MK-801 free base · Synonyms: Dizocilpine

Dizocilpine, a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist.

For research use only. Not for human or veterinary use.

Target iGluR

Research area Neurological Disease

Purity >98% Stock Inquire

Data Sheet SDS COA

MK-801 structure

CAS No.: 77086-21-6

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 440.00	BP-02085-250mg	In stock	Get quote
500 mg	USD 730.00	BP-02085-500mg	In stock	Get quote
1 g	USD 1,170.00	BP-02085-1g	In stock	Get quote
2 g	USD 1,875.00	BP-02085-2g	In stock	Get quote
3 g	USD 2,250.00	BP-02085-3g	In stock	Get quote
5 g	USD 3,000.00	BP-02085-5g	In stock	Get quote
10 g	USD 4,800.00	BP-02085-10g	In stock	Get quote

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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.

Biological activity

In Vitro Dizocilpine (MK-801) progressively suppresses of current induced by NMDA. Mg2+ (10 mM) prevents Dizocilpine from blocking the N-Me-D-Asp-induced current, even when Dizocilpine is applied for a long time in the presence of NMDA. Dizocilpine blocks NMDA-activated single-channel activity in outside-out patches. Dizocilpine (MK-801; <500 μM) inhibits activation of microglia induced by LPS with increased Cox-2 protein expression in BV-2 cells. Dizocilpine (<500 μM) reduces microglial TNF-α output with an EC50 of 400 μM in BV-2 cells.

Identifiers

SMILES: C[C@]12N[C@H](CC3=CC=CC=C13)C1=CC=CC=C21
InChIKey: LBOJYSIDWZQNJS-CVEARBPZSA-N

Specifications

MW (average): 221.2970
Formula: C₁₆H₁₅N
CAS No.: 77086-21-6
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

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]. 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.

[4]. 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.

[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.

Same target

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