Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 51, Issue 13, Pages 3684-3687Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm800338j
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The discovery of a novel class of peripheral tryptophan hydroxylase (TPH) inhibitors is described. This class of TPH inhibitors exhibits excellent potency in in vitro biochemical and cell-based assays, and it selectively reduces serotonin levels in the murine intestine after oral administration without affecting levels in the brain. These TPH1 inhibitors may provide novel treatments for gastrointestinal disorders associated with dysregulation of the serotonergic system, such as chemotherapy-induced emesis and irritable bowel syndrome.
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