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rat cortex

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55

Inhibitors & Agonists

1

Biochemical Assay Reagents

4

Peptides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-101333

    (RS)-CPPG

    mGluR Neurological Disease
    CPPG ((RS)-CPPG) is a potent group II/III mGlu receptors antagonist. CPPG exhibits some selectivity (approximately 20 fold) for group III (IC50=2.2 nM) over group II (IC50=46.2 nM) mGlu receptors in the rat cerebral cortex. CPPG has weak effects at group I mGlu receptors .
    CPPG
  • HY-103509

    GABA Receptor Neurological Disease
    NNC 05-2090 hydrochloride is a GABA uptake inhibitor and inhibitor of the β-GABA transporter (BGT-1) (IC50< /sub>: 10.6 μM). NNC 05-2090 hydrochloride also inhibits mGAT2 with a Ki value of 1.4 μM. NNC 05-2090 has anticonvulsant activity and can be used in the study of epilepsy and neurological diseases .
    NNC 05-2090 hydrochloride
  • HY-P1212

    CST-14 (mouse, rat)

    Somatostatin Receptor Neurological Disease
    Cortistatin 14, mouse, rat (CST-14, human, rat), a neuropeptide with neuronal depressant and sleep modulating properties, can bind to all five cloned somatostatin receptors (SSTRs) and ghrelin receptor to exert its biological activities and co-exists with GABA within the cortex and hippocampus .
    Cortistatin 14 (mouse, rat)
  • HY-107563

    Histamine Receptor Inflammation/Immunology
    ROS 234 is a potent H3 antagonist, with a pKB of 9.46 for Guinea-pig ileum H3-receptor, a pKi of 8.90 for Rat cerebral cortex H3-receptor, and a ED50 of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 diaplays poor central access .
    ROS 234
  • HY-107563A

    Histamine Receptor Inflammation/Immunology
    ROS 234 dioxalate is a potent H3 antagonist, with a pKB of 9.46 for Guinea-pig ileum H3-receptor, a pKi of 8.90 for Rat cerebral cortex H3-receptor, and a ED50 of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 dioxalate diaplays poor central access .
    ROS 234 dioxalate
  • HY-106874B

    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-W203728

    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-P1588

    Neurokinin Receptor Neurological Disease Endocrinology
    Scyliorhinin II is a selective neurokinin-3 receptor agonist, with a Ki of 2.5 nM for neurokinin-3 receptor in rat cerebral cortex.
    Scyliorhinin II
  • HY-107562

    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-119409

    Phacetoperane free base

    Dopamine Transporter Neurological Disease
    Levophacetoperane (Phacetoperane free base) competitively inhibits the uptake of norepinephrin and dopamine .
    Levophacetoperane
  • HY-121186

    Adrenergic Receptor Calcium Channel Cardiovascular Disease Neurological Disease Metabolic Disease
    Bevantolol hydrochloride is a selective β1 and α1-adrenergic receptor antagonist with pKi values of 7.83, 6.9 in rat cerebral cortex, respectively. Bevantolol hydrochloride is a potent Ca 2+ antagonist .
    Bevantolol hydrochloride
  • HY-100481

    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-12959A

    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-12959

    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-160932

    Adrenergic Receptor Endocrinology
    RS-15385-198 is the enantiomer of Delequamine (RS-15385-197) (HY-106874). RS-15385-198 exhibits a pKi of 6.32 for α2-adrenoceptors in the rat cortex. RS-15385-198 is an antagonist for UK-14304 (HY-B0659) in the rat vas deferens and in the guinea-pig ileum .
    RS-15385-198
  • HY-126862

    mAChR Others
    AQ-RA 721 is a muscarinic receptor antagonist with differential affinity for the m4 and M2 sites, which can be used to characterize muscarinic receptor subtypes. Other muscarinic receptor antagonists have differential affinity for the M1 (rat cerebral cortex), M2 (rat heart), M3 (rat submandibular gland), m4 (receptor expressed in Chinese hamster ovary cells transfected with CHO), and guinea pig uterine smooth muscle at the muscarinic binding site .
    AQ-RA 721
  • HY-18138

    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-121186R

    Reference Standards Adrenergic Receptor Calcium Channel Neurological Disease Metabolic Disease
    Bevantolol (hydrochloride) (Standard) is the analytical standard of Bevantolol (hydrochloride). This product is intended for research and analytical applications. Bevantolol hydrochloride is a selective β1 and α1-adrenergic receptor antagonist with pKi values of 7.83, 6.9 in rat cerebral cortex, respectively. Bevantolol hydrochloride is a potent Ca 2+ antagonist .
    Bevantolol hydrochloride (Standard)
  • HY-10711A

    (R)-NFPS hydrochloride

    GlyT Neurological Disease
    ALX-5407 ((R)-NFPS) hydrochloride is a selective and orally active glycine transporter GlyT1 inhibitor with an IC50 value of 3 nM. ALX-5407 hydrochloride can be used the research of N-methyl-D-aspartate-receptor function and schizophrenia .
    ALX-5407 hydrochloride
  • HY-168859

    JNK GSK-3 Amyloid-β Neurological Disease
    JNK3 inhibitor-9 (Compound 24a) is a potent, selective and BBB-permeable JNK3 inhibitor with an IC50 value of 12 nM. JNK3 inhibitor-9 also potently inhibits GSK3α/β (IC50s: 14 and 35 nM, respectively) involved in Tau phosphorylation. JNK3 inhibitor-9 reduces c-Jun and APP phosphorylation. JNK3 inhibitor-9 protects neurons from 1-42 toxicity .
    JNK3 inhibitor-9
  • HY-101075

    Phosphatase Others
    L-690330 is a competitive inhibitor of inositol monophosphatase (IMPase) with Kis of 0.27 and 0.19 μM for recombinant human and bovine IMPase, 0.30 and 0.42 μM for human and bovine frontal cortex IMPase, respectively. L-690330 exhibits 10-fold more sensitive than mouse and rat IMPase .
    L-690330
  • HY-103133

    5-HT Receptor Neurological Disease
    WAY 208466 dihydrochloride is a potent and selective 5-HT6 receptor agonist (EC50=7.3 nM for the human 5-HT6 receptor). WAY-208466 dihydrochloride elevates cortical GABA levels in rat frontal cortex . WAY 208466 dihydrochloride exhibits antidepressant and anxiolytic-like effects .
    WAY208466 dihydrochloride
  • HY-101075A

    Phosphatase Others
    L-690330 hydrate is a competitive inhibitor of inositol monophosphatase (IMPase) with Kis of 0.27 and 0.19 μM for recombinant human and bovine IMPase, 0.30 and 0.42 μM for human and bovine frontal cortex IMPase, respectively. L-690330 hydrate exhibits 10-fold more sensitive than mouse and rat IMPase .
    L-690330 hydrate
  • HY-117839

    Cholecystokinin Receptor Neurological Disease
    PD-135666 is a dipeptide inhibitor of cholecystokinin B (CCK B) receptors, binding to CCK B receptors in mouse cerebral cortex with IC50 of 0.1 nM. Its enantiomer, PD-140548, preferentially binds to CCK A receptors with IC50 of 2.8 nM in rat pancreas. PD-135666 exhibits anxiolytic effects in animal models .
    PD-135666
  • HY-114753

    CR-2249; XY-2401

    iGluR Neurological Disease
    Neboglamine (CR-2249; XY-2401) is a modulator for N-methyl-D-aspartate (NMDA) receptor. Neboglamine increases the levels of fos-like immunoreactivity (FLI)-positive cells in the prefrontal cortex, nucleus accumbens, and lateral septal nucleus in rat models, .restores NMDA (HY-17551) -mediated neurotransmitter release, and inhibits phencyclidine-induced hyperlocomotion .
    Neboglamine
  • HY-11051

    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

    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-18730

    W1400

    NO Synthase Apoptosis Cardiovascular Disease Inflammation/Immunology Cancer
    1400W is a slow, tight binding, and highly selective inducible nitric-oxide synthase (iNOS) inhibitor, with a Kd value ≤ 7 nM. 1400W inhibits iNOS induction in microglial cells, and reduces generation of NO, thereby mitigating oxidative stress and neuronal cell apoptosis in the rat cerebral cortex, and improving the spatial memory dysfunction caused by acute hypobaric hypoxia-reoxygenation .
    1400W
  • HY-W795507

    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-105115

    ZK 112119

    GABA Receptor Neurological Disease
    Abecarnil (ZK 112119) is a ligand or a partial agonist for benzodiazepine (BZ) receptor. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil can act as a positive allosteric modulator of GABAA receptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with an IC50 of 0.82 nM. Abecarnil can be used for epilepsy research .
    Abecarnil
  • HY-170409

    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-111066

    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-P3883

    Neurokinin Receptor Neurological Disease
    [DAla4] Substance P (4-11) is an analog of Substance P (Substance P (HY-P0201)) that inhibits the binding of 125I-Bolton Hunter-conjugated Eledoisin (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-13225A

    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-13225H

    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-13225D

    RJR-2403 fumarate; (E)-Metanicotine fumarate

    nAChR Neurological Disease
    Rivanicline (RJR-2403) fumarate is a neuronal nicotinic receptor agonist. Rivanicline fumarate 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 fumarate can significantly restore the learning impairment and cognitive dysfunction. Rivanicline fumarate can be used for the study of neurodegenerative diseases (such as schizophrenia or Alzheimer's disease) .
    Rivanicline fumarate
  • HY-17550

    DM-235

    iGluR Neurological Disease
    Sunifiram (DM-235) is an ampakine-like compound and an agonist of AMPA receptor with oral activity. Sunifiram can increase the release of acetylcholine in the rat cerebral cortex and exhibits potent cognitive enhancement effects with better nootropic activity compared to piracetam (HY-B0585). Sunifiram is promising for research in neurodegenerative diseases such as mild cognitive impairment (MCI) and Alzheimer's disease (AD) .
    Sunifiram
  • HY-W028142

    5-HT Receptor SARS-CoV Neurological Disease
    Quipazine is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine behaves as a 5-HT3R agonist in peripheral models. Quipazine can be used for neurological disease research .
    Quipazine
  • HY-101046

    Quipazine dimaleate

    5-HT Receptor SARS-CoV Neurological Disease
    Quipazine dimaleate is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine dimaleate shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine dimaleate behaves as a 5-HT3R antagonist in peripheral models. Quipazine dimaleate can be used for neurological disease research .
    Azaperone dimaleate
  • HY-18731
    1400W Dihydrochloride
    Maximum Cited Publications
    20 Publications Verification

    NO Synthase Apoptosis Cardiovascular Disease Inflammation/Immunology Cancer
    1400W dihydrochloride is the dihydrochloride form of 1400W (HY-18730). 1400W is a slow, tight binding, and highly selective inducible nitric-oxide synthase (iNOS) inhibitor, with a Kd value ≤ 7 nM. 1400W inhibits iNOS induction in microglial cells, and reduces generation of NO, thereby mitigating oxidative stress and neuronal cell apoptosis in the rat cerebral cortex, and improving the spatial memory dysfunction caused by acute hypobaric hypoxia-reoxygenation .
    1400W Dihydrochloride
  • HY-19651B

    TAK-147 fumarate

    Cholinesterase (ChE) Neurological Disease
    Zanapezil (TAK-147) fumarate is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil fumarate shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil fumarate shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil fumarate can be used for the research of early stages of Alzheimer's disease (AD) .
    Zanapezil fumarate
  • HY-19651A

    TAK-147

    Cholinesterase (ChE) Neurological Disease
    Zanapezil (TAK-147) is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil can be used for the research of early stages of Alzheimer's disease (AD) .
    Zanapezil
  • HY-59201A

    nAChR 5-HT Receptor Neurological Disease
    A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist of α7 nAChR, with Kis of 10.8 and 16.7 nM in rat brain membranes and human frontal cortex, respectively. A-582941 dihydrochloride also binds to human 5-HT3 receptor with a Ki of 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research .
    A-582941 dihydrochloride
  • HY-13225

    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-129245

    Hoe 175

    Endogenous Metabolite Neurological Disease
    Razobazam (Hoe 175) is a benzodiazepine derivative with cognitive activity. Razobazam has been shown to improve learning performance in socially deprived rats. Razobazam increased avoidance scores by 18% after training. Razobazam caused significant changes in the optical density of certain areas of the rat brain, including a 22% decrease in the lateral habenula and a 25% increase in the ventral tegmental area. Razobazam also caused a 13% increase in optical density in the prefrontal cortex of rats .
    Razobazam
  • 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-106874A

    RS-15385-197 hydrochloride

    Adrenergic Receptor Neurological Disease
    Delequamine (RS-15385-197) hydrochloride is an orally active and selective α2-adrenergic receptor antagonist with a pKi of 9.5 for α2-adrenoceptors in rat cortex. Delequamine hydrochloride shows >1000 fold selectivity against 5-HT1A receptors and α1-adrenoceptors. Delequamine hydrochloride can be used for the study of erectile dysfunction .
    Delequamine hydrochloride
  • HY-106874

    RS-15385-197

    Adrenergic Receptor Neurological Disease
    Delequamine (RS-15385-197) is an orally active and selective α2-adrenergic receptor antagonist with a pKi of 9.5 for α2-adrenoceptors in rat cortex. Delequamine shows >1000 fold selectivity against 5-HT1A receptors and α1-adrenoceptors. Delequamine can be used for the study of erectile dysfunction .
    Delequamine
  • HY-19651

    TAK-147 free base

    Cholinesterase (ChE) Neurological Disease
    Zanapezil (TAK-147) free base is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil free base shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil free base shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil free base can be used for the research of early stages of Alzheimer's disease (AD) .
    Zanapezil free base
  • HY-17550R

    DM-235 (Standard)

    Reference Standards iGluR Neurological Disease
    Sunifiram (Standard) is the analytical standard of Sunifiram. This product is intended for research and analytical applications. Sunifiram (DM-235) is an ampakine-like compound and an agonist of AMPA receptor with oral activity. Sunifiram can increase the release of acetylcholine in the rat cerebral cortex and exhibits potent cognitive enhancement effects with better nootropic activity compared to piracetam (HY-B0585). Sunifiram is promising for research in neurodegenerative diseases such as mild cognitive impairment (MCI) and Alzheimer's disease (AD) .
    Sunifiram (Standard)

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