.cp_wz tabla {borde superior: 1px sólido #ccc; borde izquierdo: 1px sólido #ccc; } .cp_wz table td {borde derecho: 1px sólido #ccc; borde inferior: 1px sólido #ccc; padding: 5px 0px 0px 5px;} .cp_wz table th {border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; relleno: 5px 0px 0px 5px;} \ n Peso molecular: 221,3 MK-801 (Dizocilpina) es un potente antagonista del receptor de N-metil-D-aspartato (NMDA) con Ki de 30,5 nM. \ n Actividad biológica Estudios neurofisiológicos in vitro, utilizando una preparación de corte cortical de rata, demuestra una acción antagonista potente, selectiva y no competitiva de la dizocilpina sobre las respuestas despolarizantes a N-Me-D-Asp pero no a kainato o quiscualato. Las potencias de fenciclidina, SKF 10047, y los enantiómeros de dizocilpina como antagonistas de N-Me-D-Asp se correlacionan estrechamente (r = 0,99) con sus potencias como inhibidores de la unión de [3H] dizocilpina. Esto sugiere que los sitios de unión de la dizocilpina están asociados con los receptores N-Me-D-Asp y proporciona una explicación del mecanismo de acción de la dizocilpina como anticonvulsivo. Todas las ratas de control tienen graves déficits neurológicos permanentes después de una lesión isquémica de la médula espinal (ISCI), mientras que las ratas tratadas con dizocilpina tienen protocolo estadístico (solo como referencia)
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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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Conversión de diferentes modelos de animales basados en BSA (valor basado en datos del Borrador de Directrices de la 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 ejemplo, para modificar la dosis de resveratrol utilizada para un ratón (22,4 mg / kg) a una dosis basada en el BSA para una rata, multiplique 22,4 mg / kg por el factor Km para un ratón y luego divida por el factor Km para una rata. Este cálculo da como resultado una dosis equivalente para ratas de 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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Información 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 molaridad Calculadora de dilución Calculadora de peso molecular
Grupos de Producto : Señalización neuronal > Inhibidor de GluR
