ONO-2952 / Ono Pharmaceutical - LARVOL DELTA

The translocator protein antagonist ONO-2952 attenuates neuroinflammation and neuronal apoptosis in an epilepsy rat model. (PubMed, Front Neurol) - "The results showed that ONO-2952 could down-regulate the expression of translocator protein 18 kDa, reduce the level of proinflammatory cytokines and peripheral immune cell infiltration, thereby inhibiting neuroinflammation in epileptic rats, and it could also relieve hippocampal neuronal apoptosis and effectively improve the cognitive dysfunction of model rats. This study confirms that ONO-2952 can regulate the expression of translocator protein 18 kDa, inhibit neuroinflammation and neuronal apoptosis, and improve cognitive function in epileptic rats, and further research is required to fully elucidate its specific biological effects."

Journal • Preclinical • CNS Disorders • Cognitive Disorders • Epilepsy • Inflammation

Tryptophan Metabolism-Related Biomarkers in Acute Myocardial Infarction Identified by Machine Learning. (PubMed, J Vis Exp) - "Molecular docking and molecular dynamics simulations demonstrated a stable interaction between TSPO and ONO-2952. Furthermore, single-cell and SCENIC analyses identified monocytes as key cell populations and TFEC and CEBPD as potential transcriptional regulators of key gene expression. Collectively, this study provides a comprehensive characterization of TrM-related molecular alterations in AMI and identifies ADM, MCEMP1, and TSPO as potential diagnostic key genes, offering new insights into disease mechanisms and candidate targets for future therapeutic investigation."

Biomarker • Journal • Cardiovascular • Myocardial Infarction

Pharmacological and Genetic Inhibition of Translocator Protein 18 kDa Ameliorated Neuroinflammation in Murine Endotoxemia Model. (PubMed, Shock) - "Interestingly, pretreatment with the TSPO antagonist, ONO-2952, or germ-line deletion of the TSPO gene exhibited an anti-inflammatory effect with significant suppression of LPS-induced production of those cytokines...Collectively, these results suggest that TSPO plays a critical role in the SAE mouse model. Based on this finding, monitoring TSPO activity, as well as the progress of endotoxemia and its sequelae in the animal model, would deepen our understanding of the underlying molecular mechanism of SAE."

Journal • CNS Disorders • Immunology • Infectious Disease • Inflammation • Septic Shock • IL1B • PCR • TNFA

Antidepressant effect of the translocator protein antagonist ONO-2952 on mouse behaviors under chronic social defeat stress. (PubMed, Neuropharmacology) - "Treating animals with ONO-2952 during chronic social defeat stress ameliorated impairments in social avoidance and anxiety-like behaviors and suppressed pro-inflammatory cytokine production, suggesting that ONO-2952 exerted an anti-stress effect in this animal model of depression. Thus, targeting TSPO as a candidate for the development of antidepressants that reduce susceptibility to chronic stress could pave the way toward therapeutic interventions for relapse prophylaxis in depression."

Biomarker • Journal • Preclinical

Translocator protein 18kDa antagonist ameliorates stress-induced stool abnormality and abdominal pain in rodent stress models. (PubMed, Neurogastroenterol Motil) - "On the other hand, ONO-2952 did not affect spontaneous defecation, gastrointestinal transit, visceral nociceptive threshold, and neurosteroid production in non-stressed rats even at a dose 10 times higher than its effective dose in the stress models. These results suggest that TSPO antagonism results in antistress action, and that ONO-2952 is a promising candidate for IBS without side effects associated with current treatment."

Journal • Preclinical