受注:045-509-1970 |
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Synonyms | C13737 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C16H15N.C4H4O4 |
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分子量 | 337.37 | CAS No. | 121917-57-5 | |
Solubility (25°C)* | 体外 | DMSO | 67 mg/mL (198.59 mM) | |
Ethanol | 7 mg/mL (20.74 mM) | |||
Water | Insoluble | |||
* <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. |
製品説明 | (-)-Dizocilpine (MK 801, Dizocilpine, C13737) Maleate is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM. |
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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] |
キナーゼアッセイ | In vitro binding assays | |
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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. | ||
細胞アッセイ | 細胞株 | mixed neuronal/glial cell cultures |
濃度 | 10 μM | |
反応時間 | 30 minutes | |
実験の流れ | 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. | |
動物実験 | 動物モデル | ischemic spinal cord injury medel |
投薬量 | 1 mg/kg | |
投与方法 | IV |
Data from [Data independently produced by , , Pharmacology, Biochemistry and Behavior, 2016, 146-147:21–27.]
Sevoflurane upregulates neuron death process-related Ddit4 expression by NMDAR in the hippocampus [ Aging -Albany NY), 2023, 15(12):5698-5712] | PubMed: 37348034 |
Sevoflurane upregulates neuron death process-related Ddit4 expression by NMDAR in the hippocampus [ Aging (Albany NY), 2023, 15(12):5698-5712] | PubMed: 37348034 |
Characterization of Non-Specific Uptake and Retention Mechanisms of [177Lu]Lu-PSMA-617 in the Salivary Glands [ Pharmaceuticals (Basel), 2023, 16(5)692] | PubMed: 37242475 |
Functionally distinct roles for eEF2K in the control of ribosome availability and p-body abundance [ Nat Commun, 2021, 12(1):6789] | PubMed: 34815424 |
Lipid bilayers regulate allosteric signal of NMDA receptor GluN1 C-terminal domain [ Biochem Biophys Res Commun, 2021, 585:15-21] | PubMed: 34781056 |
Ketamine inhibits aerobic glycolysis in colorectal cancer cells by blocking the NMDA receptor-CaMK II-c-Myc pathway. [ Clin Exp Pharmacol Physiol, 2020, 47(5):848-856] | PubMed: 31889340 |
Propofol Disrupts Aerobic Glycolysis in Colorectal Cancer Cells via Inactivation of the NMDAR-CAMKII-ERK Pathway [ Cell Physiol Biochem, 2018, 46(2):492-504] | PubMed: 29614493 |
Local Administration of Thiamine Ameliorates Ongoing Pain in a Rat Model of Second-Degree Burn [Zhang K J Burn Care Res, 2017, 38(5):e842-e850] | PubMed: 28181986 |
Shift in interictal relative gamma power as a novel biomarker for drug response in two mouse models of absence epilepsy [Maheshwari A Epilepsia, 2016, 57(1):79-88] | PubMed: 26663261 |
Resveratrol protects CA1 neurons against focal cerebral ischemic reperfusion-induced damage via the ERK-CREB signaling pathway in rats [Li Z, et al. Pharmacol Biochem Behav, 2016, 146-147:21-27] | PubMed: 27143440 |
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