生物活性

• 描述Endothelial cells (EC) can regulate the permeability in brain endothelium which is helpful to overcome the restriction of drug delivery into the brain. Dexamethasone Acetate is an acetate form of Dexamethasone. Dexamethasone is a corticosteroid medication used in modulating tight junction permeability and interleukin receptor modulator with different EC50 values and IC50 values in different kind of cells. GPNT cells treated with 1 μM dexamethasone demonstrated no change in transendothelial resistance, which decreased the permeability and reduced the size of the small pore as well. Dexamethasone treatment can lead to IL-6 and RPM18226 repressions with IC50 values of 1.4 and 6.5 nM respectively. The binding Ki of glucocorticoid receptor (GR) and mineralocorticoid (MR) were 2.1 and 7.2 nM respectively. While in human SW1353 cells, dexamethasone treatment showed an IC50 of GR binding of 3.5nM, the IC50 for transrepression of IL-1 induced MMP-13 expression and transrepression HWB-TNFα were 1.8 and 21 nM respectively. In LPS stimulated human PBMCs, DM affected cytokine production with EC50 values ranging from 10 to 72 nM, while the values were ranged from 0.47 to 4.1 nM and from 0.92 to >200 nM in Anti-CD3 and PHA stimulated human PBMCs respectively. In human H13 cells, DM inhibited GR with EC50 of 9.7 nM, all together suggesting a good in vitro and in vivo anti-inflammatory activity of this compound . DM exposure in the 5-month-old ewes demonstrated unchanged blood pressure and eNOS RNA and protein levels, increased sensitivity to endothelin-1 (ET), enhanced acetylcholine-induced relaxation and abolished L-NAME suppressible vasodilatory response to ET, suggesting that DM led to endothelial dysfunction and vasodilatory compensation in these animals.

• 动物研究
  剂量	Horse: 83 μg/kg[3] (i.m.) Rat: 0.527 μg/kg[3] (p.o.) Cow: 40 μg/kg[3] (i.v.)
  给药途径	i.m., p.o., i.v.

• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT03283046	Malignant Neoplasms Stated as ... more >>Primary Lymphoid Haematopoietic Multiple Myeloma Collapse <<	Phase 1	Withdrawn(Similar to another s... more >>tudy.) Collapse <<	October 2020	-
  NCT03740659	Cataract	Phase 2	Recruiting	March 2019	Italy ... more >> ASST Santi Paolo e Carlo di Milano - P.O. San Paolo di Milano Recruiting Milano, MI, Italy, 20142 Contact: Luca Rossetti, Prof.    +390250323150    luca.rossetti@unimi.it    Principal Investigator: Luca Rossetti, Prof.          A.O.U. Pisana - P.O. di Cisanello Recruiting Pisa, PI, Italy, 56124 Contact: Marco Nardi, Prof.       marco.nardi@med.unipi.it    Principal Investigator: Marco Nardi, Prof. Collapse <<
  NCT03122756	Cesarean Section	Early Phase 1	Recruiting	October 2018	Egypt ... more >> Ain Shams Maternity Hospital Recruiting Cairo, Egypt Contact: Mahmoud AA ElShourbagy, MD    +201001448189    elshourbagym22@hotmail.com Collapse <<

• 更多
• 参考文献

• [1] LaLone CA, Villeneuve DL, et al. Effects of a glucocorticoid receptor agonist, dexamethasone, on fathead minnow reproduction, growth, and development. Environ Toxicol Chem. 2012 Mar;31(3):611-22.

  [2] Blanco FJ, Guitian R, et al. Effect of antiinflammatory drugs on COX-1 and COX-2 activity in human articular chondrocytes. J Rheumatol. 1999 Jun;26(6):1366-73.

  [3] Dexamethasone