Catalog No.
Product Name
Application
Product Information
Citations
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Calmodulin Inhibitor
Zaldaride is a selective calmodulin inhibitor that effectively inhibits CaM-stimulated cAMP phosphodiesterase activity, exhibiting an IC50 of 3.3 nM. This compound demonstrates significant biological activity by preventing estrogen-induced transcription activation mediated by estrogen receptors. Additionally, Zaldaride reversibly blocks voltage-activated sodium, calcium, and potassium currents in PC12 cells, and also inhibits nicotinic acetylcholine receptors (nAChR), making it a valuable tool for research into calcium signaling pathways and their related physiological processes. -
GABA/Glutamate-gated Chloride Channel Potentiator
4''-Oxoavermectin B1a is a potent modulator of GABA (γ-aminobutyric acid) and glutamate-gated chloride channels, exhibiting significant insecticidal and acaricidal properties. This compound demonstrates efficacy in disrupting neurological processes in target pests, making it a valuable tool for research in agricultural pest management. Its application contributes to understanding the mechanisms of action in pest control strategies. -
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. -
Stable Isotope
γ-Aminobutyric acid-d6 is a deuterium-labeled form of γ-Aminobutyric acid, a crucial inhibitory neurotransmitter in the mammalian central nervous system. This compound primarily targets ionotropic GABA receptors (GABAA) and metabotropic receptors (GABAB), playing a significant role in regulating neuronal excitability. It is useful in research applications focused on neurotransmitter dynamics, GABAergic signaling, and metabolic studies involving stable isotopes. -
GABA(A) Receptors Blocker
Bicuculline methiodide is a potent blocker of GABA(A) receptors, serving to inhibit GABA-mediated neurotransmission. By altering membrane properties and firing patterns, it effectively reduces Apamin-sensitive afterhyperpolarization, enhancing neuronal excitability. This compound is valuable for research applications focused on understanding the role of GABA(A) receptors in synaptic transmission and studying neuronal firing behaviors in various neurological models. -
GABAB Receptor Antagonist
Saclofen is a competitive antagonist of the GABAB receptor, exhibiting an IC50 value of 7.8 μM. It demonstrates weak antagonistic activity towards the GABAB1b and GABAB2 heterodimeric receptors. Saclofen effectively inhibits Baclofen binding to rat cerebellar membranes and blocks Baclofen-induced circadian phase shifts. Additionally, it has shown anti-inflammatory and analgesic effects in preclinical models. This makes Saclofen a valuable tool for investigating GABAB receptor functions and related biological processes. -
GABAB Receptor Antagonist
CGP35348 is a selective GABAB receptor antagonist exhibiting a central nervous system penetration with an EC50 of 34 μM. This compound specifically targets the GABAB receptor, demonstrating potential to enhance neuromuscular coordination and spatial learning in animal models, particularly following neonatal brain injury. Its unique mechanism offers a valuable tool for researching the effects of GABAB receptor modulation on cognitive functions and motor behavior. -
GABAB Receptor Antagonist
CGP55845 hydrochloride is a potent and selective antagonist of the GABAB receptor, exhibiting an IC50 of 6 nM. This compound is valuable in neurological research, providing insights into GABAergic signaling pathways and their implications in various neurological disorders. Researchers use CGP55845 hydrochloride to investigate the role of GABAB receptors in synaptic transmission and neuronal excitability. -
GABA Receptor
17β-Estradiol sulfate sodium is a neuroactive steroid that acts as a modulator of the GABA receptor. This compound exhibits significant biological activity by influencing neurotransmission and neuroprotection, making it useful in research related to neuropharmacology and hormone signaling. Its applications include studying the effects of estrogens on the central nervous system and investigating potential therapeutic targets for neurological disorders. -
GABAA Receptor Modulator
AZD7325 is a potent and orally active partial positive allosteric modulator (PAM) of the GABAA receptor, specifically targeting the α2 and α3 subtypes (Ki=0.3 nM and 1.3 nM, respectively), while exhibiting reduced antagonistic activity at the α1 and α5 subtypes. It serves as a valuable tool for research applications related to anxiety disorders and Dravet syndrome. Additionally, AZD7325 acts as a moderate inducer of CYP1A2 and a potent inducer of CYP3A4 in vitro, making it relevant for studies on drug metabolism and interactions. -
GABA Receptor Activator
Alpha-Asarone (α-Asarone) acts as a GABA receptor activator, demonstrating significant antidepressant-like activity in preclinical mouse models. This compound is of interest in neuropharmacology research for its potential effects on mood regulation and anxiety disorders. Its mechanism may provide insights into novel therapeutic approaches for treating depression and related conditions. -
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. -
GABAA Agonist
Clomethiazole is a potent, orally active GABAA agonist that enhances inhibitory neurotransmission within the central nervous system. This compound exhibits anticonvulsant properties, making it particularly relevant for the treatment of convulsive status epilepticus. Additionally, Clomethiazole has been shown to inhibit cytochrome P450 isoforms CYP2A6 and CYP2E1 in human liver microsomes, which may impact metabolic pathways relevant to drug interactions in pharmacological studies. -
GABAA Receptor Antagonist
Bicuculline (methochloride) 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 mammals and is also capable of blocking Ca2+-activated potassium channels. Bicuculline (methochloride) is utilized in research focused on epilepsy and related psychiatric disorders, providing valuable insights into neuronal excitability and inhibitory transmission. -
GABA Receptor Antagonist
L-Allylglycine is an amino acid derivative that acts as a GABA receptor antagonist through the inhibition of glutamate decarboxylase (GAD), consequently reducing GABA biosynthesis in the brain. This compound exhibits convulsant activity, making it a valuable tool in neurological research. L-Allylglycine is utilized to study the roles of GABAergic signaling in various physiological and pathological conditions. -
GABAA PAM
Darigabat is a selective positive allosteric modulator (PAM) targeting GABAA receptors, specifically the α2, α3, and α5 subtypes. This compound exhibits high affinity for GABAA receptors with K_i values of 2.9 nM for α2 and 21 nM for α3, while demonstrating significantly lower affinity for α4 and α6 subunits. Darigabat effectively penetrates the blood-brain barrier and possesses anxiolytic properties, indicating its potential use in treating conditions such as anxiety and epilepsy. -
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. -
Stable Isotope
γ-Aminobutyric acid-d2 is a deuterium-labeled form of γ-Aminobutyric acid, a critical inhibitory neurotransmitter in the mammalian central nervous system. It functions by binding to both ionotropic GABA receptors (GABAA) and metabotropic GABA receptors (GABAB), playing a vital role in neuronal signaling and modulation. This stable isotope is particularly useful in research applications involving metabolic tracing, pharmacokinetics, and the study of neurochemical pathways. -
GABA Receptor Antagonist
CGP 54626 hydrochloride is a potent and selective antagonist of the GABAB receptor, exhibiting an IC50 value of 4 nM. This compound is valuable in research aimed at elucidating the role of GABAB receptors in various neurological signaling pathways. Its use can enhance the understanding of GABAB receptor-mediated mechanisms in both normal physiology and pathological conditions. -
GABABR Agonist
Baclofen hydrochloride is a selective agonist of the metabotropic GABAB receptor (GABABR). This lipophilic derivative of γ-aminobutyric acid (GABA) mimics GABA's action, inducing presynaptic inhibition and facilitating muscle relaxation. With its ability to penetrate the blood-brain barrier effectively, Baclofen hydrochloride is valuable for research applications focused on muscle spasticity and neurological disorders. -
GABA Agonist
Piperidine-4-sulfonic acid is a potent GABA agonist targeting GABA receptors, exhibiting an IC50 of 0.034 μM for the inhibition of H-GABA binding. This compound is valuable in research applications involving neuropharmacology and the study of GABAergic neurotransmission, providing insights into potential therapeutic strategies for neurological disorders. -
α5-GABAAR Antagonist
Afizagabar (S44819) is a selective antagonist of the GABA-binding site at the α5-GABA receptor subtype, displaying an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. This compound has been shown to enhance synaptic plasticity within the hippocampus, thus demonstrating potential pro-cognitive effects. Afizagabar serves as a valuable tool for research focused on cognitive enhancement and the modulation of GABAergic signaling pathways. -
GABA Receptor Activator
Kavain is a kavalactone derived from Piper methysticum, primarily acting as a GABA receptor activator. This compound has demonstrated anxiolytic effects in both animal and human studies. Its ability to positively modulate the gamma-aminobutyric acid type A (GABAA) receptor makes it relevant for research into anxiety disorders and related neurological conditions. -
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. -
GABAB Receptor Antagonist
Phaclofen is a selective GABAB receptor antagonist primarily acting on both central and peripheral systems. This compound is instrumental for research into the physiological roles of baclofen-sensitive and bicuculline-insensitive GABA receptors. Its diverse applications in neuropharmacology make it valuable for studies aimed at understanding GABAergic signaling and related physiological processes. -
GABAA PAM
(2S)-6-Prenylnaringenin is a potent positive allosteric modulator of the GABAA receptor, specifically targeting the α+β binding interface. It demonstrates significant biological activity within the forebrain, enhancing inhibitory neurotransmission. This compound is valuable for research applications focused on neuroscience, particularly in the study of anxiety, neuroprotection, and the modulation of synaptic transmission. -
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. -
GABA Receptor Modulator
TPA-023B is an orally active partial agonist at the GABAA receptor α2 and α3 subtypes, with affinities of 0.73 nM and 2 nM, respectively, while acting as an antagonist at the α1 subtype with a Ki of 1.8 nM. This compound exhibits non-sedating anxiolytic-like properties, making it a valuable tool for research into anxiety disorders and GABAergic signaling. Its selective modulation of specific GABA receptor subtypes allows for nuanced studies on neuropharmacological effects. -
GABAA Receptor Agonist
Isonipecotic acid is a GABAA receptor partial agonist that modulates inhibitory neurotransmission in the central nervous system. Its biological activity includes the potential to enhance GABAergic signaling, making it a valuable tool for studying anxiety, seizure disorders, and other neurophysiological processes. This compound is applicable in research focused on developing therapeutic strategies for CNS-related conditions. -
GABA Receptor Antagonist
L-Allylglycine hydrochloride is an amino acid derivative that acts as a GABA receptor antagonist by inhibiting glutamate decarboxylase (GAD), thereby reducing GABA biosynthesis in the brain. This compound exhibits convulsant activity, making it a valuable tool for investigating the role of GABA in neurological disorders and for studying excitatory-inhibitory balance in neural circuits. Its applications extend to pharmacological research focused on seizures and related neurotransmission studies. -
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.
