Dizocilpine
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 Ca2+ flux[1][2].
Product Specifications
CAS Number
77086-21-6
Product Name Alternative
MK-801
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
IGluR
Type
Reference compound
Related Pathways
Membrane Transporter/Ion Channel; Neuronal Signaling
Applications
Neuroscience-Neurodegeneration
Field of Research
Neurological Disease
Assay Protocol
https://www.medchemexpress.com/dizocilpine-free-base.html
Purity
99.95
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
C[C@]1(N2)C3=CC=CC=C3C[C@]2([H])C4=CC=CC=C14
Molecular Formula
C16H15N
Molecular Weight
221.30
Precautions
H302, H315, H319, H335
References & Citations
[1]Wong EH, et al. The anticonvulsant MK-801 is a potent N-methyl-D-aspartate antagonist. Proc Natl Acad Sci U S A. 1986 Sep;83 (18) :7104-8.|[2]Wegener N, et al. Evaluation of brain pharmacokinetics of (+) MK-801 in relation to behaviour. Neurosci Lett. 2011 Sep 26;503 (1) :68-72. |[3]Huettner JE, et al. Block of N-methyl-D-aspartate-activated current by the anticonvulsant MK-801: selective binding to open channels. Proc Natl Acad Sci U S A. 1988 Feb;85 (4) :1307-11.|[4]Thomas DM, et al. MK-801 and dextromethorphan block microglial activation and protect against methamphetamine-induced neurotoxicity. Brain Res. 2005 Jul 19;1050 (1-2) :190-8.|[5]Brown TE, et al. The NMDA antagonist MK-801 disrupts reconsolidation of a cocaine-associated memory for conditioned place preference but not for self-administration in rats. Learn Mem. 2008 Dec 2;15 (12) :857-65.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
NMDA Receptor
Citation 01
Basic Clin Neurosci. 2023 Jan-Feb;14 (1) :103-116.|Behav Brain Res. 2026 Feb 26:498:115917.|Bioorg Med Chem. 2022 Apr 1:59:116675.|Br J Pharmacol. 2020 Oct;177 (20) :4720-4733.|Brain Res. 2023 Aug 1:1812:148409.|Cell Biosci. 2023 Mar 16;13 (1) :57.|Eur J Pharmacol. 2022 Dec 5:936:175343.|Front Biosci (Landmark Ed) . 2023 Jul 19;28 (7) :140.|Int J Mol Sci. 2022 Dec 18;23 (24) :16150.|J Cell Mol Med. 2020 Aug;24 (16) :9287-9299.|J Med Chem. 2023 May 11;66 (9) :6274-6287.|J Orthop Surg Res. 2025 Jan 23;20 (1) :83.|J Physiol. 2023 Aug;601 (16) :3585-3604.|Mol Neurobiol. 2024 Jul;61 (7) :4166-4177.|Molecules. 2023 Mar 2;28 (5) :2304.|Nat Neurosci. 2022 Jan;25 (1) :39-49.|Neuropharmacology. 2025 Jan 20:110318.|Neurosci Lett. 2023 Sep 25:814:137471.|RSC Adv. 2022 Oct 3;12 (43) :28098-28103.|Sci Rep. 2025 May 25;15 (1) :18255.|Virulence. 2025 Dec;16 (1) :2490208.|Cell. 2023 Nov 22;186 (24) :5347-5362.e24.|Eur J Neurosci. 2024 Sep;60 (5) :4830-4842.|Eur J Pharmacol. 2019 Aug 15:857:172427.|Evid Based Complement Alternat Med. 2020 Mar 10;2020:3524641.|Front Cell Dev Biol. 2020 Feb 4;8:24. |Front Cell Neurosci. 2019 Jun 25:13:276.|Front Neurosci. 2019 Nov 19;13:1225.|Life Sci. 2022 Apr 15:295:120419.|Mol Psychiatry. 2022 Sep;27 (9) :3885-3897.|Neuropharmacology. 2024 Dec 24:110284.|Neuroreport. 2017 May 24;28 (8) :444-450. |Prog Neuropsychopharmacol Biol Psychiatry. 2025 Dec 20:143:111555.|Psychoneuroendocrinology. 2024 Oct:168:107138.|Psychopharmacology (Berl) . 2025 Mar;242 (3) :651-661.|Res Sq. 2024 Jul 15.|Sci Bull. 2025 Apr 15;70 (7) :1126-1138.|SSRN. 2025 Jun 18.
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