Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
GABAA Receptor Antagonist
Golexanolone is a GABAA receptor antagonist that modulates steroid activity. This compound demonstrates significant effects on reducing peripheral inflammation and neuroinflammation, contributing to enhanced cognitive and motor functions in hyperammonemic rat models. Golexanolone serves as a valuable tool for investigating the mechanisms underlying neurological disorders and peripheral inflammation. -
GABAA receptor Positive Allosteric Modulator
Carbiphene is a positive allosteric modulator of the GABAA receptor. It inhibits [35S] TBPS binding while enhancing [3H] muscimol binding in rat forebrain membranes, targeting specific subsets of the GABAA receptor. This compound is valuable in research focused on schizophrenia and related neurological disorders. -
GABAA Receptor Positive Modulator
Androst-16-en-3-ol is a positive allosteric modulator of GABAA receptors, influencing neurotransmission in the central nervous system. This compound is known for its anxiolytic, antidepressant, and anticonvulsant properties, evidenced through behavioral studies in mice. Additionally, it serves as a pheromone, eliciting mating responses in estrous sows, and is present in human biological fluids such as urine and sweat. Its modulation of GABAA receptors positions Androst-16-en-3-ol as a significant reagent for investigating neuropharmacological mechanisms and exploring potential therapeutic applications. -
GABABR1 Receptor Agonist
(iodo-125)-CGP 71872 is a radiolabeled agonist of the GABABR1 receptor, featuring an azido group that allows for photoactivation. This compound is useful in studies aimed at characterizing GABAB receptors, facilitating investigations into their role in various neurological processes. Its specific targeting of GABAB receptors makes it a valuable tool for research in neuropharmacology and receptor signaling. -
GABA Receptor
Imagabalin is a compound that acts as a selective modulator of the GABA receptor, contributing to its potential in addressing neurological disorders. This reagent is instrumental in the study of conditions such as anxiety and epilepsy, where GABAergic signaling is disrupted. The synthesis of imagabalin not only produces the active compound but also characterizes key intermediates like 3-methylvaleryl chloride and 3-methylvaleric anhydride, providing valuable insights into the underlying reaction mechanisms in organic synthesis. -
GABA Receptor Ligand
Saripidem is a non-selective ligand for the ω modulatory sites of the GABA receptor. This compound exhibits anxiolytic and sedative properties by enhancing GABAergic neurotransmission. It is applicable in research focused on neuropharmacology, particularly in the study of anxiety, sleep disorders, and other neuropsychiatric conditions. -
GABA Receptor inverse agonist
Suritozole is an inverse agonist targeting the GABA receptor, specifically acting on benzodiazepine binding sites within GABAA ion channel complexes. This compound has demonstrated cognitive enhancement properties and is relevant in the investigation of neurodegenerative diseases. Research applications include studying the modulation of GABAergic neurotransmission and its implications in cognitive function and pathophysiology of neurological disorders. -
GABAAR Antagonist
GMQ is a competitive antagonist of the GABAergic receptor, primarily targeting the GABA(A) receptor subtypes α1β2, α1β2γ2, α4β2γ2, and α5β2γ2. This compound potently inhibits GABAAR activity, enhancing neuronal excitation by disrupting GABAergic transmission. Additionally, GMQ offers anti-histaminic effects within the enteric system, specifically inhibiting gastric acid secretion, making it valuable for research in neuropharmacology and gastrointestinal function. -
GABA Receptor Antagonist
GABAB receptor antagonist 3 is a potent inhibitor of the GABAB receptor, which plays a crucial role in neurotransmission and modulation of synaptic activity. This compound effectively blocks GABAB receptor signaling, making it valuable for studying the physiological and pathological roles of GABA in the central nervous system. Its applications include research into anxiety, epilepsy, and other neuropsychiatric disorders, providing insights into potential therapeutic interventions. -
GABAA Agonist
DS1 is a potent agonist of the GABAA receptor, enhancing its activity. This compound stimulates serum response element (SRE) and cAMP response element (CRE) promoters, leading to increased expression of luteinizing hormone beta (LHbeta) and follicle-stimulating hormone beta (FSHbeta) genes. DS1 is valuable for research applications focused on the modulation of GABAA receptor activity and its effects on hormone regulation. -
Tuclazepam
Tuclazepam is a benzodiazepine derivative primarily targeting the central nervous system to exert its anxiolytic and sedative effects. This compound is utilized in research focused on anxiety disorders and sleep-related studies due to its ability to modulate GABA receptor activity. Its significant calming properties make Tuclazepam an important reagent for investigating the neuropharmacological mechanisms underlying anxiety and sedation. -
GABAB Receptor Agonist
CGP47656 is a potent GABAB receptor agonist that selectively inhibits forskolin-stimulated adenylyl cyclase activity while enhancing noradrenaline-stimulated adenylyl cyclase activity. This compound is valuable for investigating the role of GABAB receptors in various neurological functions and diseases, offering potential insights into therapeutic strategies for brain function-related disorders. Its unique mechanism of action makes it a useful tool for researchers studying synaptic transmission and neuropharmacology. -
GABA Receptor Agonist
(R)-Baclofen hydrochloride is a selective agonist of the GABAB receptor. This compound is primarily utilized for its muscle relaxant properties and has been studied for its potential therapeutic effects in conditions such as spasticity and pain management. Its mechanism of action involves the modulation of neurotransmitter release, thereby influencing synaptic transmission and muscle tone. Research applications include neuroscience studies and investigations into GABAB receptor pathways. -
GABAB Receptor Antagonist
CGP 62349 is a selective GABAB receptor antagonist that exhibits oral bioactivity. This compound has been shown to enhance cognitive performance across various learning paradigms, making it a valuable tool in neuroscience research. Its application can provide insights into the modulation of cognitive processes and the therapeutic potential for cognitive impairments. -
GABA Antagonist
CGS-9895 is a GABA antagonist that functions by binding to the benzodiazepine site on GABA receptors. This compound selectively inhibits the activity of GABA, a major inhibitory neurotransmitter in the central nervous system. Its application in research includes studies on anxiety, depression, and seizure disorders, providing insights into the modulation of GABAergic signaling. -
GABAA receptors agonist
JY-XHe-053 is a selective agonist of GABAA receptors, particularly targeting those containing the α5 subunit, with an affinity of 0.7 nM. This compound demonstrates significant biological activity at GABAA receptors, particularly at the α2 and α3 subunits. Despite its potency, JY-XHe-053 exhibits minimal anti-anxiety activity, making it a valuable tool for investigating GABAA receptor function and the role of the α5 subunit in neurological research. -
GABAA Receptor Agonist
PF-0713 is a selective agonist of the GABAA receptor, which plays a crucial role in inhibitory neurotransmission within the central nervous system. This compound exhibits significant anxiolytic and anticonvulsant properties, making it valuable for research in neuropharmacology and potential therapeutic applications in anxiety disorders and epilepsy. PF-0713's mechanism of action can aid in understanding GABAA receptor modulation and its implications in various neurological conditions.
