Peso molecular: 392,46 La dexametasona es un potente miembro sintético de la clase de glucocorticoides de fármacos esteroides y un modulador del receptor de interleucina que tiene efectos antiinflamatorios e inmunosupresores. \ N Actividad biológica
|
Description
|
Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects.
|
|
In vitro
|
Dexamethasone results in decrease in transmonolayer paracellular permeability mainly to sucrose, fluorescein and dextrans of up to 20 KDa in an immortalised rat brain endothelial cell line (GPNT). Dexamethasone results in filamentous actin and the cytoskeleton associated protein cortactin being highly concentrated in the regions of cell-cell contact with few F-actin stress fibres visible within the cytoplasm in cultured rat brain endothelial cells, an observation consistent with a more differentiated barrier phenotype induced by dexamethasone. Dexamethasone treatment has been shown to strongly stimulate the level of the Id-1 protein, which is a serum-inducible helix-loop-helix transcriptional repressor, involved in cell differentiation, and this effect was shown to be associated with reorganisation of ZO-1 to the cell periphery in Con8 mammary epithelial tumor cells. Dexamethasone prevents cytokine-induced enhanced expression of MMP-9 and alterations in the expression of ZO-1 in untreated GPNT monolayers. [1] Dexamethasone depletes both basal and TNF-alpha-stimulated GSH levels by down-regulating the gamma-GCS-heavy subunit transcription via a mechanism involving AP-1 (c-Jun) in alveolar epithelial cells. Dexamethasone decreases both basal and stimulated GSH levels (TNF-α-treated) in alveolar epithelial cells (A549), without any change in GSSG. [2]
|
|
In vivo
|
Dexamethasone is administered i.m. to pregnant ewes, leads to the following results (1) blood pressure is unchanged; (2) as previously reported in the fetus, sensitivity to endothelin-1 (ET) is increased; (3) acetylcholine-induced relaxation is increased; (4) L-NAME suppressible vasodilatory response to ET is abolished; (5) there is no change in endothelium-independent vasodilatation; and (6) there is no change in eNOS RNA and protein levels, when compared to saline treated controls. [3]
|
|
Features
|
|
Protocolo (solo como referencia) Conversión de diferentes modelos de animales basados en BSA (valor basado en datos del Borrador de Directrices de la FDA)
|
Species
|
Baboon
|
Dog
|
Monkey
|
Rabbit
|
Guinea pig
|
Rat
|
Hamster
|
Mouse
|
|
Weight (kg)
|
12
|
10
|
3
|
1.8
|
0.4
|
0.15
|
0.08
|
0.02
|
|
Body Surface Area (m2)
|
0.6
|
0.5
|
0.24
|
0.15
|
0.05
|
0.025
|
0.02
|
0.007
|
|
Km factor
|
20
|
20
|
12
|
12
|
8
|
6
|
5
|
3
|
|
Animal A (mg/kg) = Animal B (mg/kg) multiplied by
|
Animal B Km
|
|
Animal A Km
|
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.
|
Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×
|
mouse Km(3)
|
= 11.2 mg/kg
|
|
rat Km(6)
|
1 Referencias [1] Romero IA, et al. Neurosci Lett, 2003, 344 (2), 112-116. [2] Rahman I y col. Biochem Pharmacol, 2000, 60 (8), 1041-1049. [3] Molnar J, et al. J Physiol, 2003, 547 (Parte 1), 61-66. [4] Suzuki E y col. Clin Cancer Res, 2005, 11 (18), 6713-6721. [5] Kunnumakkara AB, et al. Cancer Res, 2007, 67 (8), 3853-3861. \ n Información química
|
Molecular Weight (MW)
|
392.46
|
|
Formula
|
C22H29FO5
|
|
CAS No.
|
50-02-2
|
|
Storage
|
3 years -20℃Powder
|
|
6 months-80℃in solvent (DMSO, water, etc.)
|
|
Synonyms
|
|
|
Solubility (25°C) *
|
In vitro
|
DMSO
|
79 mg/mL
(201.29 mM)
|
|
Water
|
<1 mg/mL
(
|
|
Ethanol
|
6 mg/mL
(15.28 mM)
|
|
In vivo
|
30% PEG400/0.5% Tween80/5% propylene glycol
|
30 mg/mL
|
|
|
Chemical Name
|
(8S,9R,10S,11S,13S,14S,16R,17R)-9-fluoro-11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-7,8,11,12,13,15,16,17-octahydro-6H-cyclopenta[a]phenanthren-3(9H,10H,14H)-one
|
Grupos de Producto : Otros > Inhibidor del receptor de IL
