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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
30 Results for "
MK-801
" in MedChemExpress (MCE) Product Catalog:
Products (30)
30 Results for "MK-801" in MCE Product Catalog:
49
Target:
Research Areas:
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 .
49
49 Cited Publications
Synonyms: (+)-MK 801 Maleate
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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.
Synonyms: (-)-MK-801 maleate
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(-)-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 .
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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 .
Synonyms: SUVN-502 mesylate
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Masupirdine mesylate (SUVN-502 mesylate) is a potent, selective, orally active, and brain-penetrating 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine mesylate has pro-cognitive effects on all stages of cognition (acquisition, consolidation, and retention), and can reverse Scopolamine (HY-N0296), MK-801 (HY-15084B)-induced and aging-related memory deficits. Masupirdine mesylate can be used in the research of Alzheimer's disease .
Cat. No.: HY-179004
CAS No.: 2640753-22-4
Synonyms: VU6022856
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ONO-9517601 is a potent, orally active, selective and CNS
penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC50= 0.067 μM, TREK-2 IC50= 0.23 μM). ONO-9517601 displays robust efficacy in an
MK-801 (HY-15084B) challenge rat novel object recognition (NOR) paradigm.
ONO-9517601 can be used for research on neurological and cognitive
disorders .
Cat. No.: HY-172419
CAS No.: 2881017-49-6
Synonyms: GM-1020
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Blixeprodil (GM-1020) is an orally active, blood-brain barrier-penetrant NMDA receptor inhibitor with a Ki of 3.25 µM in rat cortical tissues. Blixeprodil binds to the MK-801 ion channel site and blocks NMDA receptor-mediated currents in hyperpolarized states in a voltage-dependent manner. Blixeprodil modulates the power of cortical EEG frequency bands, alters spontaneous motor activity, and induces ataxia at high doses. Blixeprodil can be used in the research of depression .
Cat. No.: HY-164264
CAS No.: 217176-91-5
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Caged MK801 (cMK801) is a selective, non-competitive, irreversible NMDA receptor open-channel blocker. NVOC cages are neuro pharmocologically compatible .
Cat. No.: HY-107694
CAS No.: 70449-94-4
Synonyms: (Rac)-MK-801
(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 .
Cat. No.: HY-107695
CAS No.: 111686-79-4
Synonyms: FPL 12924AA
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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 .
Cat. No.: HY-179005
CAS No.: 2640753-27-9
Synonyms: VU6024391
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ONO-7927846 is a potent, orally active, selective and CNS penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC50= 0.11 μM, TREK-2 IC50= 0.29 μM). ONO-7927846 displays robust efficacy in an MK-801 (HY-15084B) challenge rat novel object recognition (NOR) paradigm. ONO-7927846 can be used for research on neurological and cognitive disorders .
Cat. No.: HY-170499
Synonyms: BI02982816
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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 .
Cat. No.: HY-19021
CAS No.: 55643-87-3
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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 .
Cat. No.: HY-109118
CAS No.: 701205-60-9
Synonyms: SUVN-502 free base
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Masupirdine free base (SUVN-502 free base) is a potent, selective, orally active, and brain-penetrating 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine free base has pro-cognitive effects on all stages of cognition (acquisition, consolidation, and retention), and can reverse Scopolamine (HY-N0296), MK-801 (HY-15084B)-induced and aging-related memory deficits. Masupirdine free base can be used in the research of Alzheimer's disease .
Cat. No.: HY-169001
CAS No.: 2718990-76-0
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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 .
Cat. No.: HY-179008
CAS No.: 2841457-05-2
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5-HT2CR agonist 2 (Compound 16k) is a selective, blood-brain barrier-penetrating and Gq-biased 5-HT2CR agonist, with an EC50 of 36 nM. 5-HT2CR agonist 2 attenuates MK801 (HY-15084B)-induced hyperlocomotion and reverses Phencyclidine-induced hyperlocomotor activity .
Cat. No.: HY-175532
CAS No.: 3062458-27-6
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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
Cat. No.: HY-157955
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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 .
Cat. No.: HY-19841
CAS No.: 452917-21-4
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AVE-5997 is a selective b>D3 antagonist. AVE-5997 antagonizes MK-801 (HY-15084B)-induced hyperactivity. AVE-5997 can be used in the research of schizophrenia .
Cat. No.: HY-N5159
CAS No.: 197960-94-4
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
