Download Files:
Products Details
Product Description
– 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].
Web ID
– HY-15084B
Shipping
– Room temperature
Applications
– Neuroscience-Neurodegeneration
Molecular Formula
– C16H15N
Citations
– Basic and Clinical Neuroscience. 2021 Jul.|Bioorg Med Chem. 2022 Feb 18;59:116675.|Br J Pharmacol. 2020 Oct;177(20):4720-4733.|Brain Res. 2023 May 17;1812:148409.|Cell Biosci. 2023 Mar 16;13(1):57.|Eur J Pharmacol. 2022 Oct 25;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 2.|J Physiol. 2023 Jul 8.|Molecules. 2023 Mar 2.|Nat Neurosci. 2021 Dec 9.|Neurosci Lett. 2023 Sep 4;137471.|RSC Adv. 2022 Oct 3;12(43):28098-28103.|Cell Host Microbe. 2023 Nov 8;31(11):1792-1803.e7.|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 Feb 17;295:120419.|Mol Psychiatry. 2022 Jun 17.|Neuroreport. 2017 May 24;28(8):444-450.
References
– [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]Vardhan Reddy KH, et al. Convergent Strategy to Dizocilpine MK-801 and Derivatives. J Org Chem. 2018 Apr 6;83(7):4264-4269.|[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.
CAS Number
– 77086-21-6
Molecular Weight
– 221.30
SMILES
– C[C@]1(N2)C3=CC=CC=C3C[C@]2([H])C4=CC=CC=C14
Clinical Information
– No Development Reported
Research Area
– Neurological Disease
Solubility
– 10 mM in DMSO
Target
– iGluR
Isoform
– NMDA Receptor
Pathway
– Membrane Transporter/Ion Channel;Neuronal Signaling
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
