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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
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