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. Author manuscript; available in PMC: 2021 Jan 1.
Published in final edited form as: Drug Discov Today. 2019 Sep 18;25(1):89–106. doi: 10.1016/j.drudis.2019.09.009

TABLE 2.

Glucocorticoid-receptor-modifying drugs in brain disorders

Drug Neurological effects Refs

Steroidal agonist Dexamethasone • Prevents tissue edema in meningitis cases [100,137140,142, 171,180,192]
• Reduces peritumoral edema in glioma and meningioma cases
• Inhibits apoptotic protein expression, inflammation and blood–brain barrier breakdown in eosinophilic meningitis
• Reduces meningitis-associated mortality and cerebrospinal fluid pressure
• Reduces risk of cerebral swelling during subdural grid electroencephalography
• Treats epileptic encephalopathy with continuous spike-and-wave during sleep
Methylprednisolone • Acute treatment for relapses of multiple sclerosis (MS) [145149,181,182]
• Reduces edema in brain tumors and surgical procedures
• Treats children with epileptic encephalopathy without underlying lesions
Hydrocortisone • Reduces blood–brain barrier breakdown in inflammation [183,184]
• Reduces levels of serotonin in the brain
Betamethasone • Reduces vascular density and suppresses expression of vascular endothelial growth factor [55]
• Increases pericyte coverage of neurovasculature
Nonsteroidal agonist Ginsenosides • Improve outcome in rat stroke model [153,185]
• Reduce blood–brain barrier damage in experimental autoimmune encephalitis MS model
Antagonist Mifepristone • Neuroprotection in traumatic brain injury in rats [157162,186]
• Treatment of glioma and selective induction of tumor cell death
• Improvement in mood disorders
• Improves working memory and reduces depressive symptoms in bipolar disorder
Relicorilant (CORT125134) • Treats Cushing disease and tumor pathology (Phase II/III clinical trial) [164166]
Ketoconazole • Treatment of refractory depression and major depressive disorder [187]
• Treatment of depressive symptoms in bipolar disorder
Aminogluthetimide • Protection from ischemic injury and NMDA excitotoxicity [188]
Selective antagonist LGD5552 • Prevents incidence of disease in experimental autoimmune encephalitis MS rat model [171]
CORT118335 • Reduction of stress response [163]
CORT108297 • Reduction of stress response, with delayed recovery from stress [164]
Modulator Melatonin • Reverses glucocorticoid-induced enhancement of cytotoxicity and reduction of hippocampal cell proliferation [189]
Icariin • Ameliorates disease pathology and improves clinical score in experimental autoimmune encephalitis rat model [190,191]