.cp_wz table {border-top: 1px solid #ccc; border-left: 1px solid #ccc; } .cp_wz table td {border-right: 1px solid #ccc; borda inferior: 1px sólido #ccc; preenchimento: 5px 0px 0px 5px;} .cp_wz tabela th {border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; preenchimento: 5px 0px 0px 5px;} \ n Peso molecular: 221,3 MK-801 (Dizocilpina) é um potente antagonista do receptor N-metil-D-aspartato (NMDA) com Ki de 30,5 nM. \ n Estudos neurofisiológicos de atividade biológica in vitro, usando uma preparação de fatia cortical de rato, demonstra uma ação antagonista potente, seletiva e não competitiva da dizocilpina nas respostas despolarizantes a N-Me-D-Asp, mas não ao cainato ou quisqualato. As potências da fenciclidina, SKF 10047 e os enantiômeros da dizocilpina como antagonistas de N-Me-D-Asp correlacionam-se intimamente (r = 0,99) com suas potências como inibidores da ligação da [3H] dizocilpina. Isso sugere que os locais de ligação da dizocilpina estão associados aos receptores N-Me-D-Asp e fornece uma explicação para o mecanismo de ação da dizocilpina como anticonvulsivante. Todos os ratos de controle têm déficits neurológicos permanentes graves após lesão isquêmica da medula espinhal (ISCI), enquanto os ratos tratados com dizocilpina têm protocolo estatisticamente (apenas para referência)
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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.
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Cell lines
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mixed neuronal/glial cell cultures
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Concentrations
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10 μM
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Incubation Time
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30 minutes
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Method
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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.
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Animal Models
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ischemic spinal cord injury medel
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Formulation
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N/A
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Dosages
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1 mg/kg
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Administration
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IV
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Solubility
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30% PEG400/0.5% Tween80/5% propylene glycol,
15 mg/mL
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* 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.
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Conversão de diferentes modelos de animais com base em BSA (valor com base em dados das diretrizes preliminares da FDA)
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Species
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Baboon
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Dog
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Monkey
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Rabbit
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Guinea pig
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Rat
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Hamster
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Mouse
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Weight (kg)
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12
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10
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3
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1.8
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0.4
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0.15
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0.08
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0.02
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Body Surface Area (m2)
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0.6
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0.5
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0.24
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0.15
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0.05
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0.025
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0.02
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0.007
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Km factor
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20
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20
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12
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12
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8
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6
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5
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3
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Animal A (mg/kg) = Animal B (mg/kg) multiplied by
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Animal B Km
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Animal A Km
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Por exemplo, para modificar a dose de resveratrol usada para um camundongo (22,4 mg / kg) para uma dose baseada na BSA para um rato, multiplique 22,4 mg / kg pelo fator Km para um camundongo e, em seguida, divida pelo fator Km para um rato. Este cálculo resulta em uma dose equivalente de rato para o resveratrol de 11,2 mg / kg.
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Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×
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mouse Km(3)
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= 11.2 mg/kg
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rat Km(6)
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Informação Química
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Molecular Weight (MW)
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221.3
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Formula
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C16H15N
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CAS No.
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77086-21-6
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Storage
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3 years -20℃Powder
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6 months-80℃in solvent (DMSO, water, etc.)
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Synonyms
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Solubility (25°C) *
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In vitro
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DMSO
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67 mg/mL
(302.75 mM)
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Water
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<1 mg/mL
(
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Ethanol
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7 mg/mL
(31.63 mM)
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In vivo
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30% PEG400/0.5% Tween80/5% propylene glycol
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15 mg/mL
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* <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.
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Chemical Name
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5H-Dibenzo[a,d]cyclohepten-5,10-imine, 10,11-dihydro-5-methyl-, (5S,10R)-
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Calculadora de molaridade Calculadora de diluição Calculadora de peso molecular
Grupo de Produto : Sinalização Neuronal > Inibidor GluR
