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Catalog No.
Product Name
Application
Product Information
Citations
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NMDA NR2B Inhibitor
BZAD-01 is a selective inhibitor of the NMDA NR2B subunit, exhibiting a Ki value of 72 nM. This compound demonstrates significant biological activity by improving postural asymmetry and reducing Apomorphine-induced rotation. BZAD-01 is utilized in research applications focused on neurological disorders and synaptic transmission modulation. -
NMDAR/SERT Inhibitor
Antidepressant agent 9 is an orally active NMDAR and SERT inhibitor with IC50 values of 3.50 μM and 1044 nM, respectively. This compound demonstrates good metabolic stability and significant plasma exposure, making it suitable for in vivo studies. Antidepressant agent 9 has been shown to exhibit antidepressant-like effects in the mouse forced swim test, highlighting its potential application in depression research. -
nAChR Inhibitor
Meclofenoxate, a nAChR inhibitor, is an ester derived from dimethylaminoethanol (DMAE) and para-chlorophenylalanine (pCPA). It is known for its potential to enhance memory and cognitive function. Meclofenoxate is commonly utilized in neurological research to investigate mechanisms underlying cognitive enhancement and memory improvement. -
NMDA Inhibitor
5-Chloro-1,4-dihydro-2,3-quinoxalinedione is a weak inhibitor of the NMDA receptor, exhibiting an IC50 value of 56.3 μM. This compound is relevant for investigations into neurological disorders, particularly in understanding excitotoxicity and synaptic plasticity. Its role in modulating NMDA receptor activity makes it a valuable tool for research in neuropharmacology. -
NR1/NR2B NMDA Receptor Inhibitor
NR2B-selective NMDA receptor antagonist 1 is a potent inhibitor of the NR1/NR2B NMDA receptor with an IC50 of 0.05 μM. It demonstrates selectivity against other targets such as hERG and α1-AdR, with IC50 values of 0.73 μM and 2.4 μM, respectively. This compound exhibits excellent permeability across the blood-brain barrier, making it a valuable tool for research into neuropharmacology and the therapeutic exploration of NMDA receptor-related disorders. -
NMDA Inhibitor
Fluorolintane is a potent NMDA receptor inhibitor, with a Ki value of 87.92 nM. This compound effectively disrupts prepulse inhibition in rat models, demonstrating its capacity to modulate synaptic transmission. Additionally, Fluorolintane inhibits NMDA receptor-induced field excitatory postsynaptic potentials in rat hippocampal slices, making it a valuable tool for studying excitatory neurotransmission and its implications in neurological research. -
AchE Inhibitor/NMDAR Antagonist
Memagal is a potent acetylcholinesterase (AChE) inhibitor with an IC50 of 1.16 nM and acts as an N-methyl-D-aspartate receptor (NMDAR) antagonist with a Ki of 4.6 μM. This compound effectively inhibits neurotoxicity triggered by NMDA, demonstrating an IC50 value of 0.28 nM. Memagal serves as a valuable tool for research focused on Alzheimer's disease, providing insights into mechanisms and potential therapeutic approaches. -
NMDAR Inhibitor
AChE-IN-53 is a potent inhibitor of the NMDA receptor (NMDAR), which plays a key role in mediating excitatory synaptic transmission and is implicated in various neurological disorders. This compound exhibits significant neuroprotective effects and has shown potential in behavioral research applications related to cognitive decline and neurodegenerative conditions. AChE-IN-53 can be utilized to explore therapeutic strategies targeting NMDAR dysregulation in various models of neural injury and disease. -
NMDA Receptor Inhibitor
NMDA-IN-2 is a selective NMDA receptor 2B subtype inhibitor derived from Procaine. It demonstrates potent inhibitory effects on NMDA receptor activity, making it valuable for studying synaptic transmission and neurotoxicity. This compound has applications in researching neurological disorders and may aid in the development of therapeutic strategies for conditions associated with NMDA receptor dysregulation. -
NMDA Inhibitor
UBP618 is a non-selective N-methyl-D-aspartate (NMDA) receptor inhibitor. This compound exhibits significant modulation of NMDA receptor activity, making it valuable for studying excitatory neurotransmission and various neurological disorders. UBP618 is utilized in research addressing conditions such as Alzheimer's disease, schizophrenia, and other neurodegenerative disorders, providing insights into synaptic plasticity and neuroprotection mechanisms. -
AChE Reversible Inhibitor
Asoxime dichloride is a reversible inhibitor of acetylcholinesterase (AChE) that functions as a thiosemicarbazone-based antidote. Its primary mechanism involves reactivating AChE that has been inhibited by nerve agents, thus restoring cholinergic nerve function. Additionally, Asoxime dichloride enhances muscle function in the presence of poisoning without reactivating AChE and acts as an antagonist to acetylcholine receptors, including nicotinic and α7 nAChRs. Due to its immunomodulatory properties, Asoxime dichloride can also enhance the immune response of the nervous system, making it valuable in neuropharmacological research. -
nAChR Inhibitor
Lupanine is a natural ketonic derivative of Sparteine that acts as an inhibitor of nicotinic acetylcholine receptors (nAChR). It exhibits binding affinity to these receptors with a Ki value of 500 nM, demonstrating its potential as a ganglioplegic agent. Lupanine is utilized in research applications related to neuromodulation and the study of cholinergic signaling pathways. -
nAChR Inhibitor
CVN417 is an orally active antagonist of the α6 subunit-containing nicotinic acetylcholine receptors (nAChRs). This inhibitor modulates phasic dopaminergic neurotransmission in an impulse-dependent manner and exhibits inhibitory effects on Ca(2+) efflux through various nAChR subunits, with IC50 values of 0.086 μM for α6, 2.56 μM for α3, and 0.657 μM for α4. CVN417 has demonstrated efficacy in reducing resting tremors in rodent models and may offer therapeutic potential for improving movement dysfunction associated with Parkinson's disease. -
nAChR Inhibitor
Triflumezopyrim is a selective inhibitor of the nicotinic acetylcholine receptor (nAChR), exhibiting potent insecticidal activity at low dosages. Its primary application is in the control of hopper species, where it demonstrates rapid efficacy while maintaining low toxicity to non-target arthropods. This compound is particularly valuable in agricultural research and pest management studies focused on sustainable and selective insect control strategies. -
nAChR Inhibitor
nAChR-IN-1 (2,2,6,6-Tetramethylpiperidin-4-yl heptanoate) is a selective inhibitor of nicotinic acetylcholine receptors (nAChRs) that specifically targets receptors lacking α5, α6, or β3 subunits. This compound demonstrates significant potential in alleviating nerve disorders and is valuable for research focused on nAChR dysfunction and various neurological conditions. Its mechanism of action makes it an essential tool for studying the role of nAChRs in neurological signaling pathways. -
nAChR Inhibitor
Azemiopsin is a potent inhibitor of nicotinic acetylcholine receptors (nAChR), exhibiting IC50 values of 0.18 μM against the T. californica nAChR and 22 μM against the human α7 nAChR. This compound effectively blocks acetylcholine-induced currents in Xenopus oocytes that are heterologously expressing human muscle-type nAChR. Azemiopsin serves as a valuable tool for investigating nAChR-mediated signaling pathways and contributes to studies on neuropharmacology and synaptic transmission. -
nAChR Inhibitor
nAChR-IN-2 is an inhibitor of insect nicotinic acetylcholine receptors (nAChR), targeting the acetylcholine binding site and the NCB/PCP binding site. It demonstrates an IC50 of 360 μM for α-bungarotoxin binding and 84 μM for Phencyclidine binding in honeybee head preparations. This compound is valuable for studying nAChR-mediated signaling pathways and their role in insect neurobiology. Research applications include investigating insecticide mechanisms and assessing the neurophysiological effects of nAChR modulation. -
nAChRs Inhibitor
bPiDI is a selective antagonist of the α6β2 nicotinic acetylcholine receptors (nAChRs). It effectively inhibits nicotine-evoked dopamine release in the striatum, making it a valuable tool for studying dopaminergic signaling pathways. This compound is particularly useful in research pertaining to nicotine addiction and dopamine-related disorders. -
AChE Reversible Inhibitor
Asoxime dimesylate is a reversible inhibitor of acetylcholinesterase (AChE) that serves as a thiosemicarbazone-based antidote. Its primary mechanism of action involves reactivating AChE inhibited by nerve agents, thus restoring cholinergic nerve function. Additionally, Asoxime dimesylate has been shown to significantly restore muscle function compromised by poisoning without the reactivation of AChE. It also acts as an antagonist at acetylcholine receptors, including nicotinic receptors and α7 nAChR, and demonstrates potential as an immunomodulator, enhancing immune responses in the nervous system. This compound is valuable for research in neuropharmacology and toxicology. -
nAChR Inhibitor
Lupanine perchlorate is a natural ketonic derivative of sparteine that functions as an nAChR inhibitor. It exhibits significant ganglioplegic activity and demonstrates a binding affinity for nicotinic receptors with a Ki value of 500 nM. This compound is commonly utilized in research focused on studying neuronal signaling and the effects of cholinergic modulation. -
nAChR Inhibitor
Ferulamide is a derivative of ferulic acid that acts as a competitive inhibitor of nicotinic acetylcholine receptors (nAChRs). It exhibits significant anticholinesterase activity, making it a valuable tool for studying cholinergic signaling pathways. This compound is useful in research related to neurodegenerative diseases and the modulation of synaptic transmission. -
α7 nAChR Inhibitor
QND8 is a selective and potent inhibitor of the α7 nicotinic acetylcholine receptor (nAChR). It demonstrates significant biological activity by alleviating thermal and mechanical hyperalgesia in carrageenan-induced inflammatory pain models. QND8 effectively reduces swelling, inhibits the release of pro-inflammatory cytokines, and prevents leukocyte infiltration at the inflammatory site. This compound is valuable for research applications focused on inflammation and neurological disorders, including arthritis. -
nAChR Inhibitor
Aristoquinoline is a naturally occurring alkaloid derived from Aristotelia chilensis, functioning primarily as an inhibitor of the α3β4 nicotinic acetylcholine receptor (nAChR). This compound demonstrates significant biological activity by modulating neurotransmitter signaling, making it a valuable tool for research in neuropharmacology, particularly in studies related to addiction, cognitive function, and neurodegenerative diseases. Its specific inhibitory effect on nAChR presents opportunities for investigating the receptor's role in various physiological processes. -
nAChR Inhibitor
nAChR-IN-1 hydrochloride is a selective nicotinic acetylcholine receptor (nAChR) inhibitor that specifically targets nAChRs lacking the α5, α6, or β3 subunits. This compound is particularly useful in studying the roles of nAChRs in neurological disorders and offers potential insights into therapeutic strategies for conditions involving nicotinic acetylcholine receptor dysfunction. Its effectiveness in modulating nAChR activity makes it a valuable tool for chemical biology and pharmacological research. -
nAChR Inhibitor
Lupanine hydrochloride is a natural ketonic derivative of Sparteine, functioning as a nicotinic acetylcholine receptor (nAChR) inhibitor. It demonstrates binding affinity for the nAChR with a Ki value of 500 nM, indicating its potential role in modulating cholinergic signaling. This compound is suitable for research applications related to neuromuscular transmission and ganglioplegic activity. -
nAChR Inhibitor
Xanthoplanine is an nAChR inhibitor derived from the root of Xylopia parviflora. It effectively inhibits the EC50 acetylcholine responses of both alpha7 and alpha4beta2 nicotinic acetylcholine receptors, demonstrating estimated IC50 values of 9 μM for alpha7 and 5 μM for alpha4beta2. Its potent inhibitory activity makes it a valuable tool for studying cholinergic signaling and related neurological pathways in research applications. -
NF-κB Inhibitor
(R)-(+)-Anatabine is an NF-κB inhibitor that acts to lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). As the less active R-enantiomer of Anatabine, it retains the ability to modulate α4β2 nAChR activity. This compound exhibits anti-inflammatory properties and is being investigated for its potential applications in the treatment of neurodegenerative disorders. -
AChE/nAChR Inhibitor
AChE/nAChR-IN-1 is a dual inhibitor targeting acetylcholinesterase (AChE) and nicotinic acetylcholine receptors (nAChR). This compound exhibits potent toxicity and larvicidal activity against Culex pipiens larvae, with an LC50 of 4 ng/mL. AChE/nAChR-IN-1 is utilized in research focused on controlling mosquito populations and studying mosquito-borne diseases. -
AChE Inhibitor
Sinapine is an acetylcholinesterase (AChE) inhibitor derived from cruciferous seeds. This compound demonstrates a range of biological activities, including anti-inflammatory, antioxidant, anti-tumor, anti-angiogenic, and radio-protective effects. Sinapine is instrumental in research targeting neurodegenerative disorders such as Alzheimer's disease, myasthenia gravis, ataxia, and Parkinson’s disease, making it a valuable tool for advancing scientific understanding in these areas. -
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. -
GABAA Receptor Chloride channel Inhibitor
Leptophos oxon is a potent GABAA receptor chloride channel inhibitor, exhibiting an IC50 value of 89.6 μM. This compound effectively inhibits GABA-induced chloride influx through binding to the TBPS sites associated with GABAA receptors, as well as inhibiting TBPS binding to voltage-dependent chloride channels. Leptophos oxon is primarily utilized in studies related to neurological diseases and functions as an insecticide, making it relevant for research in both neurobiology and pest management. -
GABA Receptor Inhibitor
Aminoxyacetic acid acts as an inhibitor of the GABA receptor by targeting the GABA-degrading enzyme GABA-T. Its primary mechanism disrupts the metabolism of gamma-aminobutyric acid, leading to increased GABA levels. This compound is valuable for research studies investigating GABAergic signaling, neuropharmacology, and the modulation of neurotransmitter dynamics in various models of neurological disorders. -
GABA Uptake Inhibitor
Nipecotic acid is a potent inhibitor of GABA uptake in neurons and glial cells, significantly impacting GABAergic neurotransmission. This compound has also been shown to directly activate GABAA-like chloride channels, with an effective concentration (EC50) of approximately 300 μM. Its biological activity makes nipecotic acid valuable for research applications focused on GABAergic signaling and associated neurological processes. -
GABA/mGAT2 Inhibitor
NNC 05-2090 hydrochloride is a potent inhibitor of GABA uptake, specifically targeting the β-GABA transporter (BGT-1) with an IC50 value of 10.6 μM, and exhibiting inhibitory activity against mGAT2 with a Ki of 1.4 μM. This compound demonstrates anticonvulsant properties, making it valuable for research in epilepsy and other neurological disorders. Its unique mechanism allows for exploration of GABAergic signaling pathways and therapeutic interventions in related conditions. -
GABA Transaminase Inhibitor
γ-Acetylenic GABA hydrochloride is an irreversible inhibitor of GABA transaminase, effectively increasing GABA levels in the brain. This compound is utilized in studies investigating the modulation of neurotransmitter systems and has applications in neuropharmacology. Additionally, γ-Acetylenic GABA hydrochloride serves as a click chemistry reagent, featuring an alkyne functional group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules. -
GABAA Receptor Inhibitor
FG 7142 is a non-selective inverse agonist of the GABAA receptor, exhibiting high affinity for the α1 subunit (Ki = 91 nM). It effectively modulates GABA-induced chloride flux at GABAA receptors containing the α1 subunit (EC50 = 137 nM). Additionally, FG 7142 has been shown to enhance tyrosine hydroxylation and upregulate β-adrenoceptors in the mouse cerebral cortex, making it valuable for research in neuropharmacology and the study of anxiety-related disorders. -
β1-containing GABAA Inhibitor
SCS (Salicylidene salicylhydrazide) is a selective allosteric inhibitor of β1-containing GABAA receptors, exhibiting a potency with an IC50 of 32 nM against the α2β1γ1θ subtype as determined by VIPR measurement. In addition to its inhibitory effects, SCS demonstrates metal ion chelation properties. This compound is valuable for research applications investigating GABAA receptor modulation and the role of metal ions in neuropharmacology. -
GABA Inhibitor
DL-Gabaculine hydrochloride is an irreversible inhibitor of bacterial pyridoxal phosphate-linked γ-aminobutyric acid-α-ketoglutaric acid transaminase, with a Ki of 2.86 μM. This neurotoxin effectively disrupts GABA metabolism, leading to increased levels of γ-aminobutyric acid in biological systems. It is utilized primarily in research applications focused on neuropharmacology and the study of neurotransmitter regulation. -
GABA Uptake Inhibitor
Arecaidine hydrochloride is a pyridine alkaloid that acts as a potent GABA uptake inhibitor. By functioning as a substrate for the H+-coupled amino acid transporter 1 (PAT1, SLC36A1), it competitively inhibits the uptake of L-proline. This compound is valuable for research into GABAergic signaling and neuropharmacology, aiding in the exploration of neurological disorders and potential therapeutic interventions. -
GABA Uptake Inhibitor
Spinacine ((S)-Spinacine) functions as a GABA uptake inhibitor, increasing synaptic GABA availability by inhibiting its reuptake in cortical neuronal tissues. This compound effectively modulates reflex responses in isolated spinal cord preparations and decreases motor activity, as well as reducing exploratory behaviors in conflict situations, such as approaching water dispensers. Additionally, Spinacine elevates pain sensitivity thresholds when administered via subarachnoidal injection, making it valuable for research in neuropharmacology and pain modulation studies. -
GABA Uptake Inhibitor
CI-966 hydrochloride is a selective GABA uptake inhibitor targeting the GABA transporter GAT-1. With IC50 values of 0.26 μM for human GAT-1 and 1.2 μM for rat GAT-1, it demonstrates over 200-fold selectivity compared to GAT-2, GAT-3, and BGT-3. This compound possesses anticonvulsant and neuroprotective properties, making it a valuable tool in neurological research and potential therapeutic applications. -
GABA Uptake Inhibitor
Guvacine hydrobromide is a potent GABA uptake inhibitor that specifically targets rat GABA transporters GAT-1, GAT-2, and GAT-3 with IC50 values of 39 μM, 58 μM, and 378 μM, respectively. This compound is derived from the nut of Areca catechu and plays a significant role in modulating GABAergic neurotransmission. Guvacine hydrobromide is particularly valuable for research applications focused on neuropharmacology and the exploration of GABA-related pathways in various physiological and pathological conditions. -
GABA Uptake Inhibitor
Arecaidine hydrobromide is a pyridine alkaloid that functions as a potent GABA uptake inhibitor. It acts as a substrate for the H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits the uptake of L-proline. This compound is utilized in research exploring GABAergic signaling and transport mechanisms, providing insights into neurological conditions and potential therapeutic strategies. -
GABA Transaminase Inhibitor
γ-Acetylenic GABA serves as an irreversible inhibitor of GABA-transaminase, effectively elevating GABA levels in the rat brain. It is utilized in research to investigate the modulation of GABAergic neurotransmission. Additionally, γ-Acetylenic GABA features an alkyne group, making it suitable for click chemistry applications, particularly copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing substrates. -
GABA Transaminase Inhibitor
L-DABA hydrobromide is a GABA transaminase inhibitor, known for its ability to modulate gamma-aminobutyric acid (GABA) levels. With an IC50 greater than 500 μM, it demonstrates weak inhibition of this enzyme. Additionally, L-DABA has shown antitumor activity in both in vivo and in vitro studies, making it a valuable compound for research in cancer biology and neurochemical signaling. -
AChE Inhibitor/GABAA Receptor Antagonist
Bis(7)-tacrine dihydrochloride is a dimeric inhibitor of acetylcholinesterase (AChE) and a potent antagonist of GABAA receptors. This compound exhibits neuroprotective properties by preventing glutamate-induced neuronal apoptosis through NMDA receptor blockade. Bis(7)-tacrine dihydrochloride is valuable for research applications related to Alzheimer's disease and other neurological disorders. -
GABA(A) Receptor Inhibitor
MIDD0301 is a potent inhibitor of the γ-aminobutyric acid type A (GABA(A)) receptor, demonstrating significant biological activity as an anti-asthmatic agent. This compound effectively relaxes histamine-contracted airway smooth muscle in both guinea pigs and humans, making it relevant for research into bronchoconstrictive diseases. Furthermore, MIDD0301 has shown immunotoxicological safety in mice, exhibiting no adverse effects on lymphocyte, monocyte, or granulocyte populations with repeated dosing. -
GABA Receptor Inhibitor
Sandaracopimaric acid is a diterpenoid that functions as a GABA receptor inhibitor. It exhibits significant anti-inflammatory properties and has been shown to reduce the contraction of phenylephrine-induced pulmonary arteries, with an EC50 value of 43.93 μM. This compound is useful for research applications in studying the modulation of GABAergic signaling and its effects on vascular tone. -
GABA Uptakp Inhibitor
Guvacine, a GABA uptake inhibitor derived from the nut of Areca catechu, selectively targets GABA transporters. It demonstrates potent inhibition of rat GAT-1, GAT-2, and GAT-3, with IC50 values of 39 μM, 58 μM, and 378 μM, respectively. This compound is instrumental in studies investigating GABAergic signaling and its implications in neurological research. Guvacine's properties make it a valuable tool for exploring therapeutic approaches for disorders linked to altered GABA uptake. -
GABA/mGAT2 Inhibitor
NNC 05-2090 is a GABA uptake inhibitor that primarily targets the β-GABA transporter (BGT-1) with an IC50 of approximately 10.6 μM, and exhibits potent inhibition of mGAT2 with a Ki value of 1.4 μM. This compound demonstrates anticonvulsant activity, making it a valuable tool for investigating epilepsy and other neurological conditions. Its effectiveness in modulating GABA transport provides insights into potential therapeutic strategies for neurological disorders.
