Substituted 3-(4-(1,3,5-triazin-2-yl)-phenyl)-2-aminopropanoic acids as novel tryptophan hydroxylase inhibitors |
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Authors: | Haihong Jin Giovanni Cianchetta Arokiasamy Devasagayaraj Kunjian Gu Brett Marinelli Lakshman Samala Sheldon Scott Terry Stouch Ashok Tunoori Ying Wang Yi Zang Chengmin Zhang S. David Kimball Alan J. Main Zhi-Ming Ding Weimei Sun Qi Yang Xiang-Qing Yu David R. Powell Alan Wilson Zhi-Cai Shi |
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Affiliation: | 1. Lexicon Pharmaceuticals, 350 Carter Road, Princeton, NJ 08540, United States;2. Lexicon Pharmaceuticals, 8800 Technology Forest Place, The Woodlands, TX 77381, United States |
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Abstract: | Tryptophan hydroxylase (TPH) is a key enzyme in the synthesis of serotonin. As a neurotransmitter, serotonin plays important physiological roles both peripherally and centrally. Here we describe the discovery of substituted triazines as a novel class of tryptophan hydroxylase inhibitors. This class of TPH inhibitors can selectively reduce serotonin levels in murine intestine after oral administration without affecting levels in the brain. These TPH 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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