etazolate (SQ-20009) / Eurobio Scientific - LARVOL DELTA

Phosphodiesterase 4 regulates pyroptosis in subarachnoid hemorrhage. (PubMed, Neural Regen Res) - "A phosphodiesterase 4-specific inhibitor, etazolate, was intraperitoneally injected 30 minutes after subarachnoid hemorrhage induction...Together, the results indicate that phosphodiesterase 4 regulates NLRP3-mediated neuronal pyroptosis in early brain injury after subarachnoid hemorrhage. Phosphodiesterase 4 may be a potential therapeutic molecular target for subarachnoid hemorrhage."

Journal • CNS Disorders • Hematological Disorders • Inflammation • Metabolic Disorders • Subarachnoid Hemorrhage • Vascular Neurology • NLRC5 • NLRP3

Clerodane Diterpenes from Casearia corymbosa as Allosteric GABA Receptor Modulators. (PubMed, J Nat Prod) - "To explore possible binding sites at the receptor, the most abundant diterpenoid 8 was tested in combination with diazepam, etazolate, and allopregnanolone. Compound 8 potentiated GABA-induced currents with both receptor subunit compositions [EC (αβγS) = 43.6 μM; E = 809% and EC (αβ) = 57.6 μM; E = 534%]. The positive modulation of GABA-induced currents was not inhibited by flumazenil, thereby confirming an allosteric modulation independent of the benzodiazepine binding site."

Journal • Review

Antiallodynic action of phosphodiesterase inhibitors in a mouse model of peripheral nerve injury. (PubMed, Neuropharmacology) - "Mechanical hypersensitivity, evaluated using von Frey filaments, was relieved by sustained treatment with the non-selective PDEi theophylline and ibudilast (AV-411), with PDE4i rolipram, etazolate and YM-976, and with PDE5i sildenafil, zaprinast and MY-5445, but not by treatments with PDE1i vinpocetine, PDE2i EHNA or PDE3i milrinone. Rolipram had anti-neuroimmune action, as shown by its impact on levels of the pro-inflammatory cytokine tumor necrosis factor-α (TNFα) in the dorsal root ganglia of mice with peripheral nerve injury, as well as in human peripheral blood mononuclear cells (PBMCs) stimulated with lipopolysaccharides. This study suggests that PDEs, especially PDE4 and 5, may be targets of interest in the treatment of neuropathic pain."

Journal • Preclinical • Immunology • Neuralgia • Oncology • Pain • TNFA

Diagnostic accuracy of the BJI InoPlex™ (Diaxonhit) immunoassay on blood samples for periprosthetic joint infection in complex microbiological situations. Preliminary results of 24 cases in a French Reference Center for Complex Bone and Joint Infection (CRIOAC). (PubMed, Orthop Traumatol Surg Res) - "While innovative, minimally invasive, and rapid (results in a few hours), the BJI InoPlex does not provide an effective diagnosis of chronic PJI in complex microbiological situations. In this study, we used the test in the most difficult situations possible and on a small number of patients, which may explain why the results were not as good as in other studies. Its current performance and cost mean there is no role for it in our algorithm for treating patients with a suspected PJI, contrary to other biomarkers. Its spectrum must include other bacterial strains involved in chronic PJI. Knowledge of the specific infectious agent increases its diagnostic value, it could be used to monitor the outcome of a PJI, although other studies would be needed to support this use."

Clinical • Journal • Musculoskeletal Diseases • Orthopedics

Effect of etazolate upon cuprizone induced demyelination in vivo: Behavioral and myelin gene analysis. (PubMed, Neuroscience) - "Altogether, this study shows that the beneficial effect of etazolate upon demyelination does not occur at the gene expression level. Furthermore, our results also highlight the difficulty in revealing functional sequelae following cuprizone intoxication."

Journal • CNS Disorders • Immunology • Inflammation • Multiple Sclerosis

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Cardiovascular

Evaluation of Modulators of cAMP-Response in Terms of Their Impact on Cell Cycle and Mitochondrial Activity of Leishmania donovani. (PubMed, Front Pharmacol) - "Treatment of etazolate at subcytotoxic concentration to infected macrophages significantly reduced parasite burden, and administration of etazolate to Leishmania-infected BALB/c mice showed reduced liver and spleen parasite burden. Collectively, these results imply involvement of cAMP in various crucial processes paving the avenue for developing potent antileishmanial agent."

Journal

Molecular Targets for the Interactive Effect of Etazolate during Post-Traumatic Stress Disorder: Role of Oxidative Stress, BDNF and Histones. (PubMed, Behav Brain Res) - "Etazolate treatment, on the other hand, led to prevention of changes in these oxidative stress biomarkers (GSH, GSSG, GPx and TBARS), BDNF levels, and histones acetylation. In conclusion, oxidative stress and modulation of BDNF and histones acetylation induced by PTSD can be prevented by treatment with etazolate."

Biomarker • Journal • Alzheimer's Disease • CNS Disorders • Depression • Mood Disorders • Post-traumatic Stress Disorder

A novel model of trauma-induced cerebellar injury and myelin loss in mouse organotypic cerebellar slice cultures using live imaging. (PubMed, J Neurosci Methods) - "Etazolate, a known protective compound, was able to reduce both the PI-fluorescence increase and the loss of GFP-fluorescence, emphasizing its protective effect on myelin loss. In line with the existing models of focal injury, we characterized trauma-induced cerebellar lesion with an increase of PI fluorescence by live imaging. Our findings describe a novel tool to study trauma-induced myelin damage in cerebellar slices and to test biomolecules of therapeutic interest for myelin protection."

Journal • Preclinical