Tryptophan hydroxylase (TPH) inhibitor
CAS：1137608-69-5
分子式：C36H35ClF3N7O6
分子量：754.17
纯度：98%
存储：Store at -20°C

Background:

Telotristat etiprate (LX1606 Hippurate) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.

Telotristat ethyl (15, 50, 150, 300 mg/kg, po, qd) reduces serotonin content in the periphery, but not in the brain of the mice. Telotristat ethyl (200 mg/kg po, qd) prevents the increase in blood neutrophil counts that is observed after TNBS challenge, provides significant protection in a mouse model of inflammatory bowel disease. Telotristat ethyl (200 mg/kg po, qd) protects the mouse IBD model confirmed by histopathology evaluation[1]. Telotristat ethyl (15, 50, 150, 300 mg/kg) depletes 5-HT from the jejunum but not the brain. But Telotristat ethyl (200 mg/kg, p.o.) does not deplete enteric neuronal serotonin (5-HT), or alter constitutive gastrointestinal motility in mice. Telotristat ethyl (200 mg/kg) alleviates the severity of trinitrobenzene sulfonic acid (TNBS)-induced colitis[2].?

Reference:
[1]. Tamas Oravecz, et al. LX1606 (aka LX1032), a Novel Inhibitor of Serotonin Synthesis, Alleviates Development of Inflammatory Bowel Disease in a Preclinical Model.
[2]. Margolis, K.G., et al., Pharmacological reduction of mucosal but not neuronal serotonin opposes inflammation in mouse intestine. Gut, 2013.