生物活性

• 描述Both mineralocorticoid receptors and glucocorticoid receptors belong to the family of nuclear receptors. They are respectively encoded by the Nuclear Receptor Subfamily 3 Group C Member 2 and Member 1. The mineralocorticoid receptors mediate aldosterone actions on salt and water balance within restricted target cells and thus function as ligand-dependent transcription factors that bind to mineralocorticoid response elements in order to transactivate target genes. The glucocorticoid receptors function both as transcription factors that bind to glucocorticoid response elements in the promoters of glucocorticoid responsive genes to activate their transcription, and as regulators of other transcription factors. Corticosterone is an adrenocortical steroid that has modest but significant activities as a mineralocorticoid and a glucocorticoid. Corticosterone can act as ligand of both mineralocorticoid receptors and glucocorticoid receptors. In cultured PFC pyramidal neurons, 30 min treatment of 100 nM corticosterone enhanced mEPSC amplitude. In an immunocytochemical approach, 30 min treatment of 100 nM corticosterone increased neuron surface GluR1 cluster density, cluster size and cluster fluorescence intensity^[3]. Revealed by a co-immunoprecipitation assay, 30 min treatment of 100 nM corticosterone increased the formation of GDI-Rab4 complex^[3]. HT22 cells treated by 400 μM corticosterone for 3h resulted in remarkable increase of nuclear localized glucocorticoid receptor^[4]. In an ex vivo experiment, corticosterone inhibited [³H]MMP⁺ uptake in 3V-MH tissue with an IC₅₀ of 0.152 μM^[5].
• 作用机制Corticosterone is an adrenocortical steroid can act as ligand of both mineralocorticoid receptors and glucocorticoid receptors. Corticosterone may exert its actions by binding directly to receptors^[6].
• 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
  NCT02054208	Alzheimer's Disease	Phase 1 Phase 2	Recruiting	July 2019	Korea, Republic of ... more >> Samsung Medical Center Recruiting Seoul, Korea, Republic of Contact: Yunkyung Choi, MD    82-2-3410-6486    yk221.choi@samsung.com    Principal Investigator: Duk L. Na, MD Collapse <<
  NCT03172117	Alzheimer's Disease	Phase 1 Phase 2	Recruiting	December 31, 2021	Korea, Republic of ... more >> Samsung Medical Center Recruiting Seoul, Korea, Republic of Contact: Heejin Choi, MD    +82-2-3410-1947    evekhj@gmail.com    Principal Investigator: Duk L Na, MD Collapse <<
  NCT00667810	Alzheimer Disease	Phase 3	Terminated(The study was termi... more >>nated on August 6, 2012, because 2 large Phase 3 studies showed no clinical benefit. This decision was not based on any new safety concerns.) Collapse <<	-	-

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• 参考文献

• [1] Pinson SE, Wilson JL, et al. Timing matters: corticosterone injections 4 h before ovulation bias sex ratios towards females in chickens. J Comp Physiol B. 2015 Jul;185(5):539-46.

  [2] Ebada ME, Latif LM, et al. Corticosterone protects against memory impairments and reduced hippocampal BDNF levels induced by a chronic low dose of ethanol in C57BL/6J mice. Rom J Morphol Embryol. 2014;55(4):1303-16.

  [3] Liu W, Yuen EY, Yan Z. The stress hormone corticosterone increases synaptic alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors via serum- and glucocorticoid-inducible kinase (SGK) regulation of the GDI-Rab4 complex. J Biol Chem. 2010 Feb 26;285(9):6101-8.

  [4] Xu B, Lang L, Li S, Yuan J, Wang J, Yang H, Lian S. Corticosterone Excess-Mediated Mitochondrial Damage Induces Hippocampal Neuronal Autophagy in Mice Following Cold Exposure. Animals (Basel). 2019 Sep 14;9(9):682.

  [5] Gasser PJ, Lowry CA, Orchinik M. Corticosterone-sensitive monoamine transport in the rat dorsomedial hypothalamus: potential role for organic cation transporter 3 in stress-induced modulation of monoaminergic neurotransmission. J Neurosci. 2006 Aug 23;26(34):8758-66.

  [6] Bering T, Hertz H, Rath MF. Rhythmic Release of Corticosterone Induces Circadian Clock Gene Expression in the Cerebellum. Neuroendocrinology. 2020;110(7-8):604-615.

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