Serlipet (piboserod) / GSK, Serodus - LARVOL DELTA

Discovery, Biological Evaluation and Binding Mode Investigation of Novel Butyrylcholinesterase Inhibitors Through Hybrid Virtual Screening. (PubMed, Molecules) - "Among them, piboserod and Rotigotine demonstrated the best BChE inhibitory potency (IC50 = 15.33 μM and 12.76 μM, respectively) and exhibited favorable safety profiles as well as neuroprotective effects in vitro...Fluorescence spectroscopy, molecular docking, and molecular dynamics simulations further clarified their binding modes and stability. This study provides an innovative screening strategy for the discovery of BChE inhibitors, which not only identifies promising drug candidates for the treatment of AD but also demonstrates the potential of machine learning in drug discovery."

Journal • Preclinical • Alzheimer's Disease • CNS Disorders

The effect of ginger extract on cisplatin-induced acute anorexia in rats. (PubMed, Front Pharmacol) - "Furthermore, the injection of 5-HT and receptors antagonists (palonostron, 0.1 mg/kg, i.p.; piboserod, 1 mg/kg, i.p., respectively) in cisplatin treated rats prevented the decrease in food intake. Although [6]-gingerol or [6]-shogaol alone failed to alleviate the evoked anorexia, when treated together, the effect was significant on the cisplatin-induced decrease in food intake. These results show that GE can be considered a treatment option to alleviate cisplatin-induced anorexia."

Journal • Preclinical • Anorexia • Oncology

Differential contribution of 5-HT, 5-HT, and 5-HT receptors to acute pruriceptive processing induced by chloroquine and histamine in mice. (PubMed, Biol Pharm Bull) - "In the present study, scratching behavior induced by chloroquine (CQ) was ameliorated by milnacipran or mirtazapine, and these effects were reversed by SB207266, a 5-HT antagonist, or SB258585, a 5-HT antagonist, but not by SB258585, a 5-HT antagonist. Similarly, the amelioration of histamine-induced scratches by these antidepressants was not reversed by the 5-HT, 5-HT, or 5-HT receptor antagonist. Therefore, 5-HT is involved in the amelioration of CQ-induced scratches by milnacipran and mirtazapine, and 5-HT, 5-HT, and 5-HT receptors play differential roles in acute pruriceptive processing after administration of CQ or histamine."

Journal • Preclinical • Dermatology • Pruritus

Serotonin Exhibits an Inhibitory Effect on NETosis (ISTH 2023) - "In qualitative and quantitative approaches, serotonin showed a significant, dose-dependent inhibitory effect on PMA-induced NETosis (2h, n=5, 100 μM P< 0.0001, 10 μM P< 0.05, 1 μM P=0.18). This was reproducible despite longer coincubation periods (n=5, 100 µM, 3h P< 0.001, 4h P< 0.01). Furthermore, serotonin's inhibitory effect was significantly blocked by preincubation with SB-269970 hydrochloride (n=5, 100 µM, 3h P< 0.05) but not with piboserod (P=0.26)."

CEACAM8 • ITGAM • MPO

5-Hydroxytryptamine: a potential therapeutic target in amyotrophic lateral sclerosis. (PubMed, Neural Regen Res) - "This involved intraperitoneal injections of either granisetron, piboserod, or ritanserin, which inhibit the 5-HT3, 5-HT4, and 5-HT2 receptors, respectively...These results indicate that 5-HT deficiency may play a role in the pathogenesis of amyotrophic lateral sclerosis by inducing the abnormal expression and/or distribution of TDP-43 and SOD1-G93A and by activating glial cells. 5-HT could therefore be a potential therapeutic target for amyotrophic lateral sclerosis."

Journal • Amyotrophic Lateral Sclerosis • CNS Disorders • SOD1 • TARDBP