ArticleProceedings of the National Academy of Sciences of the United States of America2013
Differential targeting of brain stress circuits with a selective glucocorticoid receptor modulator.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT05217758 (RESET-medication), which is not on this map. Cited by 55 papers, 1 of them a synthesis that pooled it.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
RESET-medication: Glucocorticoid Receptor (GR) Blockade As Diseasemodifying Treatment for Depression with Childhood Trauma
Who cites it
55 citing papers in PubMed, 1 synthesis or guideline pooled it, 117 citations in OpenAlex.
- A meta-analysis on the incidence rate of depression in Chinese menopausal women.BMC psychiatry · 2025Pooled it
- Acute Activation of Metabolic Syndrome Components in Pediatric Acute Lymphoblastic Leukemia Patients Treated with Dexamethasone.PloS one · 2016Trial
- Data mining historical Chinese medical recipe collections and nuclear receptor profiling identify plant fractions that modulate glucocorticoid receptor activity.Frontiers in pharmacology · 2025Article
- Emotional comorbidities in epilepsy result from seizure-induced corticosterone activity.Neurobiology of stress · 2024Article
- The cortisol switch between vulnerability and resilience.Molecular psychiatry · 2024Review
- Stress-induced Neuroinflammation of the Spinal Cord is Restrained by Cort113176 (Dazucorilant), A Specific Glucocorticoid Receptor Modulator.Molecular neurobiology · 2024Article
- Glucocorticoid Receptor (GR) antagonism as disease-modifying treatment for MDD with childhood trauma: protocol of the RESET-medication randomized controlled trial.BMC psychiatry · 2023Article
- Glucocorticoid Receptor and Ovarian Cancer: From Biology to Therapeutic Intervention.Biomolecules · 2023Review
- Peripheral glucocorticoid receptor antagonism by relacorilant with modest HPA axis disinhibition.The Journal of endocrinology · 2023Article
- Neuroendocrine pathogenesis of perimenopausal depression.Frontiers in psychiatry · 2023Review
- Protective effects and mechanisms of the Erzhi formula on glucocorticoid induced primary cortical neuron injury.Frontiers in pharmacology · 2023Article
- Psychological stress induces an increase in cholinergic enteric neuromuscular pathways mediated by glucocorticoid receptors.Frontiers in neuroscience · 2023Article
- Monoamine Neurotransmitters Control Basic Emotions and Affect Major Depressive Disorders.Pharmaceuticals (Basel, Switzerland) · 2022Review
- The infralimbic mineralocorticoid blockage prevents the stress-induced impairment of aversive memory extinction in rats.Translational psychiatry · 2022Article
- Mineralocorticoid receptor and glucocorticoid receptor work alone and together in cell-type-specific manner: Implications for resilience prediction and targeted therapy.Neurobiology of stress · 2022Article
- Alcohol dependence and withdrawal increase sensitivity of central amygdalar GABAergic synapses to the glucocorticoid receptor antagonist mifepristone in male rats.Neurobiology of disease · 2022Article
- Cell type specificity of glucocorticoid signaling in the adult mouse hippocampus.Journal of neuroendocrinology · 2022Article
- Stress-Related Dysfunction of Adult Hippocampal Neurogenesis-An Attempt for Understanding Resilience?International journal of molecular sciences · 2021Review
- The glucocorticoid receptor specific modulator CORT108297 reduces brain pathology following status epilepticus.Experimental neurology · 2021Article
- Glucocorticoid receptor modulators decrease alcohol self-administration in male rats.Neuropharmacology · 2021Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
15 authors at 5 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Glucocorticoid receptor (GR) antagonism may be of considerable therapeutic value in stress-related psychopathology such as depression. However, blockade of all GR-dependent processes in the brain will lead to unnecessary and even counteractive effects, such as elevated endogenous cortisol levels. Selective GR modulators are ligands that can act both as agonist and as antagonist and may be used to separate beneficial from harmful treatment effects. We have discovered that the high-affinity GR ligand C108297 is a selective modulator in the rat brain. We first demonstrate that C108297 induces a unique interaction profile between GR and its downstream effector molecules, the nuclear receptor coregulators, compared with the full agonist dexamethasone and the antagonist RU486 (mifepristone). C108297 displays partial agonistic activity for the suppression of hypothalamic corticotropin-releasing hormone (CRH) gene expression and potently enhances GR-dependent memory consolidation of training on an inhibitory avoidance task. In contrast, it lacks agonistic effects on the expression of CRH in the central amygdala and antagonizes GR-mediated reduction in hippocampal neurogenesis after chronic corticosterone exposure. Importantly, the compound does not lead to disinhibition of the hypothalamus-pituitary-adrenal axis. Thus, C108297 represents a class of ligands that has the potential to more selectively abrogate pathogenic GR-dependent processes in the brain, while retaining beneficial aspects of GR signaling.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.