GABAC Receptor Antagonist
TPMPA is a selective antagonist of the GABAC receptor, exhibiting a binding affinity of KB = 2.1 μM. It does not significantly interact with GABAA or GABAB receptors, with binding constants of KB = 320 μM and EC50 = 500 μM, respectively. This compound is valuable in research focused on modulating orientation selectivity in ganglion cells, making it an important tool for exploring neural signaling mechanisms. -
GABA Aminotransferase Activator
3-Methyl-GABA is a potent GABA aminotransferase activator that enhances the activity of L-glutamic acid decarboxylase (GAD). This compound fits into the binding pocket of the GABAA receptor (GABAaR), facilitating the modulation of GABAergic signaling. 3-Methyl-GABA demonstrates anticonvulsant properties, making it a valuable reagent for research in neuropharmacology and the study of seizure disorders. -
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. -
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.
