(-)-MK 801马来酸 T6352

Product Introduction
Bioactivity


英文名: (-)-Dizocilpine maleate

描述: (-)-Dizocilpine maleate ((-)-MK 801 (Maleate)) 是一种选择性且非竞争性的 N-甲基-D-天冬氨酸 (NMDA) 受体拮抗剂，Ki 为 211.7 nM。它是一种 Dizocilpine 的活性较低的 (-)-对映体，具有抗抑郁作用。

细胞实验: 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.

激酶实验: 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.

动物实验: Animal Models: ischemic spinal cord injury medelFormulation: N/ADosages: 1 mg/kgAdministration: IV

体外活性: 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.

体内活性: 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.

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

溶解度: Ethanol : 7 mg/mL(20.7 mM)
DMSO : 68 mg/mL (201.55 mM)


关键字: less-active | transporters | ()Dizocilpine maleate | C 13737 | Inhibitor | Dizocilpine | inhibit | NMDA | ( ) Dizocilpine maleate | MK-801 Maleate | C-13737 | MK801 | monoamine | Ionotropic glutamate receptors | iGluR | Dizocilpine Maleate | antidepressant | MK-801 | MK801 Maleate | MK 801 | MK 801 Maleate

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相关库: Ion Channel Inhibitor Library | Anti-Neurodegenerative Disease Compound Library | Neurotransmitter Receptor Compound Library | Anti-Parkinson's Disease Compound Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Neuronal Signaling Compound Library | Antidepressant Compound Library | Inhibitor Library | NO PAINS Compound Library

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