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brain cortex

" in MedChemExpress (MCE) Product Catalog:

58

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1

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3

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1

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1

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6

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15498
    Rimegepant
    Maximum Cited Publications
    10 Publications Verification

    BMS-927711; BHV-3000

    		 CGRP Receptor Neurological Disease
    Rimegepant (BMS-927711) is an orally bioavailable and blood-brain barrier permeable antagonist of CGRP and AMY1 receptors, with a pIC50 of 8.01 and a Ki of 0.027 nM for human CGRP receptors. Rimegepant antagonizes cAMP production induced by αCGRP, βCGRP and amylin at CGRP and AMY1 receptors in humans, rats and mice, as well as at rat AMY3 receptors. Rimegepant can be used in research related to migraine .
    Rimegepant
  • HY-W115718
    Cuprizone
    3 Publications Verification

    		 Dopamine β-hydroxylase Neurological Disease
    Cuprizone is a copper chelating agent that forms a deep blue copper ketone complex with copper (II). The copper ketone reaction can be used in colorimetric tests for the presence of trace copper. Cuprizone can be used to induce some schizophrenia-like behavior in mice. Cuprizone acts on copper enzymes, including SOD1, cytochrome oxidase, and DβH, thereby causing oxidative stress and increasing DA levels in certain brain regions such as the medial prefrontal cortex (PFC) .
    Cuprizone
  • HY-17416
    Guanfacine hydrochloride
    3 Publications Verification

    		 Adrenergic Receptor Cardiovascular Disease Infection Neurological Disease Metabolic Disease
    Guanfacine hydrochloride is an orally active and blood-brain barrier permeability noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD) .
    Guanfacine hydrochloride
  • HY-W013215
    Adrenic acid
    1 Publications Verification

    cis-7,10,13,16-Docosatetraenoic acid

    		 Endogenous Metabolite Metabolic Disease Inflammation/Immunology
    Adrenic Acid (cis-7,10,13,16-Docosatetraenoic acid) is a naturally polyunsaturated fatty acid in the adrenal gland, brain, kidney, and vasculature. Adrenic Acid can regulate the vascular tone in arteries of the adrenal cortex. Adrenic Acid also is an inflammation enhancer in non-alcoholic fatty liver disease .
    Adrenic acid
  • HY-B2167R
    Docosahexaenoic acid (Standard)

    DHA (Standard); Cervonic acid (Standard)

    		 Reference Standards Endogenous Metabolite Neurological Disease Cancer
    Docosahexaenoic acid (Standard) is the analytical standard of Docosahexaenoic acid. This product is intended for research and analytical applications. Docosahexaenoic Acid (DHA) is an omega-3 fatty acid abundantly present brain and retina. It can be obtained directly from fish oil and maternal milk. In Vitro: Docosahexaenoic acid (DHA) is essential for the growth and functional development of the brain in infants. DHA is also required for maintenance of normal brain function in adults. The inclusion of plentiful DHA in the diet improves learning ability and memory . DHA is an essential requirement in every step of brain development like neural cell proliferation, migration, differentiation, synaptogenesis. The multiple double bonds and unique structure allow DHA to impart special membrane characteristics for effective cell signaling. Many development disorders like dyslexia, autism spectrum disorder, attention deficit hyperactivity disorder, schizophrenia etc. are causally related to decreased level of DHA . DHA is a potent RXR ligand inducing robust RXR activation already at low micro molar concentrations. The EC50 for RXRα activation by DHA is about 5-10 μM fatty acid . In Vivo: Docosahexaenoic acid administration over 10 weeks significantly reduces the number of reference memory errors, without affecting the number of working memory errors, and significantly increases the docosahexaenoic acid content and the docosahexaenoic acid/arachidonic acid ratio in both the hippocampus and the cerebral cortex . DHA treatment exerts neuroprotective actions on an experimental mouse model of PD. There is a decrease tendency in brain lipid oxidation of MPTP mice but it does not significantly .
    Docosahexaenoic acid (Standard)
  • HY-100834
    5,7-Dichlorokynurenic acid
    1 Publications Verification

    5,7-DCKA

    		 iGluR Neurological Disease
    5,7-Dichlorokynurenic acid (5,7-DCKA) is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid reduces NMDA-induced neuron injury. 5,7-Dichlorokynurenic acid increases social interaction time, increases open arm exploration time, disinhibits suppressed conflict responding in rodent models. 5,7-Dichlorokynurenic acid exhibits anxiolytic-like activity in rodent models and supports exploration of glycine’s role in NMDA receptor-mediated synaptic transmission .
    5,7-Dichlorokynurenic acid
  • HY-N0167
    Gynostemma Extract
    1 Publications Verification

    Ginsenoside C-Mx1; Gypenoside IX

    		 p38 MAPK Akt NF-κB COX Interleukin Related NO Synthase Metabolic Disease Inflammation/Immunology
    Gynostemma Extract (Gypenoside IX) is a triterpenoid saponin. Gynostemma Extract can be isolated from Panax notoginseng. Gynostemma Extract reduces NFκB nuclear translocation and transcriptional activity by inhibiting the p38 MAPK/Akt/NFκB signaling pathway. Gynostemma Extract reduces the expression of cytokines (COX-2, IL-6) and the production of NO. Gynostemma Extract has anti-inflammatory activity. Gynostemma Extract can be used in the study of liver injury and neuroinflammation .
    Gynostemma Extract
  • HY-N0506
    Rosarin

    		Interleukin Related Neurological Disease
    Rosarin is a cinnamyl alcohol?glycoside isolated from?Rhodiola rosea. Rosarin has anti-inflammatory and neuroprotective effects. Rosarin supresses the expression of the proinflammatory factors iNOS, IL-1?β, and TNF- α in the kidney and prefrontal cortex of brain in mice? .
    Rosarin
  • HY-B0416
    Gallamine Triethiodide

    		mAChR Adrenergic Receptor Neurological Disease
    Gallamine Triethiodide is a blood-brain barrier-permeable skeletal muscle relaxant. Gallamine Triethiodide induces skeletal muscle paralysis by blocking acetylcholine. Gallamine Triethiodide directly stimulates intracardiac β receptors. Gallamine Triethiodide prolongs the duration of afterdischarge in the cat cerebral cortex. Gallamine Triethiodide can be used in studies related to convulsive disorders .
    Gallamine Triethiodide
  • HY-16728
    Rapastinel
    1 Publications Verification

    GLYX-13

    		 iGluR ERK mTOR Neurological Disease Cancer
    Rapastinel (GLYX-13) is a potent NMDAR modulator capable of crossing the blood-brain barrier, and it exhibits extremely high affinity for human NMDAR (EC50=0.0017-9.9 nM). Rapastinel enhances ERK signaling and activates the mTOR pathway, thereby upregulating the expression of BDNF and VGF, and inducing significant neuroplastic changes such as enhanced LTP and increased mature dendritic spine density in the hippocampus. Rapastinel moderately elevates the efflux of dopamine, norepinephrine and 5-HT in the prefrontal cortex, and uniquely avoids side effects of traditional antidepressants such as dissociation, addiction or sedation. Rapastinel is applicable to the research of major depressive disorder and hepatocellular carcinoma .
    Rapastinel
  • HY-102050
    PF-05085727

    		Phosphodiesterase (PDE) Neurological Disease
    PF-05085727 is a potent, selective and brain penetrant inhibitor of cGMP-dependent PDE2A (IC50=2 nM). PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11 .
    PF-05085727
  • HY-N2411
    Geissoschizine methyl ether
    1 Publications Verification

    		 5-HT Receptor Neurological Disease
    Geissoschizine methyl ether is an orally active, blood-brain barrier permeable alkaloid, and a partial agonist of the 5-HT1A receptor. It can be isolated from Uncaria hook. Geissoschizine methyl ether potently inhibits the binding of [ 3H]8-OH-DPAT to the 5-HT1A receptor in a concentration-dependent manner, with an IC50 of 0.904 μM. It ameliorates isolation-induced increased aggression and reduced sociability in mice. Geissoschizine methyl ether promotes oligodendrocyte differentiation and remyelination in the medial prefrontal cortex of adult mice .
    Geissoschizine methyl ether
  • HY-P6292
    KS-133

    		PACAP Receptor PKA ERK PI3K Akt GSK-3 Neurological Disease Cancer
    KS-133 is a bicyclic peptide with VIPR2 antagonistic activity that can cross the blood-brain barrier. KS-133 selectively blocks VIPR2-mediated Gq/Ca, Gs/cAMP, cAMP/PKA/ERK and PI3K/AKT/GSK3β signaling pathways. KS-133 inhibits VIPR2 agonist-induced CREB phosphorylation in the prefrontal cortex of mice. KS-133 shifts the polarization direction of macrophages toward M1. KS-133 attenuates cancer cell proliferation and reduces the cell cycle distribution level at the S-M phase. KS-133 exerts antitumor effects in a mouse model of colorectal cancer. KS-133 reverses cognitive decline in mouse models of psychiatric disorders. KS-133 can be used for research related to schizophrenia, colorectal cancer and breast cancer .
    KS-133
  • HY-W203728
    L-β-Imidazolelactic acid

    		Amino Acid Derivatives Neurological Disease
    L-β-Imidazolelactic acid is a histidine derivative and an oxidizing agent that can trigger antioxidant effects in the brain cortex of rats .
    L-β-Imidazolelactic acid
  • HY-139427
    3-Methylglutaconic acid

    β-Methylglutaconic acid

    		 GABA Receptor Cardiovascular Disease Neurological Disease Metabolic Disease
    3-Methylglutaconic acid is the major metabolites accumulating in 3-Methylglutaconic aciduria (MGTA). 3-Methylglutaconic acid can induce lipid oxidative damage and protein oxidative. 3-Methylglutaconic acid decreases the non-enzymatic antioxidant defenses in cerebral cortex supernatants to elicit oxidative stress in the cerebral cortex. 3-Methylglutaconic acid can be used for brain damage disease research .
    3-Methylglutaconic acid
  • HY-12959A
    Repinotan hydrochloride

    BAY x 3702

    		 5-HT Receptor Neurological Disease
    Repinotan hydrochloride (BAY x 3702) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus Repinotan hydrochloride has a weak affinity for other related receptors. Repinotan hydrochloride has pronounced neuroprotective effects .
    Repinotan hydrochloride
  • HY-13225B
    Rivanicline hemioxalate
    1 Publications Verification

    RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate

    		 nAChR Neurological Disease
    Rivanicline (RJR-2403) hemioxalate is a neuronal nicotinic receptor agonist. Rivanicline hemioxalate is highly selective for the rat brain cortex nAChRs (Ki = 26 nM, EC50 of 732 nM) and α4β2 subtype (Ki = 26 nM, EC50 = 16 μM). Rivanicline hemioxalate can significantly restore the learning impairment and cognitive dysfunction. Rivanicline hemioxalate can be used for the study of neurodegenerative diseases (such as schizophrenia or Alzheimer's disease) .
    Rivanicline hemioxalate
  • HY-16728B
    Rapastinel Trifluoroacetate
    1 Publications Verification

    GLYX-13 Trifluoroacetate

    		 iGluR mTOR ERK Neurological Disease
    Rapastinel (GLYX-13) Trifluoroacetate is a potent NMDAR modulator capable of crossing the blood-brain barrier, and it exhibits extremely high affinity for human NMDAR (EC50=0.0017-9.9 nM). Rapastinel Trifluoroacetate enhances ERK signaling and activates the mTOR pathway, thereby upregulating the expression of BDNF and VGF, and inducing significant neuroplastic changes such as enhanced LTP and increased mature dendritic spine density in the hippocampus. Rapastinel Trifluoroacetate moderately elevates the efflux of dopamine, norepinephrine and 5-HT in the prefrontal cortex, and uniquely avoids side effects of traditional antidepressants such as dissociation, addiction or sedation. Rapastinel Trifluoroacetate is applicable to the research of major depressive disorder and hepatocellular carcinoma .
    Rapastinel Trifluoroacetate
  • HY-106584
    Mosapramine

    Clospipramine

    		 Drug Derivative Dopamine Receptor 5-HT Receptor Neurological Disease
    Mosapramine (Clospipramine) is an orally active antipsychotic agent and one of the metabolites of Clocapramine (HY-B2073) after oral absorption. Mosapramine exerts its effects by specifically binding to striatal dopamine D2 receptors and frontal lobe 5-HT2 receptors, with a D2/5-HT2 receptor occupancy ratio of 7.4. Mosapramine induces typical neuropharmacological responses in rat brain regions, including extrapyramidal symptoms, hyperprolactinemia, increased salivation, constipation, and upregulated Fos protein expression. Mosapramine also features a reduced incidence of weight loss. Mosapramine is applicable to research related to schizophrenia .
    Mosapramine
  • HY-W795507
    Cyanopindolol

    		Adrenergic Receptor 5-HT Receptor Neurological Disease
    Cyanopindolol is an β3-adrenoceptor antagonist. Cyanopindolol is a potent and selective antagonist at the presynaptic serotonin autoreceptor in the rat brain cortex. Cyanopindolol has binding affinity for 5-HT1A and 5-HT1B receptor (Ki: 2.1 and 3 nM respectively) .
    Cyanopindolol
  • HY-P3801
    [Glp5,(Me)Phe8,Sar9] Substance P (5-11)

    DiMe-C7

    		 Neurokinin Receptor Neurological Disease Metabolic Disease
    [Glp5,(Me)Phe8,Sar9] Substance P (5-11) (DiMe-C7) is a Substance P (HY-P0201) analogue that has approximately the same effects as Substance P (HY-P0201) on neurokinin 1 receptor (NK1R) in rat brain, but with a much longer duration of action. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) selectively activates dopamine metabolism in the mesencephalon and midbrain cortex of the rat brain. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) also increases motor activity and induces recovery of addictive agent-seeking behavior in rats .
    [Glp5,(Me)Phe8,Sar9] Substance P (5-11)
  • HY-120717
    VU6001966

    		mGluR Cytochrome P450 Neurological Disease
    VU6001966 is a brain-penetrant and selective mGlu2 receptor inhibitor. VU6001966 blocks mGlu2 receptor activity, counteracts LY379268 (HY-103558)-mediated blood-brain barrier protection and inflammatory cytokine dampening in microglia under inflammatory conditions. VU6001966 enhances antidepressant effects when combined with Scopolamine (HY-N0296). VU6001966 can be used for the research of major depressive disorder .
    VU6001966
  • HY-P3883
    [DAla4] Substance P (4-11)

    		Neurokinin Receptor Neurological Disease
    [DAla4] Substance P (4-11) is an analog of Substance P (HY-P0201) that inhibits the binding of 125I-Bolton Hunter-conjugated Eledoisin (HY-P0006) (IC50 of 0.5 μM) and 125I-Bolton Hunter-conjugated Substance P (IC50 of 0.15 μM) to rat brain cortex membranes .
    [DAla4] Substance P (4-11)
  • HY-123858
    VU6001221

    		nAChR Neurological Disease
    VU6001221 is a blood-brain barrier permeable Choline Transporter (CHT) inhibitor (IC50 = 270 nM). VU6001221 increases the likelihood of extracellular choline elevation activating synaptic α7 nicotine ACh receptors. VU6001221 attenuates potassium-induced ACh levels in the prefrontal cortex .
    VU6001221
  • HY-13225A
    Rivanicline

    RJR-2403; (E)-Metanicotine

    		 nAChR Neurological Disease
    Rivanicline (RJR-2403) is a neuronal nicotinic receptor agonist. Rivanicline is highly selective for the rat brain cortex nAChRs (Ki = 26 nM, EC50 of 732 nM) and α4β2 subtype (Ki = 26 nM, EC50 = 16 μM). Rivanicline can significantly restore the learning impairment and cognitive dysfunction. Rivanicline can be used for the study of neurodegenerative diseases (such as schizophrenia or Alzheimer's disease) .
    Rivanicline
  • HY-102043
    PDM-631

    		Phosphodiesterase (PDE) Neurological Disease
    PDM-631 is a selective and orally active PDE2A inhibitor with blood-brain barrier penetration. PDM-631 exhibits potent inhibitory activity against human and rat recombinant PDE2A with IC50 values of 1.5 nM and 4.2 nM, respectively. PDM-631 increases cGMP levels in the rat cerebral cortex. PDM-631 can be used for the study of schizophrenia and neurodegenerative disorders .
    PDM-631
  • HY-W115718R
    Cuprizone (Standard)

    		Reference Standards Dopamine β-hydroxylase Neurological Disease
    Cuprizone is a copper chelating agent that forms a deep blue copper ketone complex with copper (II). The copper ketone reaction can be used in colorimetric tests for the presence of trace copper. Cuprizone can be used to induce some schizophrenia-like behavior in mice. Cuprizone acts on copper enzymes, including SOD1, cytochrome oxidase, and DβH, thereby causing oxidative stress and increasing DA levels in certain brain regions such as the medial prefrontal cortex (PFC) .
    Cuprizone (Standard)
  • HY-170409
    BNN27

    		Trk Receptor Apoptosis Neurological Disease Inflammation/Immunology
    BNN27 is the agonist for TrkA receptor and p75NTR receptor, that exhibits neurotrophic and anti-apoptotic effects. BNN27 increases the levels of glutamate, GABA, and glutamine in the rat hippocampus and prefrontal cortex, improves glutamate turnover. BNN27 exhibits neuroprotective efficacy in mouse amyotrophic lateral sclerosis (ALS) model, exhibits anti-inflammatory efficacy in experimental autoimmune encephalomyelitis (EAE) model, exhibits retinal protective efficacy in rat diabete models. BNN27 is blood-brain barrier penetrable .
    BNN27
  • HY-N0506R
    Rosarin (Standard)

    		Reference Standards Interleukin Related Neurological Disease
    Rosarin (Standard) is the analytical standard of Rosarin. This product is intended for research and analytical applications. Rosarin is a cinnamyl alcohol glycoside isolated from Rhodiola rosea. Rosarin has anti-inflammatory and neuroprotective effects. Rosarin supresses the expression of the proinflammatory factors iNOS, IL-1 β, and TNF- α in the kidney and prefrontal cortex of brain in mice .
    Rosarin (Standard)
  • HY-12959
    Repinotan

    BAY x 3702 free base

    		 5-HT Receptor Neurological Disease
    Repinotan (BAY x 3702 free base) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus). Repinotan has a weak affinity for other related receptors. Repinotan has pronounced neuroprotective effects .
    Repinotan
  • HY-59201A
    A-582941 dihydrochloride

    		ERK 5-HT Receptor Epigenetic Reader Domain nAChR Neurological Disease Metabolic Disease
    A-582941 dihydrochloride is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with Ki values of 10.8 nM and 17 nM in rat brain and human frontal cortex, respectively. A-582941 dihydrochloride exhibits agonistic activity at 5-HT3 receptors, with a Ki of 150 nM. A-582941 dihydrochloride triggers phosphorylation of ERK1/2 and CREB, inhibits GSK-3β via Ser-9 phosphorylation, increases acetylcholine release, induces the expression of Arc and c-Fos, activates brain regions associated with working memory and attention, and reduces cell death caused by nerve growth factor (NGF) deprivation. A-582941 dihydrochloride is applicable for the research of Alzheimer's disease and schizophrenia .
    A-582941 dihydrochloride
  • HY-13225
    Rivanicline oxalate

    RJR-2403 oxalate; (E)-Metanicotine oxalate

    		 nAChR Neurological Disease
    Rivanicline (RJR-2403) oxalate is a neuronal nicotinic receptor agonist. Rivanicline oxalate is highly selective for the rat brain cortex nAChRs (Ki = 26 nM, EC50 of 732 nM) and α4β2 subtype (Ki = 26 nM, EC50 = 16 μM). Rivanicline oxalate can significantly restore the learning impairment and cognitive dysfunction. Rivanicline oxalate can be used for the study of neurodegenerative diseases (such as schizophrenia or Alzheimer's disease) .
    Rivanicline oxalate
  • HY-116738
    Trimecaine

    		Sodium Channel Neurological Disease
    Trimecaine, a local neural blockade agent, has a strong depressant effect on the cerebral cortex and the ascending reticular formation of the brain stem .
    Trimecaine
  • HY-107562
    JNJ 10181457 dihydrochloride

    		Histamine Receptor Neurological Disease
    JNJ-10181457 is a neutral, potent, brain-penetrant and selective non-imidazole H3 antagonist which increases NE and ACh concentrations in rat frontal cortex. JNJ-10181457 can be used for neurological research .
    JNJ 10181457 dihydrochloride
  • HY-100481
    RP 72540

    RPR101048

    		 Cholecystokinin Receptor Neurological Disease
    RP 72540 is a selective CCK-B receptor antagonist, with IC50 values of 2.4, 1.2, and 3.8 nM for CCK-B receptors in the guinea pig cerebral cortex, rat cerebral cortex, and mouse brain, respectively. RP 72540 effectively inhibits CCK-8-induced neuronal firing and dose-dependently inhibits gastric acid secretion, making it potentially valuable in studies of acid secretion. RP 72540 is an important tool for investigating the physiological functions of CCK B receptors .
    RP 72540
  • HY-18138
    PF-03382792

    		5-HT Receptor Neurological Disease
    PF-03382792 is a potent 5-HT4 partial agonist with a Ki of 2.7 nM and an EC50 of 0.9 nM for 5-HT4d. PF-03382792 can penetrate the brain. PF-03382792 produces moderate increases in cortical Ach in the rat prefrontal cortex .
    PF-03382792
  • HY-11051
    JNJ-20788560

    		Opioid Receptor Inflammation/Immunology
    JNJ-20788560 is a selective and orally active delta opioid receptor agonist with an affinity of 2.0 nM for DOR (rat brain cortex binding assay). JNJ-20788560 also is a potent and efficacious antihyperalgesic agent that does not produce respiratory depression, pharmacologic tolerance, or physical dependence. JNJ-20788560 can be used for the research of the relief of inflammatory hyperalgesia .
    JNJ-20788560
  • HY-116062
    JNJ-7925476 hydrochloride

    		Monoamine Transporter Dopamine Transporter Adrenergic Receptor Others
    JNJ-7925476 (hydrochloride) is a triple monoamine uptake inhibitor with the ability to regulate neurotransmitter levels and antidepressant activity. JNJ-7925476 (hydrochloride) can be rapidly absorbed into the plasma in rats, with a higher concentration in the brain than in plasma. It can induce an increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex, and exhibits antidepressant activity in the mouse tail suspension test.
    JNJ-7925476 hydrochloride
  • HY-111066
    JNJ-37822681

    		Dopamine Receptor Others
    JNJ-37822681 is a fast dissociating D2 antagonist with activity in inhibiting schizophrenia. JNJ-37822681 has high specificity for D2 receptors and is effective in animal models, inducing increased levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex, and exhibiting antidepressant activity in the mouse tail suspension test, while having a good brain distribution and lower prolactin release.
    JNJ-37822681
  • HY-13225H
    Rivanicline hydrochloride

    RJR-2403 hydrochloride; Metanicotine hydrochloride

    		 nAChR Neurological Disease
    Rivanicline (RJR-2403) hydrochloride is a neuronal nicotinic receptor agonist. Rivanicline hydrochloride is highly selective for the rat brain cortex nAChRs (Ki = 26 nM, EC50 of 732 nM) and α4β2 subtype (Ki = 26 nM, EC50 = 16 μM). Rivanicline hydrochloride can significantly restore the learning impairment and cognitive dysfunction. Rivanicline hydrochloride can be used for the study of neurodegenerative diseases (such as schizophrenia or Alzheimer's disease) .
    Rivanicline hydrochloride
  • HY-106874B
    rel-Delequamine

    rel-RS-15385-197

    		 Adrenergic Receptor Neurological Disease
    rel-Delequamine (rel-RS-15385-197) is an orally active, brain-penetrant, potent and selective M2-adrenoceptor antagonist and α2-adrenoceptor antagonist. rel-Delequamine has a pKi of 9.45 for α2-adrenoceptors in the rat cortex. rel-Delequamine augments K +-evoked release of noradrenaline with an EC50 of 1 nM .
    rel-Delequamine
  • HY-U00033
    Iomazenil

    		Endogenous Metabolite Neurological Disease
    Iomazenil is a benzodiazepine receptor antagonist with partial inverse agonist activity. Iomazenil can assess the binding potential of central benzodiazepine receptors in the cerebral cortex and may reflect neuronal function in viable tissue. Iomazenil use is associated with improved cognitive function in adult patients with ischemic cerebral pathology after indirect revascularization surgery. Iomazenil demonstrated restoration of benzodiazepine receptor binding potential in the affected hemisphere after surgery on brain SPECT imaging .
    Iomazenil
  • HY-B0416R
    Gallamine Triethiodide (Standard)

    		Reference Standards mAChR Cardiovascular Disease
    Gallamine Triethiodide (Standard) is the analytical standard of Gallamine Triethiodide. This product is intended for research and analytical applications. Gallamine Gallamine Triethiodide is a blood-brain barrier-permeable skeletal muscle relaxant. Gallamine Triethiodide induces skeletal muscle paralysis by blocking acetylcholine. Gallamine Triethiodide directly stimulates intracardiac β receptors. Gallamine Triethiodide prolongs the duration of afterdischarge in the cat cerebral cortex. Gallamine Triethiodide can be used in studies related to convulsive disorders .
    Gallamine Triethiodide (Standard)
  • HY-178153
    BPAM363

    		iGluR Neurological Disease
    BPAM363 is an orally active, selective positive allosteric modulator (PAM) of AMPARs with blood-brain barrier penetration. BPAM363 selectively potentiates AMPAR activity in human and rat models, with an EC2x value of 0.96 μM in rat embryonic cortex primary neurons. BPAM363 upregulates BDNF protein expression in rat primary cortical neuronal cultures. BPAM363 enhances AMPA-mediated excitatory postsynaptic responses in rat and mice. BPAM363 can be used for the study of cognitive disorders .
    BPAM363
  • HY-116062A
    JNJ-7925476

    		Histone Methyltransferase Neurological Disease
    JNJ-7925476 is a triple reuptake inhibitor that selectively and potently inhibits the activity of the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT). JNJ-7925476 is rapidly absorbed into the blood and its concentration in the brain is 7-fold higher than that in plasma. The occupancy ED(50) values of JNJ-7925476 for SERT, NET, and DAT in the rat brain are 0.18, 0.09, and 2.4 mg/kg, respectively. JNJ-7925476 rapidly induces a significant increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex in a dose-dependent manner. JNJ-7925476 exhibits potent antidepressant-like activity in the mouse tail suspension test. These results suggest that JNJ-7925476 has in vivo efficacy in biochemical and behavioral models of depression .
    JNJ-7925476
  • HY-16728A
    Rapastinel acetate

    GLYX-13 acetate

    		 iGluR mTOR ERK Neurological Disease
    Rapastinel (GLYX-13) acetate is a potent NMDAR modulator capable of crossing the blood-brain barrier, and it exhibits extremely high affinity for human NMDAR (EC50=0.0017-9.9 nM). Rapastinel acetate enhances ERK signaling and activates the mTOR pathway, thereby upregulating the expression of BDNF and VGF, and inducing significant neuroplastic changes such as enhanced LTP and increased mature dendritic spine density in the hippocampus. Rapastinel acetate moderately elevates the efflux of dopamine, norepinephrine and 5-HT in the prefrontal cortex, and uniquely avoids side effects of traditional antidepressants such as dissociation, addiction or sedation. Rapastinel acetate is applicable to the research of major depressive disorder and hepatocellular carcinoma .
    Rapastinel acetate
  • HY-12193
    A-349821

    		Histamine Receptor Others
    A-349821 is a histamine H3 receptor antagonist characterized as a radioligand ([3H]-A-349821) for in vivo receptor occupancy assessment. In rats, [3H]-A-349821 penetrated the brain, showing higher levels in the cortex compared to the cerebellum, indicating selective H3 receptor binding. Its cortical occupancy was saturable, correlating with in vitro binding data. Inhibition studies with ABT-239 and other H3 antagonists showed dose-dependent reductions in receptor occupancy, matching blood levels associated with cognitive efficacy in preclinical models. [3H]-A-349821 thus serves as a valid tracer for H3 receptor occupancy, aiding in the development and clinical interpretation of H3 receptor antagonists .
    A-349821
  • HY-100834A
    5,7-Dichlorokynurenic acid sodium

    5,7-DCKA sodium

    		 iGluR Neurological Disease
    5,7-Dichlorokynurenic acid (5,7-DCKA) sodium is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid sodium reduces NMDA-induced neuron injury. 5,7-Dichlorokynurenic acid sodium increases social interaction time, increases open arm exploration time, disinhibits suppressed conflict responding in rodent models. 5,7-Dichlorokynurenic acid sodium exhibits anxiolytic-like activity in rodent models and supports exploration of glycine’s role in NMDA receptor-mediated synaptic transmission .
    5,7-Dichlorokynurenic acid sodium
  • HY-183166
    Z-Arg-Lys-AOMK

    		Cathepsin Neurological Disease
    Z-Arg-Lys-AOMK is a cathepsin B inhibitor that can cross the blood-brain barrier. Z-Arg-Lys-AOMK reduces cytosolic cathepsin B activity in homogenates of mouse cerebral cortex and hippocampal tissues, and alleviates motor dysfunction associated with CCI-TBI. Z-Arg-Lys-AOMK can be used in the research of traumatic brain injury .
    Z-Arg-Lys-AOMK
  • HY-102050R
    PF-05085727 (Standard)

    		Reference Standards Phosphodiesterase (PDE) Neurological Disease
    PF-05085727 (Standard) is the analytical standard of PF-05085727 (HY-102050). This product is intended for research and analytical applications. PF-05085727 is a potent, selective and brain penetrant inhibitor of cGMP-dependent PDE2A (IC50=2 nM). PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11 .
    PF-05085727 (Standard)

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