(-)-Dizocilpine maleate

SKU: orb1300843

Description

Research Area

Neuroscience, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	121917-57-5
MW	337.37
Purity	99.89%
Formula	C₂₀H₁₉NO₄
SMILES	OC(=O)\C=C/C(O)=O.C[C@@]12N[C@@H](Cc3ccccc13)c1ccccc21
Target	NMDAR,iGluR
Solubility	Ethanol:7 mg/mL (20.75 mM);DMSO:68 mg/mL (201.56 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.93 mM)

Bioactivity

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Target IC50	NMEA:Kd：37.2nM
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. Read more...
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. Read more...
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. Read more...
Animal Research	Animal Models: ischemic spinal cord injury medelFormulation: N/ADosages: 1 mg/kgAdministration: IV

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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transporters, Dizocilpine, Dizocilpine Maleate, antidepressant, C 13737, C13737, C-13737, (-)-MK 801 (Maleate), (-)-MK 801 Maleate, ()Dizocilpine maleate, ( ) Dizocilpine maleate, iGluR, Inhibitor, less-active, inhibit, Ionotropic glutamate receptors, monoamine, NMDA Receptor, NMDA, MK 801, MK 801 Maleate, MK801, MK-801, MK801 Maleate, MK-801 Maleate

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Compound Identifiers

PubChem CID

16219612 ↗

Key Properties

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No computed properties available.

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