MK-801 (Dizocilpine)

Catalog No.S2857

MK-801 (Dizocilpine) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM.

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MK-801 (Dizocilpine) Chemical Structure

MK-801 (Dizocilpine) Chemical Structure
Molecular Weight: 221.3

Validation & Quality Control

Quality Control & MSDS

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Product Description

Biological Activity

Description MK-801 (Dizocilpine) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM.
Targets NMDA Receptor [1]
IC50 30.5 nM(Ki)
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. [1]
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. [3]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

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 Assay: [2]

Cell lines mixed neuronal/glial cell cultures
Concentrations 10 μM
Incubation Time 30 minutes
Method 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 Study: [3]

Animal Models ischemic spinal cord injury medel
Formulation N/A
Dosages 1 mg/kg
Administration IV

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Wong EH et al., Proc Natl Acad Sci U S A, 1986, 83(18), 7104-7108.

[2] Wise-Faberowski L et al., J Neurosurg Anesthesiol, 2006, 18(4), 240-246.

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Chemical Information

Download MK-801 (Dizocilpine) SDF
Molecular Weight (MW) 221.3
Formula

 

C16H15N
 
CAS No. 77086-21-6
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms C13737
Solubility (25°C) * In vitro DMSO 67 mg/mL (302.75 mM)
Ethanol 7 mg/mL (31.63 mM)
Water <1 mg/mL (<1 mM)
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 15 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 5H-Dibenzo[a,d]cyclohepten-5,10-imine, 10,11-dihydro-5-methyl-, (5S,10R)-

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