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synaptic blocking

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37

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7

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3

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0527A
    Amitriptyline hydrochloride
    5+ Cited Publications

    Serotonin Transporter 5-HT Receptor mAChR Histamine Receptor Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis Neurological Disease Inflammation/Immunology Endocrinology
    Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity .
    Amitriptyline hydrochloride
  • HY-B0527
    Amitriptyline
    5+ Cited Publications

    Serotonin Transporter Trk Receptor Sodium Channel 5-HT Receptor Histamine Receptor Adrenergic Receptor mAChR Potassium Channel Dopamine Transporter Apoptosis Neurological Disease Inflammation/Immunology Endocrinology
    Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with Ki = 2.58 μM). Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity .
    Amitriptyline
  • HY-103259
    Sodium metatungstate
    Maximum Cited Publications
    11 Publications Verification

    Sodium polyoxotungstate; POM-1

    Phosphatase P2X Receptor P2Y Receptor Pyroptosis Interleukin Related Neurological Disease Inflammation/Immunology Cancer
    Sodium metatungstate (Sodium polyoxotungstate) is a NTPDase inhibitor, with Ki values of 2.58 μM, 3.26 μM, and 28.8 μM for NTPDase 1 (CD39), NTPDase 3 and NTPDase 2 respectively . Sodium metatungstate has anti-inflammatory and anti-cancer effect. Sodium metatungstate inhibits ATP breakdown but also blocks central synaptic transmission .
    Sodium metatungstate
  • HY-P0062B
    Ziconotide acetate
    2 Publications Verification

    SNX-111 acetate

    Calcium Channel Cardiovascular Disease Inflammation/Immunology Cancer
    Ziconotide acetate (SNX-111 acetate), a peptide, is a potent and selective block of N-type calcium channels antagonist. Ziconotide acetate reduces synaptic transmission, and can be used for chronic pain research .
    Ziconotide acetate
  • HY-B0590
    Tetrabenazine
    1 Publications Verification

    Ro 1-9569

    Monoamine Transporter Dopamine Receptor Neurological Disease
    Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
    Tetrabenazine
  • HY-B0590S

    Ro 1-9569-d6

    Monoamine Transporter Neurological Disease
    Tetrabenazine-d6 (Deutetrabenazine) is a deuterium-labled Tetrabenazine (HY-B0590). Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
    Tetrabenazine-d6
  • HY-10035
    TTA-P2
    2 Publications Verification

    T-Type calcium channel inhibitor

    Calcium Channel Neurological Disease
    TTA-P2 (T-Type calcium channel inhibitor) is a selective, orally active, and BBB-penetrant T-type calcium channel blocker (IC50 = 22 nM). TTA-P2 reduces mechanical hypersensitivity and alleviates acute as well as chronic pain. TTA-P2 significantly reduces firing rates in temporal lobe epilepsy (TLE) neurons to control levels and suppresses synaptically evoked burst firing. TTA-P2 can be studied in research for neurological diseases such as tremor and absence epilepsy < sup>[4] .
    TTA-P2
  • HY-134356

    AICAR-5'-MP

    Endogenous Metabolite Others
    AICA-riboside, 5′-phosphate is AICA riboside with a phosphate group. The functions of AICA riboside include: 1) conversion into AMP mimetic to selectively activate AMPK; 2) competition with adenosine for the uptake of nucleoside transporters, reversible blocking of adenosine reuptake, increasing extracellular adenosine concentration, and indirectly activating adenosine A1 receptors. AICA riboside is involved in metabolic regulation (promoting catabolism and inhibiting anabolism) and adenosine-dependent neuroprotection (inhibiting excitatory synaptic transmission). AICA riboside can be used in the study of metabolic diseases (such as diabetes and obesity) and neurological diseases (such as ischemia and epilepsy), and has central nervous system protective activity .
    AICA-riboside, 5′-phosphate
  • HY-P0062

    SNX-111

    Calcium Channel Neurological Disease Inflammation/Immunology Cancer
    Ziconotide (SNX-111), a peptide, is a potent and selective block of N-type calcium channels antagonist. Ziconotide reduces synaptic transmission, and can be used for chronic pain research .
    Ziconotide
  • HY-113788

    Pyk2 p38 MAPK Amyloid-β Neurological Disease Inflammation/Immunology
    PF-719 is a highly selective Pyk2 inhibitor with an IC50 value of 17 nM. PF-719 promotes the activation of LKB1 and p38 MAPK. PF-719 blocks synaptic deficits induced by Amyloid-beta oligomers and reverses the inhibition of long-term potentiation induced by β-amyloid oligomers. PF-719 can be used in research related to Alzheimer's disease and autoimmune diseases .
    PF-719
  • HY-P2259
    TAT-GluA2 3Y
    2 Publications Verification

    iGluR Neurological Disease
    TAT-GluA2 3Y, an interference peptide, blocks long-term depression (LTD) at glutamatergic synapses by disrupting the endocytosis of AMPAR. TAT-GluA2 3Y can alleviate Pentobarbital-induced spatial memory deficits and synaptic depression .
    TAT-GluA2 3Y
  • HY-B0590A

    Ro 1-9569 Racemate

    Monoamine Transporter Dopamine Receptor Neurological Disease
    Tetrabenazine (Ro 1-9569) Racemate is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine Racemate binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine Racemate weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine Racemate can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
    Tetrabenazine Racemate
  • HY-164288

    TDI-006570

    Cyclic GMP-AMP Synthase STING Neurological Disease Inflammation/Immunology
    TDI-6570 (TDI-006570) is a blood-brain barrier-permeable, orally active cGAS inhibitor with an IC50 of 1.64 μM. TDI-6570 exhibits high gastrointestinal absorption and a long brain half-life in mice, and shows no toxicity to primary neurons. By inhibiting the cGAS-STING-IFN signaling pathway, TDI-6570 reduces STING levels and the activation of TBK1, blocks double-stranded DNA-induced cGAS activation and downstream interferon-stimulated gene expression, thereby reducing tau protein spread and improving synaptic loss. TDI-6570 reverses memory deficits, increases the amplitude of long-term potentiation, enhances the MEF2C transcriptional network, restores PSD-95 and vGAT punctate structures, and significantly improves cognitive resilience. TDI-6570 can be applied to the research of Alzheimer's disease, Parkinson's disease, systemic lupus erythematosus, as well as various central nervous system and autoimmune diseases .
    TDI-6570
  • HY-113995
    (-)-Vesamicol
    1 Publications Verification

    (-)-AH5183

    mAChR Neurological Disease
    (-)-Vesamicol (AH5183) is a vesicular acetylcholine transporter inhibitor. (-)-Vesamicol reversibly and non-competitively inhibits the transport of acetylcholine into circulating synaptic vesicles and blocks the activity of vesicular acetylcholine transporters in medial amygdala neurons. (-)-Vesamicol is applicable to research related to central precocious puberty .
    (-)-Vesamicol
  • HY-P0099

    nAChR Others
    Pentapeptide-3 is a pentapeptide fragment of neurotoxin waglerin-1, it can be extracted from the venom of Temple Viper. Pentapeptide-3 is a competitive antagonist of nicotinic acetylcholine receptors (nAChRs), it can blocks nerves at the post-synaptic membrane. Pentapeptide-3 has anti-aging effects and it can be used together with other cosmetic peptides .
    Pentapeptide-3
  • HY-121964

    iGluR Neurological Disease
    Cis-piperidine-2,3-dicarboxylic acid is a non-specific antagonist of NMDA, AMPA and kainate ionotropic receptors and a partial agonist for NMDA receptors. Cis-piperidine-2,3-dicarboxylic acid can be used in blocking general excitatory synaptic transmissions .
    cis-Piperidine-2,3-dicarboxylic acid
  • HY-B0527AR
    Amitriptyline hydrochloride (Standard)
    4 Publications Verification

    Reference Standards Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis Neurological Disease Inflammation/Immunology Endocrinology
    Amitriptyline hydrochloride (Standard) is the analytical standard of Amitriptyline hydrochloride (HY-B0527A). This product is intended for research and analytical applications. Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
    Amitriptyline hydrochloride (Standard)
  • HY-B0527AS

    Isotope-Labeled Compounds Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis Neurological Disease Inflammation/Immunology Endocrinology
    Amitriptyline-d6 hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
    Amitriptyline-d6 hydrochloride
  • HY-100714B

    L-APV; L-2-Amino-5-phosphonovaleric acid

    iGluR Neurological Disease
    L-AP5 (L-APV; L-2-Amino-5-phosphonovaleric acid) is an NMDA antagonist and is the isomer of D-AP5 (HY-100714A). L-AP5 shows a relatively weak amino acid and synaptic blocking activity .
    L-AP5
  • HY-107605

    iGluR Neurological Disease
    UBP296 is a potent and selective antagonist of GLUK5-containing kainate receptor in the spinal cord. UBP296 reversibly blocks ATPA-induced depressions of synaptic transmission, and affects AMPA receptor-mediated synaptic transmission directly in rat hippocampal slices .
    UBP296
  • HY-P1054

    YNVYGIEEVKI

    PKC Neurological Disease
    pep2-EVKI (YNVYGIEEVKI) is an inhibitor peptide that selectively blocks PICK1 interactions, caused the opposite effects on synaptic AMPAR function to PICK1 expression .
    pep2-EVKI
  • HY-100785A

    γDGG acetate; γ-D-Glutamylglycine acetate

    iGluR Neurological Disease
    gamma-DGG acetate (γDGG acetate) is a competitive AMPA receptor blocker. gamma-DGG acetate is also a reversible Excitatory post-synaptic potentials (e.p.s.p.s) antagonist .
    gamma-DGG acetate
  • HY-P0062A

    SNX-111 TFA

    Calcium Channel Neurological Disease Inflammation/Immunology Cancer
    Ziconotide TFA (SNX-111 TFA), a peptide, is a potent and selective block of N-type calcium channels antagonist. Ziconotide TFA reduces synaptic transmission, and can be used for chronic pain research .
    Ziconotide TFA
  • HY-169871

    iGluR Neurological Disease
    Argiotoxin 636 is a toxin and the non-specific, non-competitive, and potent ionotropic glutamate receptor (iGluR) antagonist. Argiotoxin 636 blocks excitatory synaptic transmission in neurons and has paralysis and muscle relaxation effects. Argiotoxin 636 can be used in the study of nervous system diseases .
    Argiotoxin 636
  • HY-P10630

    Amyloid-β Neurological Disease
    Pep63 is a neuroprotective peptide (VFQVRARTVA). Pep63 has a neuroprotective effect on synaptic plasticity and memory. Pep63 can competitively bind with Aβ1-42 oligomers, and can block Aβ fiber formation. Pep63 can be used for Alzheimer’s disease (AD) research .
    Pep63
  • HY-175300

    Cholinesterase (ChE) Neurological Disease
    AChE-IN-92 (Compound L4R1-3) is a highly selective acetylcholinesterase (AChE) inhibitor (IC50=4.6 nM). AChE-IN-92 blocks acetylcholine hydrolysis and elevates synaptic acetylcholine levels. AChE-IN-92 is promising for research of Alzheimer’s disease (AD) .
    AChE-IN-92
  • HY-B0590E

    Ro 1-9569 mesylate

    Monoamine Transporter Dopamine Receptor Neurological Disease
    Tetrabenazine (Ro 1-9569) mesylate is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine mesylate binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine mesylate weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine mesylate can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
    Tetrabenazine mesylate
  • HY-B1789

    mAChR Neurological Disease
    Telenzepine is an antimuscarinic agent with Kis of 0.94 nM (M1 mAChR) and 17.8 nM (M2 mAChR) binding to muscarinic receptors. Telenzepine effectively blocks synaptic transmission promoted by muscarinic or M1 receptor agonists. Thus, Telenzepine can reduce the amplitude of extracellular slow excitatory postsynaptic potentials (EC50=38 nM) and slow inhibitory postsynaptic potentials (EC50=253 nM) .
    Telenzepine
  • HY-108578

    Potassium Channel Neurological Disease
    RuBi-4AP, a derivative of 4-aminopyridine (4AP; HY-B0604), is a caged Kv channel blocker. RuBi-4AP contains a photolabile protecting group, allowing its effect to be controlled precisely in both space and time with light. RuBi-4AP can be used for the research of neuronal excitability, synaptic transmission, and signal propagation .
    RuBi-4AP
  • HY-B0590R

    Ro 1-9569 (Standard)

    Reference Standards Monoamine Transporter Dopamine Receptor Neurological Disease
    Tetrabenazine (Standard) is the analytical standard of Tetrabenazine (HY-B0590). This product is intended for research and analytical applications. Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
    Tetrabenazine (Standard)
  • HY-B0590S3

    TBZ-d7-d7; Ro 1-9569-d7

    Isotope-Labeled Compounds Monoamine Transporter Dopamine Receptor Neurological Disease
    Tetrabenazine-d7 (TBZ-d7-d7) is deuterium labeled Tetrabenazine (HY-B0590). Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
    Tetrabenazine-d7
  • HY-W795736

    (+)-AH5183

    nAChR Neurological Disease
    (+)-Vesamicol ((+)-AH5183) is an acetylcholine vesicular transport system inhibitor. (+)-Vesamicol blocks acetylcholine storage and uptake by synaptic vesicles, reducing transmitter availability for neuromuscular junction release. (+)-Vesamicol acts as a neuromuscular blocking agent, producing frequency-dependent neuromuscular block in rat hemidiaphragm preparations .
    (+)-Vesamicol
  • HY-183910

    GABA Receptor Glycine Receptor (GlyR) Neurological Disease
    Pitrazepin is a GABAA receptor antagonist and glycine receptor antagonist. Pitrazepin blocks synaptic GABA action, induces neuronal bursting and reduces inhibitory postsynaptic potentials. Pitrazepin can be used in research on depression and psychosis .
    Pitrazepin
  • HY-183269

    Serotonin Transporter Neurological Disease
    SERT-IN-5 is a potent, selective, and CNS-penetrant serotonin transporter (SERT) inhibitor with a Ki of 0.3 nM. SERT-IN-5 blocks serotonin reuptake to increase synaptic serotonin levels. SERT-IN-5 exhibits anti-anxiety effects in mice. SERT-IN-5 can be used for the research of anxiety, depression .
    SERT-IN-5
  • HY-180370

    NitroSynapsin; YQW-036; NMI-6979

    iGluR Drug Derivative Cardiovascular Disease Neurological Disease
    Nitromemantine (NitroSynapsin) is a nitrate derivative of Memantine (HY-B0591) and is a dual-functional NMDAR antagonist. Nitromemantine exhibits significant efficacy in rodent models of cerebral infarction through a dual mechanism of blocking channels and regulating receptors via NO/redox regulation. Nitromemantine can target ischemic neurons under hypoxic conditions and enhance its activity. Nitromemantine inhibits the current induced by NMDA, with its IC50 being 2.4 μM. Nitromemantine can be used for the study of cerebral ischemic stroke .
    Nitromemantine
  • HY-10035R

    T-Type calcium channel inhibitor (Standard)

    Calcium Channel Reference Standards Neurological Disease
    TTA-P2 (Standard) is the analytical standard of TTA-P2 (HY-10035). This product is intended for research and analytical applications. TTA-P2 (T-Type calcium channel inhibitor) is a selective, orally active, and BBB-penetrant T-type calcium channel blocker (IC50 = 22 nM). TTA-P2 reduces mechanical hypersensitivity and alleviates acute as well as chronic pain. TTA-P2 significantly reduces firing rates in temporal lobe epilepsy (TLE) neurons to control levels and suppresses synaptically evoked burst firing. TTA-P2 can be studied in research for neurological diseases such as tremor and absence epilepsy < sup> .
    TTA-P2 (Standard)
  • HY-182707

    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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