LX1606 is an orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.
体内研究
Telotristat ethyl (15, 50, 150, 300 mg/kg, po, qd) lowers serotonin levels in the peripheral tissues without affecting brain serotonin in mice. At a dosage of 200 mg/kg once daily, it blocks the rise in blood neutrophil counts triggered by TNBS, offering considerable protection in a mouse model of inflammatory bowel disease. This protective effect of Telotristat ethyl at 200 mg/kg daily in the IBD mouse model is verified through histopathological assessment[1].
Telotristat ethyl (15, 50, 150, 300 mg/kg) depletes serotonin (5-HT) in the jejunum but not the brain. And Telotristat ethyl (200 mg/kg, Po.). does not deplete intestinal neuronal serotonin and does not alter structural gastrointestinal motility in mice. Tiratriptan ethyl (200 mg/kg) attenuates the severity of trinitrobenzene sulfonic acid (TNBS)-induced colitis[2].
Telotristat ethyl 细胞实验
Cell Line
Concentration
Treated Time
Description
References
BON-1 cells
1 µM
2 hours
Inhibited TPH activity, preventing propionate and butyrate-induced increases in 5-HT and melatonin levels
Nutrients. 2021 Dec 28;14(1):117
Telotristat ethyl 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
NOD/SCID mice
Peritoneal dissemination xenograft model
Oral
100 mg/kg
5 days per week for 2 weeks
Evaluate the survival benefits of Telotristat ethyl in a peritoneal dissemination xenograft model. Results showed that TE alone slightly increased animal survival (52 days), and combination with chemotherapy significantly improved survival rates.
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