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Results for "

MK-801

" in MedChemExpress (MCE) Product Catalog:

17

Inhibitors & Agonists

1

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15084B
    Dizocilpine
    35+ Cited Publications

    MK-801

    		 iGluR Neurological Disease
    Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca 2+ flux .
    Dizocilpine
  • HY-15084A
    (-)-Dizocilpine maleate

    (-)-MK-801 maleate

    		 iGluR Neurological Disease
    (-)-Dizocilpine maleate ((-)-MK-801 maleate) is a less active (-)-enantiomer of Dizocilpine. (-)-Dizocilpine maleate is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with a Ki of 211.7 nM. (-)-Dizocilpine maleate has antidepressant effects .
    (-)-Dizocilpine maleate
  • HY-15084
    Dizocilpine maleate
    35+ Cited Publications

    (+)-MK 801 Maleate

    		 iGluR Neurological Disease
    Dizocilpine maleate (MK-801 maleate) is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.
    Dizocilpine maleate
  • HY-164264
    Caged MK801

    		iGluR Neurological Disease
    Caged MK801 (cMK801) is a selective, non-competitive, irreversible NMDA receptor open-channel blocker. NVOC cages are neuro pharmocologically compatible .
    Caged MK801
  • HY-107694
    (Rac)-Dizocilpine

    (Rac)-MK-801

    		 iGluR Others
    (Rac)-Dizocilpine ((Rac)-MK-801) is the racemate of Dizocilpine (HY-15084B). Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist .
    (Rac)-Dizocilpine
  • HY-107695
    Remacemide hydrochloride

    FPL 12924AA

    		 iGluR Sodium Channel Neurological Disease
    Remacemide hydrochloride (FPL 12924AA), a moderate inhibitor of the Na + channel, is a weak uncompetitive NMDA receptor antagonist with IC50s of 68 μM and 76 μM for MK-801 binding and NMDA currents, respectively . Remacemide hydrochloride is an anticonvulsant agent .
    Remacemide hydrochloride
  • HY-N5159
    Ampullosporin A

    		iGluR Neurological Disease
    Ampullosporin A is a peptaibol-type polypeptide that can be isolated from the fungus Sepedonium ampullosporum HKI-0053, exhibiting neuroleptic-like activity. Ampullosporin A can inhibit hyperactivity induced by NMDA receptor antagonist MK-801 (HY-15084B) and ameliorate social behavior abnormalities caused by subchronic drug treatment. Ampullosporin A alters the activity of glutamate receptors without affecting dopamine D1 and D2 receptors .
    Ampullosporin A
  • HY-170499
    VU6024578

    BI02982816

    		 mGluR Neurological Disease
    VU6024578 (BI02982816) is a selective, orally active positive allosteric modulator (PAM) for metabotropic glutamate receptor (mGluR1), that activates human mGluR1 and rat mGluR1 with EC50 of 54 nM and 46 nM. VU6024578 exhibits antipsychotic activity in rats amphetamine-induced hyperactivity models and MK-801 (HY-15084B)-induced novel object recognition (NOR) models. VU6024578 is blood brain barrier penetrable .
    VU6024578
  • HY-19021
    ADD-17014

    		mGluR Neurological Disease
    ADD-17014 is a L-Glu antagonist. ADD-17014 impairs presynaptic excitatory amino acid L-Glu neurotransmission. ADD-17014 is a prodrug of its β-amino alcohol metabolite, and the metabolite acts as a NMDA receptor antagonist by binding to the MK-801 site located inside the NMDA receptor or ion channel. ADD-17014 has an anticonvulsant and anti-ischemic activity. ADD-17014 can be used for neurodegenerative diseases like Parkinson’s disease, Alzheimer’s disease and stroke research .
    ADD-17014
  • HY-173032
    VU6033685

    		mGluR Neurological Disease
    VU6033685 is the orally active positive allosteric modulator (PAM) for mGlu1 that positively modulates human mGlu1 and human mGlu5 with EC50 of 39 nM and 3960 nM. VU6033685 also inhibits CYP1A2, CYP2C9 and CYP2D6 with IC50 of 26, 22.3 and 23.8 μM, respectively. VU6033685 reverses amphetamine-induced rats hyperlocomotion, protects rats from MK-801 (HY-15084B)-induced cognitive impairment. VU6033685 exhibits good pharmacokinetics characteristics in rats with an oral bioavailability of 42.8% .
    VU6033685
  • HY-156017
    5-HT6R antagonist 1

    		5-HT Receptor Cardiovascular Disease Neurological Disease
    5-HT6R antagonist 1 (Comopund 8) is a 5-HT6R antagonist (Ki: 5 nM). 5-HT6R antagonist 1 inhibits platelet aggregation. 5-HT6R antagonist 1 has excellent metabolic stability. 5-HT6R antagonist 1 reverses MK-801 (HY-15084B)-induced memory impairments in rats. 5-HT6R antagonist 1 can be used for Alzheimer's disease (AD) research .
    5-HT6R antagonist 1
  • HY-169001
    5-HT2A/5-HT2C inverse agonist 1

    		5-HT Receptor Neurological Disease
    5-HT2A/5-HT2C inverse agonist 1 is a potent and dual 5-HT2A and 5-HT2C receptor inverse agonist with a hERG inhibitions, thus avoiding cardiovascular risks. 5-HT2A/5-HT2C inverse agonist 1 shows significant antipsychotic efficacy in the MK-801 (HY-15084B)-induced mouse model. 5-HT2A/5-HT2C inverse agonist 1 is promising for research of psychosis .
    5-HT2A/5-HT2C inverse agonist 1
  • HY-175532
    M4 mAChR Modulator-2

    		mAChR Neurological Disease
    M4 mAChR Modulator-2 is an orally active, selective, brain-penetrant positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (M4 mAChR) (EC50 = 513 nM). M4 mAChR Modulator-2 exhibits high target selectivity, showing negligible affinity and low inhibition rates for non-target receptors (D1R/D2R/D3R, 5-HT subtypes, κ/δ/μ opioid receptors, H1, M1/M2) while specifically binding to M4 mAChR with a Ki of 377 nM and an inhibition rate of 62.8%. M4 mAChR Modulator-2 reverses Dizocilpine (MK-801) (HY-15084B)-induced hyperlocomotion in mice. M4 mAChR Modulator-2 can be used for the study of schizophrenia
    M4 mAChR Modulator-2
  • HY-157955
    TAAR1 agonist 1

    		Trace Amine-associated Receptor (TAAR) Neurological Disease
    TAAR1 agonist 1 (compound 6E) is a potent TAAR1 agonist with a potent TAAR1-Gs/Gq dual-pathway activation property. TAAR1 agonist 1 significantly alleviates MK-801-induced schizophrenia-like cognitive phenotypes .
    TAAR1 agonist 1
  • HY-176411
    ONO-TR-772

    VU6018042

    		 Potassium Channel Neurological Disease
    ONO-TR-772 (VU6018042) is a selective TREK inhibitor (IC50: 15 nM). ONO-TR-772 enhances recognition memory in the MK-801-stimulated NOR mouse model. ONO-TR-772 can be used in the study of diseases related to cognitive impairment .
    ONO-TR-772
  • HY-176141
    ZH8965

    		Trace Amine-associated Receptor (TAAR) Neurological Disease
    ZH8965 is an orally active TAAR1-Gs/Gq agonist (EC50: 6.1/14.8 nM). ZH8965 improves antipsychotic-like phenotypes and cognitive impairment in the MK-801-induced mouse psychosis model. ZH8965 can be used in schizophrenia research .
    ZH8965
  • HY-157959
    Orphenadrine

    (±)-Orphenadrine

    		 iGluR Cytochrome P450 Cholinesterase (ChE) Neurological Disease Cancer
    Orphenadrine ((±)-Orphenadrine) is a skeletal muscle relaxant and NMDA antagonist that also has antiparkinsonian, antihistamine, antitremor, antispasmodic, and analgesic effects. Orphenadrine inhibits the binding of [3H]MK-801 to the phencyclidine (PCP) binding site of the NMDA receptor. Orphenadrine is also an anticholinergic and CYP2B inducer. Orphenadrine may exert pro-tumor effects, causing CAR nuclear translocation, resulting in microsomal reactive oxygen species (ROS) production and oxidative stress. Orphenadrine also exerts neuronal protection, protecting rat cerebellar granule cells (CGC) from 3-NPA-induced death and has inhibitory potential against neurodegenerative diseases mediated by NMDA receptor overactivation .
    Orphenadrine

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