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.
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Entries by jeremiah@devisedesigns.com
Assessment of safety, tolerability, pharmacokinetics, and pharmacological effect of orally administered CORT125134: an adaptive, double-blind, randomized, placebo-controlled phase 1 clinical study.
Hunt et al. • 2017 • Clin Pharmacol Drug Dev. 2017 Oct 2. doi: 10.1002/cpdd.389.
FKBP5 mRNA expression is a biomarker for GR antagonism.
Bali et al. • 2016 • J Clin Endocrinol Metab. 2016;101(11):4305-4312.
Selective Glucocorticoid Receptor Modulators (SGRMs) delay castrate-resistant prostate cancer growth.
Kach et al. • 2017 • Mol Cancer Ther. 2017;16(8):1680-1692.
Selective glucocorticoid receptor antagonist CORT125281 activates brown adipose tissue and alters lipid distribution in male mice.
Kroon et al. • 2017 • Endocrinology. 2017 Sep 18. doi:10.1210/en.2017-00512.
A novel combined glucocorticoid-mineralocorticoid receptor selective modulator markedly prevents weight gain and fat mass expansion in mice fed a high-fat diet.
Mammi et al. • 2016 • Int J Obes (Lond). 2016;40(6):964-72.
Identification of a selective glucocorticoid receptor modulator that prevents both diet-induced obesity and inflammation.
van den Heuvel et al. • 2016 • Br J Pharmacol. 2016;173(11):1793-804.
Glucocorticoid antagonism limits adiposity rebound and glucose intolerance in young male rats following the cessation of daily exercise and caloric restriction.
Teich et al. • 2016 • Am J Physiol Endocrinol Metab. 2016;311(1):E56-68.
Effects of selective and non-selective glucocorticoid receptor II antagonists on rapid-onset diabetes in young rats.
Beaudry et al. • 2014 • PLoS One. 2014;9(3):e91248.
Discovery of a novel non-steroidal GR antagonist with in vivo efficacy in the olanzapine-induced weight gain model in the rat.
Hunt et al. • 2012 • Bioorg Med Chem Lett. 2012;22(24):7376-80.