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Dizocilpine

Product Specifications

UNSPSC 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].

Target Antigen

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

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

C[C@]1(N2)C3=CC=CC=C3C[C@]2([H])C4=CC=CC=C14

Molecular Weight

221.30

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]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.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.|Mol Neurobiol. 2023 Dec 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. 2023 Nov 22;186(24):5347-5362.e24.|Eur J Neurosci. 2024 Jul 23.|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. |Psychoneuroendocrinology. 2024 Oct:168:107138.|Res Sq. 2024 Jul 15.

Shipping Conditions

Blue Ice

Product Datasheet

http://file.medchemexpress.com/batch_PDF/HY-15084B/Dizocilpine-DataSheet-MedChemExpress.pdf

Product MSDS

http://file.medchemexpress.com/batch_PDF/HY-15084B/Dizocilpine-SDS-MedChemExpress.pdf

Clinical Information

No Development Reported

CAS Number

77086-21-6

Available Sizes

Curated Selection

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