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(-)-Dizocilpine maleate

Catalog No. T6352 CAS 121917-57-5

Synonyms: C13737, (-)-MK 801 (Maleate), (-)-MK 801 Maleate

(-)-Dizocilpine maleate ((-)-MK 801 (Maleate)) is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.

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(-)-Dizocilpine maleate Chemical Structure

(-)-Dizocilpine maleate, CAS 121917-57-5

Pack Size	Availability	Price/USD
10 mg	In stock	$ 43.00
25 mg	In stock	$ 74.00
50 mg	In stock	$ 122.00
100 mg	In stock	$ 228.00
1 mL * 10 mM (in DMSO)	In stock	$ 48.00

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Purity: 99.89%

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Description	(-)-Dizocilpine maleate ((-)-MK 801 (Maleate)) is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.
Targets&IC50	NMEA:Kd：37.2nM
In vitro	Neurophysiological studies in vitro, using a rat cortical-slice preparation, demonstrates a potent, selective, and noncompetitive antagonistic action of dizocilpine on depolarizing responses to N-Me-D-Asp but not to kainate or quisqualate. The potencies of phencyclidine, ketamine, SKF 10047, and the enantiomers of dizocilpine as N-Me-D-Asp antagonists correlate closely (r = 0.99) with their potencies as inhibitors of [3H] dizocilpine binding. This suggests that the dizocilpine binding sites are associated with N-Me-D-Asp receptors and provides an explanation for the mechanism of action of dizocilpine as an anticonvulsant.
In vivo	All the control rats have severe permanent neurological deficits after ischemic spinal cord injury (ISCI), whereas the dizocilpine–treated rats have statistically (P < .05) better neurological outcome and good recovery. Histopathology reveals severe neuronal necrosis in the lumbar gray matter of control rats, whereas dizocilpine–treated rats show mild injury. These results demonstrate that a single dose of dizocilpine given before ISCI provides significant neuroprotection.
Kinase Assay	In vitro binding assays:For in vitro binding assays, cerebral cortices from male Sprague-Dawley rats (200-300 g) are homogenized in 9 volumes of ice-cold sucrose by nine strokes with a Teflon/glass homogenizer at 500 rpm. The homogenate is centrifuged for 10 min at 1000 x g, and the supernatant is recentrifuged at 10,000 x g for 20 min at 4 ℃. The pellet is suspended in assay buffer and incubated for 20 min prior to final centrifugation at 10,000 x g for 20 min at 4 ℃. The pellet is resuspended in assay buffer (70 ml per gram of original tissue). Binding of [3H] dizocilpine is measured by incubating 750 ul duplicate aliquots of this crude membrane suspension (=0.75 mg of protein) with 100 ul of buffer containing displacer or of buffer alone (total binding), 100 ul of 50 nM [3H] dizocilpine, and 50 ul of buffer for 60 min at 23 ℃. Nonspecific binding is defined by unlabeled dizocilpine. Incubation is terminated by rapid filtration through Whatman GF/B filters, which are washed immediately with two 5-ml portions of ice-cold assay buffer in a Brandel M 24-R cell harvester. The time required for the complete filtration and washing procedure is less than 10 sec. Radioactivity on the filters is determined by liquid scintillation counting in standard vials with 10 ml of Hydrofluor at 41% counting efficiency.
Cell Research	Cell lines: mixed neuronal/glial cell culturesConcentrations: 10 μMIncubation Time: 30 minutesMethod: Primary mixed neuronal/glial cultures are prepared from fetal rat brains. Mature cultures are exposed to dissolved isoflurane [0.4 mM (1.8 minimum alveolar concentration) or 1.6 mM (7 minimum alveolar concentration)] or dizocilpine (10 μM), and NMDA (0 or 3 μM) at 37 ℃ for 30 minutes. Apoptosis is assessed using terminal-deoxy-nucleotidyl end-nick labeling oligonucleosomal DNA fragmentation enzyme-linked immunosorbent assay, and caspases-3 and -9 activation assays.
Animal Research	Animal Models: ischemic spinal cord injury medelFormulation: N/ADosages: 1 mg/kgAdministration: IV

Synonyms	C13737, (-)-MK 801 (Maleate), (-)-MK 801 Maleate
Molecular Weight	337.37
Formula	C20H19NO4
CAS No.	121917-57-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 7 mg/mL(20.7 mM)

DMSO: 68 mg/mL (201.55 mM)

References and Literature

1. Wong EH, et al. Proc Natl Acad Sci U S A, 1986, 83(18), 7104-7108. 2. Snell LD, et al. Eur J Pharmacol, 1988, 145(2), 223-226.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Neurodegenerative Disease Compound Library Antidepressant Compound Library Bioactive Compound Library Neurotransmitter Receptor Compound Library Neuronal Signaling Compound Library Anti-Parkinson's Disease Compound Library Ion Channel Inhibitor Library NO PAINS Compound Library Preclinical Compound Library

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Keywords

(-)-Dizocilpine maleate 121917-57-5 Membrane transporter/Ion channel Neuroscience NMDAR iGluR less-active transporters ()Dizocilpine maleate C 13737 Inhibitor C13737 (-)-MK 801 (Maleate) Dizocilpine inhibit NMDA ( ) Dizocilpine maleate MK-801 Maleate C-13737 MK801 monoamine Ionotropic glutamate receptors Dizocilpine Maleate (-)-MK 801 Maleate antidepressant MK-801 MK801 Maleate MK 801 MK 801 Maleate inhibitor

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