Catalog No.
Product Name
Application
Product Information
Citations
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GABA Receptor Ligand
GABA-A Receptor Ligand-1 is a selective ligand for the GABA-A receptor, exhibiting a pKi of 7.27. This compound demonstrates significant neuroprotective effects, reducing mitochondrial dysfunction and promoting both neurite outgrowth and neuronal regeneration. Research applications include studies on ischemic stroke models in rats, highlighting its potential for therapeutic interventions in neurodegenerative conditions. -
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 Receptor Agonist
Propanidid is a γ-aminobutyric acid type A (GABAA) receptor agonist known for its short-acting properties as a non-barbiturate general anesthetic. This compound exhibits significant analgesic effects and can effectively lower arterial pressure. Propanidid is utilized in research applications focusing on pain management, sedation, and the modulation of vascular tone. -
GABAA PAM
LI-633 is a selective and orally active positive allosteric modulator (PAM) of the GABAA receptor, exhibiting a Ki value of 21 nM. This compound effectively potentiates GABA-induced inward currents, with EC50 values ranging from 8 nM for the α5β2γ2 subtype to 128 nM for α3β2γ2. Additionally, LI-633 enhances muscimol-induced GABAergic currents in rat dorsal root ganglion neurons, displaying an EC50 of 70.4 nM. This reagent is valuable for investigating mechanisms of visceral pain. -
GABAB Receptor Agonist
Lesogaberan napadisylate is a potent and selective agonist of the GABAB receptor, exhibiting an EC50 of 8.6 nM for human recombinant receptors. It demonstrates strong affinity for rat GABAB and GABAA receptors, with Kis values of 5.1 nM and 1.4 μM, respectively. This compound effectively inhibits transient lower esophageal sphincter relaxation, making it relevant for research into gastrointestinal disorders and neuromodulation. -
GABAA Positive Allosteric Modulator
Brexanolone caprilcerbate is a potent positive allosteric modulator of the GABAA receptor. This compound enhances GABAergic neurotransmission, promoting anxiolytic and sedative effects. It is primarily utilized in research focusing on mood disorders, epilepsy, and sleep regulation. -
Potassium Channel Opener
Flupirtine hydrochloride is a potassium channel opener (Kv7 activator) recognized for its analgesic and neuroprotective properties. This compound acts as a non-opioid analgesic while also antagonizing NMDA receptors and activating GABA receptors. Flupirtine hydrochloride enhances neuronal stability by reducing oxidative stress and calcium influx, thereby protecting neurons from excitotoxicity and ischemia. It is applicable in research focused on conditions such as focal cerebral ischemia, pain management, Alzheimer’s disease, and multiple sclerosis. -
GABAA Agonist
CP-615003 is a potent partial agonist of the GABAA receptor, exhibiting subtype-selectivity with a Ki value of 1.1 μM. This compound is converted into the active metabolite CP-900725 through oxidative deamination, which also shows affinity for the GABAA receptor. Additionally, CP-615003 is a substrate of P-glycoprotein, which may restrict its central nervous system penetration. It is primarily used in research related to CNS disorders and functions of the GABAA receptor. -
GABAergic System Modulator
Sodium bromide is a GABAergic system modulator that effectively reduces and blocks epileptiform discharges by enhancing inhibitory GABAergic functions. This compound increases the amplitude of inhibitory postsynaptic currents and paired-pulse inhibition, leading to pronounced anticonvulsant effects. Additionally, sodium bromide induces stimulation-induced extracellular alkalosis while sparing baseline pH levels and subsequent acidosis processes. It demonstrates species-specific pharmacokinetic characteristics and competes with chloride for renal tubular reabsorption, making it useful as a marker for extracellular fluid volume in research focused on epilepsy and related neurological conditions. -
GABA(A) Receptors Antagonist
Etbicyphat (Trimethylopropane phosphate) is a potent competitive antagonist of GABA(A) receptors. This compound is known to induce epileptiform activity in hippocampal CA1 neurons, making it an important tool for studying GABAergic signaling and its role in neuronal excitability. Etbicyphat also demonstrates binding affinity for GABA(A)-benzodiazepine receptors, facilitating research into neurological disorders and potential therapeutic interventions. -
GABA-mimetic Prodrug
Cholesteryl γ-aminobutyrate is a GABA-mimetic prodrug that targets GABA receptors in the central nervous system. It effectively inhibits orthodromically-evoked discharges in pyramidal cells located in the CA1 region of the hippocampus. This compound demonstrates dose-dependent suppression of locomotor activity in rodents and has been shown to inhibit Bicuculline-induced seizures in mice. Cholesteryl γ-aminobutyrate is valuable for research into CNS disorders associated with dysfunctional GABAergic signaling. -
GABA Receptor Agonist
5α-Androstan-3α-ol is a potent agonist of the γ-aminobutyric acid (GABA) receptor, influencing neurochemical signaling pathways. This compound has been shown to inhibit the transcriptional activity of the orphan nuclear receptor CAR (constitutive androstane receptor) by promoting its dissociation from coactivator proteins. 5α-Androstan-3α-ol is suitable for investigating nuclear receptor-mediated processes related to hormone metabolism and drug detoxification mechanisms in various biological systems. -
GABAB Receptor Antagonist
CGP36216 is a selective antagonist of the GABAB receptor, exhibiting a binding affinity with a Ki value of 0.3 μM. This compound is valuable in the study of anxiety and trauma-related disorders, allowing researchers to explore the roles of GABAB receptor modulation in these conditions. Its specificity makes it an important tool for investigating the therapeutic potential of GABAB receptor antagonism in various neuropsychiatric research applications. -
GABAA Receptor Agonist
Lorotomidate is a GABAA receptor agonist known for its anesthetic properties, exhibiting an ED50 of 2 mg/kg intravenously in KM mice, while demonstrating an LD50 of 46.5 mg/kg in the same model. This compound’s unique profile includes the ability to maintain corticosteroid secretion, which highlights its safety and efficacy. Lorotomidate is utilized in research to explore anesthetic mechanisms and neuro pharmacology, contributing to studies aimed at understanding GABAA receptor modulation. -
GABA Receptor Modulator
GABAA receptor agent 2 is a GABA receptor modulator that serves as a valuable tool for investigating the structure and orthosteric ligand binding of GABA(A) receptors. This compound aids in elucidating the binding mechanisms of orthosteric ligands, contributing to a deeper understanding of receptor functionality. The development of binding mode hypotheses through structure-activity relationships with homologous series of orthosteric GABA(A)R antagonists further enhances its application in pharmacological research. -
GABA Receptor Agonist
Divaplon is a GABA receptor agonist, exhibiting EC50 values of 31 nM for α3β2γ2 and 2 nM for α5β2γ2 subtypes. This compound demonstrates significant anxiolytic activity, making it valuable for research applications focusing on anxiety disorders and their underlying neurobiological mechanisms. Divaplon serves as a useful tool for studying GABAergic signaling and its effects on anxiety-related behaviors. -
GABAA1 Receptor Modulator
GABAA Receptor Agent 8 is a potent positive modulator of the GABAA1 receptor. It exhibits significant anticonvulsant activity both in vitro and in vivo, demonstrating low levels of neurotoxicity. This compound holds promise for research applications in the field of epilepsy and related neurological disorders. -
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 Receptor Modulator
TG 41 is a positive modulator of the GABAA receptor. It enhances the binding affinity of gamma-aminobutyric acid (GABA) and Flunitrazepam to rat cerebral cortical membranes. This compound is valuable for studying GABAA receptor functionality and dynamics, as well as for exploring its implications in neuropharmacology and anxiety-related 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. -
GABAB Receptor Agonist
(S)-Baclofen is a potent GABAB receptor agonist that effectively crosses the blood-brain barrier and exhibits oral bioactivity. With an IC50 value of 1.77 μM for GABAB receptors and 1564 μM for GABAA receptors, (S)-Baclofen is instrumental in studying muscle disorders, particularly spasticity. Its role in modulating inhibitory neurotransmission makes it a valuable tool for neuroscientific and pharmacological research. -
GABA Receptor
SH-053-S-CH3-2'F is a selective positive allosteric modulator targeting GABA(A) receptors, specifically exhibiting mild to partial agonistic activity at the α(1) subtype. This compound has demonstrated anxiety-relieving effects without inducing the memory impairment associated with traditional benzodiazepines. Its strong selectivity for GABA(A) receptors suggests potential applications in the development of more targeted anti-anxiety therapeutics, enhancing therapeutic efficacy while minimizing adverse effects. -
GABA-ergic
GABA-palmitamide is a GABA-responsive compound that targets the GABAergic system. It demonstrates a dose-dependent bidirectional effect on stereotyped behaviors induced by apomorphine, with high doses inhibiting motor activity and low doses enhancing oral stereotypies. This compound is valuable for research applications focused on behavior regulation and the modulation of GABAergic signaling. -
GABA Receptor
2-AEMP (2-Aminoethyl methylphosphonate) functions as an antagonist of the GABA(A)-ρ1 receptor. It demonstrates competitive inhibition with an IC(50) value of 18 μM, which is substantially less potent than the 7 μM seen with TPMPA. Notably, 2-AEMP exhibits a higher release rate of inhibition upon termination compared to TPMPA. Additionally, this compound requires a shorter preincubation time to achieve its inhibitory effects, making it a valuable tool for research on GABA receptor modulation and related neurological studies. -
GABA/Serotonin Receptor Modulator
Californidine perchlorate is a modulator of γ-aminobutyric acid (GABA) and serotonin receptors. It enhances GABA-mediated chloride influx while inhibiting cytochrome P450 enzymes. This compound shows potential for research in anxiety-related studies, making it a valuable tool for exploring neuropharmacological mechanisms. -
GABA(B) receptor Antagonist
CGP 56999 is a potent antagonist of the GABA(B) receptor, exhibiting an IC50 value of 0.002 μM. This compound has been demonstrated to elevate brain-derived neurotrophic factor (BDNF) mRNA levels both in vivo and in vitro. CGP 56999 is valuable for research applications focused on neurobiology and the modulation of GABAergic signaling. -
γ-GABAAR Antagonist
GABAA receptor agent 4 is a potent γ-GABAAR antagonist with a Ki of 0.18 µM. This compound effectively rescues inhibition of T cell proliferation, demonstrating its potential as an immunomodulatory agent. GABAA receptor agent 4 is suitable for research applications related to immune response modulation and T cell activity. -
Pregabalin Prodrug
Pregabalin arenacarbil is a prodrug of Pregabalin, targeting the calcium channels involved in neurotransmitter release. It exhibits significant biological activity in pain management, specifically in conditions such as post-herpetic neuralgia, peripheral diabetic neuropathy, fibromyalgia, and epilepsy. This compound is valuable for research investigating mechanisms of neuropathic pain and anxiety disorders. -
GABAB Receptor Antagonist
GABAB Receptor Antagonist 4 is a selective inhibitor of the GABAB receptor, functioning by competitively binding to the orthosteric site. This compound effectively inhibits GABA-induced G protein activation. GABAB Receptor Antagonist 4 is valuable for investigating GABAB receptor-related neurological disorders and for studying the underlying mechanisms of synaptic transmission and plasticity. -
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 Agonist
Picamilon sodium is a GABA receptor agonist that exhibits nootropic effects. It has demonstrated efficacy in improving epilepsy models in rats and facilitating the correction of functional disorders of the pancreas in Alloxan-induced diabetes models. This compound is valuable for research applications focused on neurological conditions and metabolic disorders. -
GABA Receptor Antagonist
GABA receptor antagonist 2 targets the GABA receptor and exhibits insecticidal properties against Plutella xylostella, including its resistant strains, as well as Spodoptera frugiperda and Chilo suppressalis. With a lethal concentration (LC50) of 0.0735 μg/mL, this compound effectively disrupts GABAergic signaling by binding at the Drosophila RdlG335 site. GABA receptor antagonist 2 serves as a valuable tool in managing resistant pest populations in agricultural research applications. -
GABA Receptor Modulator
GABAA receptor modulator-5 is a selective modulator of the GABA A receptor, demonstrating EC50 values of 56 nM and 10 nM for the α1β2γ2 and α4β3δ subtypes, respectively. This compound exhibits favorable pharmacokinetic properties in rat models and shows a threshold dose of 23.3 μmol/kg for loss of rollover reflex (LORR), indicating slight toxicity. GABAA receptor modulator-5 has potential applications in the research of postpartum depression and may contribute to therapeutic strategies targeting GABAergic pathways. -
GABAA Receptor Antagonist
Bicuculline methobromide is a selective antagonist of the GABAA receptor, exhibiting an IC50 value of 3 μM. This compound is known to induce clonic-tonic convulsions in mammalian models, making it a valuable tool for investigating epilepsy and associated neurological disorders. Additionally, bicuculline methobromide functions as a blocker of Ca2+-activated potassium channels, further expanding its utility in pharmacological research focused on ion channel dynamics and excitability in neuronal systems. -
GABAB Receptor Positive Allosteric Modulator
CMPPE is a positive allosteric modulator of the GABAB receptor, enhancing the receptor's activity in response to its natural ligand. It has demonstrated efficacy in inhibiting alcohol self-administration and reinstatement behavior in rat models, making it a valuable tool for research into substance use disorders and potential therapeutic interventions. CMPPE provides insights into GABAB receptor functioning and its role in addiction-related behaviors. -
GABA Receptor Modulator
CGP 54626 is a GABAB receptor modulator that plays a crucial role in regulating neurotransmission within the central and peripheral nervous systems. This compound serves as a valuable tool for the identification and characterization of GABAB receptor agonists and antagonists, supporting drug development for various neurological disorders. Its use in conjunction with purified GABAB receptors and related molecular tools enhances research into the GABAB receptor family, facilitating advancements in therapeutic strategies through techniques such as DNA cloning and sequence analysis. -
α5 GABAA Agonist
PWZ-029 is a selective inverse agonist targeting the α5 GABAA receptor. It acts as a benzodiazepine site ligand and exhibits a partial agonistic effect on 1- and 3-containing GABAA receptors. In vitro studies demonstrate that PWZ-029 significantly increases retention session latency in mouse fibroblast cells. Furthermore, it has been shown to enhance object recognition in both normal and scopolamine-treated rat models, highlighting its potential applications in cognitive research. -
α5-GABAAR Modulator
GABAA receptor modulator-2 is a selective negative allosteric modulator of the α5-GABAAR with a Ki of 4.1 nM. This orally active compound demonstrates high metabolic stability and favorable safety profiles in the central nervous system. It is valuable for research focusing on GABAergic signaling and its implications in various neurological conditions. -
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. -
GABAA Receptor Modulator
GABAA receptor modulator-8 is a selective positive modulator of the GABAA receptor, designed for effective penetration of the blood-brain barrier. This compound exhibits significant antiepileptic activity, making it a valuable tool for research into neurological disorders. Its unique properties support studies aimed at understanding GABAA receptor interactions and their therapeutic potential in epilepsy and related conditions. -
GABAA Receptor Agonist
Moxetomidate is a GABAA receptor agonist that induces sedation by enhancing inhibitory neurotransmission. Its primary biological activity involves the modulation of chloride ion influx, leading to increased neuronal hyperpolarization. This compound is utilized in research settings to investigate mechanisms of sleep induction and potential therapeutic applications in anesthesia and neuropharmacology. -
GABA Receptor Antagonist
17-PA is a selective antagonist of GABA(A) receptors, targeting their neurosteroid potentiation and direct gating mechanisms. This compound plays a significant role in research applications related to neuropharmacology and the modulation of inhibitory neurotransmission. By inhibiting GABA(A) receptor activity, 17-PA can aid in the exploration of pathways involved in anxiety, sleep regulation, and other neuropsychiatric disorders. -
Stable Isotope
Flupirtine-d4 hydrochloride is a deuterium-labeled variant of Flupirtine hydrochloride, a non-opioid analgesic that crosses the blood-brain barrier. This compound functions primarily as a neuronal potassium channel opener (Kv7 activator) and exhibits properties as an NMDA receptor antagonist and GABA receptor activator. It is utilized in research focused on pain management, neuroprotection, and conditions such as Alzheimer’s disease and multiple sclerosis, offering insights into pathways of ischemic neuron death, oxidative stress modulation, and the maintenance of blood-brain barrier integrity. Flupirtine-d4 hydrochloride serves as a valuable tool for studying the underlying mechanisms and therapeutic approaches for neurological disorders. -
GABAA Receptor Agonist
HZ166 is a GABAA receptor agonist that selectively targets the α2- and α3-subtypes. This compound demonstrates significant anti-hyperalgesic properties, making it a valuable tool for pain research. Additionally, HZ166 features an alkyne group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions. Its unique properties make it suitable for applications in both neuropharmacology and click chemistry. -
GABAA Receptor Agonist
(S)-Norzopiclone is a GABAA receptor agonist with demonstrated anxiolytic and anticonvulsant properties. As a metabolite of zopiclone, it exhibits benzodiazepine-like activity specifically at γ2-bearing subtypes of the GABAA receptor while also inhibiting nicotinic acetylcholine (nACh) and NMDA receptors. This compound is valuable in research aimed at understanding the mechanisms of anxiety and seizure disorders, as well as exploring the pharmacological profiles of GABAA modulators. -
GABA receptor agonist
Adipiplon is a selective positive allosteric modulator of the GABAA receptor that enhances inhibitory neurotransmission. Its mechanism of action makes it valuable for studying various central nervous system (CNS) disorders, including anxiety and sleep-related conditions. By influencing GABAA receptor activity, Adipiplon serves as an important tool in pharmacological research aimed at understanding and developing therapeutic strategies for CNS-related diseases. -
GABA Receptor Activator
Emamectin B1a is a semisynthetic derivative of avermectin B1a that serves as a GABA receptor activator. It enhances GABA responses by binding to GABAA receptors, demonstrating IC50 values of 57 nM for α1β1γ2, 210 nM for α1β2γ2, and 49.8 nM for α1β3γ2. Additionally, Emamectin B1a interacts with glycine receptors, exhibiting an IC50 of 218 nM in rat spinal cord. Its potent activity is evident in pest control applications, achieving 90% mortality in S. exigua larvae at concentrations as low as 1.067 ng/mL in foliar spray bioassays and topical applications. -
GABA Receptor Agonist
CCD-3693 is a potent orally active agonist of the GABA receptor, demonstrating significant anxiolytic, anticonvulsant, and sedative hypnotic properties. This compound serves as a valuable tool in the investigation of neurological diseases, offering insights into the modulation of GABAergic signaling and its implications for therapeutic interventions. -
GABAA Receptor PAM
GBLD345 is a potent positive allosteric modulator (PAM) of the GABAA receptor, functioning as a non-selective anxiolytic agent. This compound enhances GABAA receptor activity, leading to increased inhibitory neurotransmission. Its primary applications include research on anxiety disorders and studies investigating the role of GABAergic modulation in neural function. -
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.
