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FKBP5 mRNA expression is a biomarker for GR antagonism.
Bali et al. • 2016 • J Clin Endocrinol Metab. 2016;101(11):4305-4312.
A mixed glucocorticoid/mineralocorticoid selective modulator with dominant antagonism in the male rat brain.
Atucha et al. • 2015 • Endocrinology. 2015;156(11):4105-4114.
Identification of the clinical candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): a selective Glucocorticoid Receptor (GR) antagonist.
Hunt et al. • 2017 • J Med Chem. 2017;60(8):3405-3421.
1H-pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoidreceptor antagonists with high functional activity.
Clark et al. • 2008 • Bioorg Med Chem Lett. 2008;18(4):1312-7.
Glucocorticoid receptors in the prefrontal cortex regulate dopamine efflux to stress via descending glutamatergic feedback to the ventral tegmental area.
Butts KA, Phillips AG. • 2013 • Int J Neuropsychopharmacol. 2013;16(8):1799-807.
A mixed glucocorticoid/mineralocorticoid receptor modulator dampens endocrine and hippocampal stress responsivity in male rats.
Nguyen et al. • 2017 • Physiol Behav. 2017;178:82-92.
The selective glucocorticoid receptor antagonist CORT 108297 decreases neuroendocrine stress responses and immobility in the forced swim test.
Solomon et al. • 2014 • Horm Behav. 2014;65(4):363-71.
Differential targeting of brain stress circuits with a selective glucocorticoid receptor modulator.
Zalachoras et al. • 2013 • Proc Natl Acad Sci U S A. 2013;110(19):7910-7915.
Antiglucocorticoid therapy for older adults with anxiety and co-occurring cognitive dysfunction: results from a pilot study with mifepristone.
Lenze et al. • 2014 • Int J Geriatr Psychiatry. 2014;29(9):962-9.