ArticleCell communication and signaling : CCS2013
The 1,4-benzodiazepine Ro5-4864 (4-chlorodiazepam) suppresses multiple pro-inflammatory mast cell effector functions.
Article in Cell communication and signaling : CCS, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 25 citations in OpenAlex.
- Ro5-4864, a ligand of the mitochondrial translocator protein, protects against heart failure in mice via regulation of the p62-Keap1-Nrf2 axis.The Journal of physiology · 2026Article
- In vitro γ-aminobutyric acid A (GABACommunications chemistry · 2026Article
- Integrated Transcriptomic Analyses and Experimental Validation Identify TSPO as a Mitochondria-Associated Therapeutic Target in Myocarditis.Mediators of inflammation · 2026Article
- Prevalence and treatment response of neuropsychiatric disorders in mast cell activation syndrome.Brain, behavior, & immunity - health · 2025Article
- CD3ζ-Mediated Signaling Protects Retinal Ganglion Cells in Glutamate Excitotoxicity of the Retina.Cells · 2024Article
- Longitudinal cytokine and multi-modal health data of an extremely severe ME/CFS patient with HSD reveals insights into immunopathology, and disease severity.Frontiers in immunology · 2024Article
- Article
- Mitochondrial translocator protein deficiency exacerbates pathology in acute experimental ulcerative colitis.Frontiers in physiology · 2022Article
- Article
- Benzodiazepines: Drugs with Chemical Skeletons Suitable for the Preparation of Metallacycles with Potential Pharmacological Activity.Molecules (Basel, Switzerland) · 2021Review
- A comprehensive review of remimazolam for sedation.Health psychology research · 2021Review
- [Surgical interventions in patients with systemic mast cell activation disease : Recommendations for perioperative management].Der Chirurg; Zeitschrift fur alle Gebiete der operativen Medizen · 2019Review
- Quantitative Systems Pharmacological Analysis of Drugs of Abuse Reveals the Pleiotropy of Their Targets and the Effector Role of mTORC1.Frontiers in pharmacology · 2019Article
- 4'-Chlorodiazepam Protects Mitochondria in T98G Astrocyte Cell Line from Glucose Deprivation.Neurotoxicity research · 2017Article
- Characterization of Mast Cell Activation Syndrome.The American journal of the medical sciences · 2017Article
- Memory and hippocampal architecture following short-term midazolam in western diet-treated rats.Neuroscience letters · 2016Article
- GABAergic modulation with classical benzodiazepines prevent stress-induced neuro-immune dysregulation and behavioral alterations.Brain, behavior, and immunity · 2016Article
- [Surgical interventions in patients with mast cell activation disease. Aspects relevant for surgery using the example of a cholecystectomy].Der Chirurg; Zeitschrift fur alle Gebiete der operativen Medizen · 2014Review
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Activation of mast cells (MCs) can be achieved by the high-affinity receptor for IgE (FcεRI) as well as by additional receptors such as the lipopolysaccharide (LPS) receptor and the receptor tyrosine kinase Kit (stem cell factor [SCF] receptor). Thus, pharmacological interventions which stabilize MCs in response to different receptors would be preferable in diseases with pathological systemic MC activation such as systemic mastocytosis. 1,4-Benzodiazepines (BDZs) have been reported to suppress MC effector functions. In the present study, our aim was to analyze molecularly the effects of BDZs on MC activation by comparison of the effects of the two BDZs Ro5-4864 and clonazepam, which markedly differ in their affinities for the archetypical BDZ recognition sites, i.e., the GABAA receptor and TSPO (previously termed peripheral-type BDZ receptor). Ro5-4864 is a selective agonist at TSPO, whereas clonazepam is a selective agonist at the GABAA receptor. Ro5-4864 suppressed pro-inflammatory MC effector functions in response to antigen (Ag) (degranulation/cytokine production) and LPS and SCF (cytokine production), whereas clonazepam was inactive. Signaling pathway analyses revealed inhibitory effects of Ro5-4864 on Ag-triggered production of reactive oxygen species, calcium mobilization and activation of different downstream kinases. The initial activation of Src family kinases was attenuated by Ro5-4864 offering a molecular explanation for the observed impacts on various downstream signaling elements. In conclusion, BDZs structurally related to Ro5-4864 might serve as multifunctional MC stabilizers without the sedative effect of GABAA receptor-interacting BDZs.
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Registered trials
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