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inhibitory currents

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-147423
    Zandatrigine
    1 Publications Verification

    NBI-921352; XEN901

    		 Sodium Channel Neurological Disease
    Zandatrigine (NBI-921352; XEN901) is a selective, orally active, voltage-gated sodium channel NaV1.6/SCN8A inhibitor that can penetrate the blood-brain barrier. Zandatrigine inhibits sodium influx by non-covalently binding to the VSD4 structure of NaV1.6, blocking the persistent and resuscitative currents under pathological conditions. Zandatrigine can reduce neuronal hyperexcitability and reduce epileptic seizures. Zandatrigine is 134-756-fold selective for other isoforms such as NaV1.1 and NaV1.2, and has minimal effect on NaV1.1 expressed by inhibitory interneurons. Zandatrigine can be used to study NaV1.6-mediated neuroexcitability diseases such as SCN8A-related developmental epileptic encephalopathy (SCN8A-DEE) and adult focal epilepsy .
    Zandatrigine
  • HY-12882A
    Ifenprodil tartrate
    Maximum Cited Publications
    10 Publications Verification

    NP-120 tartrate; RC-61-91 tartrate

    		 iGluR Adrenergic Receptor Potassium Channel Calcium Channel Influenza Virus Infection Neurological Disease
    Ifenprodil (NP-120) tartrate, a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil tartrate is an α1 adrenergic receptor antagonist. Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has reliable inhibitory effects against A/H1N1 strains (EC50 of 6.6 µM). Ifenprodil tartrate has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil tartrate can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease .
    Ifenprodil tartrate
  • HY-N7110
    6-Hydroxyflavone
    2 Publications Verification

    		 Akt ERK JNK GABA Receptor Neurological Disease Metabolic Disease Inflammation/Immunology
    6-Hydroxyflavone is an orally effective flavonoid compound. 6-Hydroxyflavone can inhibit LPS (HY-D1056) -induced NO production and has anti-inflammatory effects. 6-Hydroxyflavone promotes osteoblast differentiation by activating AKT, ERK 1/2 and JNK signaling pathways. 6-Hydroxyflavone has an inhibitory effect on bovine hemoglobin (BHb) glycosylation. 6-Hydroxyflavone has a kidney protective effect. In addition, 6-Hydroxyflavone enhances GABA-induced current through the Benzodiazepine sites of γ-aminobutyric acid (GABAA) receptors. 6-Hydroxyflavone shows a clear preference for α2 - and α3 - subtypes, which play an anti-anxiety role .
    6-Hydroxyflavone
  • HY-109968
    Irdabisant

    CEP-26401

    		 Histamine Receptor Neurological Disease Metabolic Disease
    Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment .
    Irdabisant
  • HY-12882
    Ifenprodil
    Maximum Cited Publications
    10 Publications Verification

    NP-120; RC-61-91

    		 iGluR Adrenergic Receptor Potassium Channel Calcium Channel Influenza Virus Infection Neurological Disease
    Ifenprodil (NP-120), a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil is an α1 adrenergic receptor antagonist. Ifenprodil inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil has reliable inhibitory effects against A/H1N1 strains (EC50 of 6.6 µM). Ifenprodil has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease .
    Ifenprodil
  • HY-N2255
    Crebanine
    4 Publications Verification

    		 Akt Apoptosis NF-κB Reactive Oxygen Species (ROS) p38 MAPK ERK Interleukin Related TNF Receptor NO Synthase nAChR Bacterial Cancer
    Crebanine is an isoquinoline-like alkaloid that can be derived from Stephania. Crebanine is an antagonist of the α7-nAChR with an IC50 of 19.1 μM. Crebanine suppresses the proliferation, migration, and invasion of cancer cells, triggers reactive oxygen species (ROS) burst, and promotes apoptosis. Crebanine inhibits the AKT/FoxO3a, NF-κB and MAPK signaling pathways. Crebanine attenuates NOX2 hyperactivation, exhibits antioxidant properties by reducing reactive oxygen species and peroxidation in microglia cells. Crebanine inhibits voltage-dependent Na + current in guinea-pig ventricular myocytes. Crebanine has high inhibitory activity against gram-positive animal pathogenic bacteria. Crebanine ameliorates ischemia-reperfusion brain damage in middle cerebral artery occlusion and reperfusion (MCAO/R) rats. Crebanine significantly improves Scopolamine (HY-N0296)-induced cognitive deficits in ICR mice. Crebanine can be used for the study of hepatocellular carcinoma (HCC), cerebral ischemia and Alzheimer's disease .
    Crebanine
  • HY-P1073
    ProTx-I

    		Calcium Channel Potassium Channel Sodium Channel TRP Channel Neurological Disease Cancer
    ProTx-I is a toxin derived from Thrixopelma pruriens and a peptide inhibitor targeting TTX-resistant sodium channels. ProTx-I interacts with voltage sensors of multiple domains such as NaV1.7, reduces neuronal excitability through allosteric modulation of channel gating and alteration of voltage dependence. The IC50 values of ProTx-I against human NaV1.7, NaV1.2, NaV1.6, and NaV1.5 are 95 nM, 104 nM, 21 nM, and 358 nM, respectively; ProTx-I also potently inhibits Ba 2+ currents of hCav3.1, while its inhibitory potency against hCav3.2 is approximately 160-fold lower. ProTx-I is applicable to the research of chronic pain .
    ProTx-I
  • HY-P4397
    (d(CH2)51,Tyr(Me)2,Thr4,Orn8,des-Gly-NH29)-Vasotocin

    		Oxytocin Receptor Endocrinology
    (d(CH2)51,Tyr(Me)2,Thr4,Orn8,des-Gly-NH29)-Vasotocin, an oxytocin receptor antagonist, abolishes oxytocin-enhanced inhibitory postsynaptic currents in CA1 pyramidal neurons .
    (d(CH2)51,Tyr(Me)2,Thr4,Orn8,des-Gly-NH29)-Vasotocin
  • HY-135809
    A2764 dihydrochloride

    		Potassium Channel Neurological Disease
    A2764 dihydrochloride is a highly selective inhibitor of TRESK (TWIK-related spinal cord K + channel, K2P18.1), which has moderate inhibitory effects on TREK-1 and TALK-1. A2764 dihydrochloride is more sensitive to the activated mTRESK channels (IC50=6.8 μM) than the basal current. A2764 dihydrochloride can lead to cell depolarization and increased excitability in native cells, it has the potential for probing the role of TRESK channel in migraine and nociception .
    A2764 dihydrochloride
  • HY-P5183
    Hm1a

    		Sodium Channel Neurological Disease
    Hm1a is a venom peptide and a selective hNaV1.1 activator with an EC50 of 7.5 nM. Hm1a enhances hNaV1.1 and hNaV1.3 channel currents via delayed inactivation. Hm1a restores action potential firing in Dravet syndrome GABAergic inhibitory interneurons, reduces interictal epileptiform discharges and whole-brain hyperexcitability, lowers seizure frequency, and rescues premature death in Dravet syndrome mice. Hm1a can be used for the research of neurological disease, such as Dravet syndrome .
    Hm1a
  • HY-106888
    CS-722 Free base

    		Endogenous Metabolite Neurological Disease
    CS-722 Free base is a synthesized centrally acting muscle relaxant, and has a muscle relaxant activity and depressant effectson the spinal reflex . CS-722 Free base inhibits spontaneous inhibitory postsynaptic currents and excitatory postsynaptic currents in hippocampal cultures probably by an inhibition of both sodium and calcium currents .
    CS-722 Free base
  • HY-100372
    E4CPG

    (RS)-ECPG

    		 mGluR Neurological Disease
    E4CPG ((RS)-ECPG) is a Group I/Group II metabotropic glutamate receptor (mGluR) antagonist. E4CPG can inhibit the paired-pulse ratio of monosynaptic inhibitory postsynaptic currents (IPSC) potentiation .
    E4CPG
  • HY-172140
    Ebio3

    		Potassium Channel Neurological Disease
    Ebio3 is a selective potassium channel (KCNQ2) inhibitor with an IC50 of 1.2 nM. Ebio3 binds to the KCNQ2 channel through its hydrophobic tail, causing the S6 helix to move inward, which leads to the closure of the inner gate. The inhibitory effect of Ebio3 is also effective in pathogenic mutants of KCNQ2 (such as R75C and I238L), where it can inhibit outward currents by more than 80%. Ebio3 is expected to be used in the research of neurological diseases such as epilepsy .
    Ebio3
  • HY-156061
    NAP-1

    		GABA Receptor Neurological Disease Inflammation/Immunology
    NAP-1 is a compound with agent that can suppress or relieve pain. effects. NAP-1 enhances the inhibitory current by binding to a specific site of GABAaR, resulting in a narcotic effect. NAP-1 can be used in research to develop clinical agent that can suppress or relieve pain .
    NAP-1
  • HY-131885
    RuBi-Glutamate hexafluorophosphate sodium

    		GABA Receptor Neurological Disease
    RuBi-Glutamate hexafluorophosphate sodium is a neuronal activator. RuBi-Glutamate hexafluorophosphate sodium photocleaves to release glutamate upon one- or two-photon excitation, activating glutamate receptors in cortical pyramidal neurons. RuBi-Glutamate hexafluorophosphate sodium reduces peak amplitude of evoked GABAergic inhibitory postsynaptic currents in its caged form. RuBi-Glutamate hexafluorophosphate sodium can be used for the research of Huntington's disease .
    RuBi-Glutamate hexafluorophosphate sodium
  • HY-135228
    GZ4

    		Calcium Channel Neurological Disease
    GZ4 is a calcium current inhibitor with direct inhibitory activity on cell surface channels. GZ4 inhibition reverses mechanical hyperalgesia/hyperalgesia in a spinal nerve ligation-induced neuropathic pain model. The mechanism of action of GZ4 is similar to that of gabapentin, but the time course of its biological effects is more rapid, indicating that GZ4 can directly inhibit calcium channel currents .
    GZ4
  • HY-161472
    Aldose reductase-IN-7

    		Aldose Reductase Cancer
    Aldose reductase-IN-7 (Compound 6k) targets Aldose reductase. Aldose reductase-IN-7 exhibits potent enzyme inhibitory activity (Ki = 0.186 ± 0.020 μM), showing superiority to Epalrestat (HY-66009), which is currently in clinical use. Aldose reductase-IN-7 is less cytotoxic and possesses potent anticancer activity .
    Aldose reductase-IN-7
  • HY-108204
    AZD 3043

    THRX 918661

    		 GABA Receptor Others
    AZD 3043 (THRX 918661) is a positive allosteric modulator of GABA(A) receptors with sedative and hypnotic activity. AZD 3043 can enhance GABA(A) receptor-mediated chloride currents in vitro and produce hypnotic and electroencephalographic inhibitory effects in vivo. Due to its esterase-dependent metabolic pathway, it has a short duration of action and can be quickly cleared even after long-term infusion, which may have clinical application potential.
    AZD 3043
  • HY-W710915
    Aprindine hydrochloride-d10

    		Isotope-Labeled Compounds Potassium Channel Cardiovascular Disease
    Aprindine hydrochloride-d10 is the deuterium labeled Aprindine hydrochloride (HY-A0236A). Aprindine hydrochloride is a class I-b anti-arrhythmic agent and a hERG channel blocker with an IC50 of 0.23 μM. Aprindine hydrochloride has inhibitory effects on Na+/Ca2+ exchanger currents, which is partly responsible for their antiarrhythmic and cardioprotective effects. Aprindine hydrochloride is widely used for trial and ventricular tachyarrhythmias research research.
    Aprindine hydrochloride-d10
  • HY-107717
    MNI-caged-NMDA

    		iGluR Neurological Disease
    MNI-caged-NMDA is a light-sensitive amino acid with rapid release properties suitable for use in the study of fast synaptic receptor mechanisms. MNI-caged-NMDA shows metered release of NMDA receptors, inducing rapid and sustained receptor activation in cerebellar interneurons. MNI-caged-NMDA is able to achieve rapid transient responses and generate large inward currents by local laser photolysis. The use of MNI-caged-NMDA can effectively study neurotransmitter signaling and its inhibitory effects on GABA-A receptors .
    MNI-caged-NMDA
  • HY-174431
    PAN endonuclease-IN-3

    		Endonuclease Influenza Virus Infection
    PAN endonuclease-IN-3 is a potent PAN endonuclease inhibitor that against influenza virus polymerase complexes with an IC50 of 17.4 nM. PAN endonuclease-IN-3 demonstrates potent inhibitory activities against PAN endonuclease. PAN endonuclease-IN-3 demonstrates robust antiviral activities against multiple current and different influenza virus strains while showing minimal cytotoxicity in MDCK cells. PAN endonuclease-IN-3 significantly suppresses viral replication in an A/WSN/33 infected mouse model.
    PAN endonuclease-IN-3
  • HY-109968A
    Irdabisant hydrochloride

    CEP-26401 hydrochloride

    		 Histamine Receptor Neurological Disease
    Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment .
    Irdabisant hydrochloride
  • HY-19397
    BMS-223131

    		Potassium Channel Cytochrome P450 Neurological Disease
    BMS-223131 (Compound 1) is a potent maxi-K potassium channel opener. BMS-223131 has a strong inhibitory effect on the CYP2C9 enzyme (IC50 = 1.7 μM) and also shows varying degrees of inhibition on other common CYP enzymes such as CYP1A2, CYP2C19, CYP2D6, and CYP3A4. BMS-223131 can enhance the outward current mediated by maxi-K, by promoting K + efflux to hyperpolarize the cell membrane and reducing Ca 2+ influx. BMS-223131 can be used for the research of neurological disease, such as stroke .
    BMS-223131
  • HY-116142
    CP-283097

    		iGluR Neurological Disease
    CP-283097 is an orally active and conformationally restricted and NR2B subtype-selective NMDA antagonist. CP-283097 efficiently competitively inhibits the binding of [³H]CP-101,606 to the rat meninges, with an IC50 value of 18 nM. CP-283097 exhibits nearly complete inhibition of the current mediated by the NR2B receptor (IC50 = 206 nM), while the inhibitory effect on the NR2A or NR2C receptors is very weak. CP-283097 demonstrates excellent central nervous system permeability and in vivo efficacy in animal models. CP-283097 can be used for neurological diseases related to excessive activation of NMDA receptors .
    CP-283097
  • HY-124057
    RO5126946

    		nAChR Neurological Disease
    RO5126946 is a selective, orally active α7 nAChR allosteric potentiator with EC50 values of 0.06 μM (hα7 nAChR) and 770 nM (α7 nAChR), and it crosses the blood-brain barrier. RO5126946 enhances synaptic transmission and positively modulates GABA-ergic responses by increasing peak current, slowing current decay, and elevating the frequency of spontaneous inhibitory postsynaptic currents, without affecting the recovery of receptors from the desensitized state. RO5126946 not only enhances subthreshold nicotine effects and improves associative learning, but also does not interfere with the original pro-cognitive effects of nicotine. RO5126946 can be used to study cognitive impairments associated with diseases such as Alzheimer's disease and schizophrenia .
    RO5126946
  • HY-106888A
    CS-722

    		Endogenous Metabolite Neurological Disease
    CS-722 is a centrally acting muscle relaxant, and has a muscle relaxant activity and depressant effectson the spinal reflex[1]. CS-722 inhibits spontaneous inhibitory postsynaptic currents and excitatory postsynaptic currents in hippocampal cultures probably by an inhibition of both sodium and calcium currents .
    CS-722
  • HY-Y0282
    Sodium bromide

    NSC 77384; Sanibrom 40

    		 Environmental Pollutants Neurological Disease
    Sodium bromide (NSC 77384; Sanibrom 40) is a GABA-ergic system modulator that crosses the blood-brain barrier, and it effectively reduces and blocks epileptiform discharges. Sodium bromide exerts significant anticonvulsant effects by enhancing GABA-ergic inhibitory functions, such as increasing the amplitude of inhibitory postsynaptic currents and paired-pulse inhibition. Sodium bromide specifically enhances stimulation-induced extracellular alkalosis without affecting baseline pH or subsequent acidosis processes. Sodium bromide exhibits species-specific pharmacokinetic characteristics, competes with chloride ions for renal tubular reabsorption sites, and serves as a marker for extracellular fluid volume. Sodium bromide can be used in the research of epilepsy and related neurological diseases .
    Sodium bromide
  • HY-183101
    AMPAR modulator-12

    		iGluR NADPH Oxidase Neurological Disease
    AMPAR modulator-12 is a blood-brain barrier-permeable AMPAR positive allosteric modulator. AMPAR modulator-12 reduces NOX-1 expression, enhances AMPAR-mediated currents, promotes excitatory postsynaptic transmission and restores AMPAR function. AMPAR modulator-12 enhances excitatory and inhibitory synaptic transmission, reduces burst firing in the lateral habenula after withdrawal, and produces rapid and sustained antidepressant-like effects. AMPAR modulator-12 is applicable for the research of depression .
    AMPAR modulator-12
  • HY-182707
    JWX-A0108

    		nAChR Interleukin Related TNF Receptor NF-κB Neurological Disease
    JWX-A0108 is a selective human α7 nAChR positive allosteric modulator with an EC50 of 4.35 μM. JWX-A0108 potentiates α7 nAChR currents only in the presence of acetylcholine, with no direct activating effect or alteration of desensitization. JWX-A0108 enhances hippocampal GABAergic synaptic transmission by increasing spontaneous inhibitory postsynaptic currents. JWX-A0108 reduces the brain expression levels of IL-1β, TNF-α, and IL-6 by blocking the NF-κB signaling pathway, and reduces microglial activation by downregulating Iba1. JWX-A0108 effectively improves cognitive deficits, neuroinflammation, and hippocampal neuronal damage in mouse models of schizophrenia and Alzheimer's disease. JWX-A0108 can be used for research related to schizophrenia and Alzheimer's disease .
    JWX-A0108

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