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Modulation of Peripheral Serotonin Levels by Novel Tryptophan Hydroxylase Inhibitors for the Potential Treatment of Functional Gastrointestinal Disorders
Journal of Medicinal Chemistry2008Vol. 51(13), pp. 3684–3687
Citations Over TimeTop 12% of 2008 papers
Zhi-Cai Shi, Arokiasamy Devasagayaraj, Kunjian Gu, Haihong Jin, Brett Marinelli, Lakshman Samala, Sheldon Scott, Terry R. Stouch, Ashok Rao Tunoori, Ying Wang, Yi Zang, Zhang Cheng-min, S. David Kimball, Alan J. Main, Weimei Sun, Qi Yang, Amr Nouraldeen, Xiang-Qing Yu, Eric C. Buxton, Shiv Patel, Nghi Nguyen, Jon Swaffield, David R. Powell, Alan Wilson, Qingyun Liu
Abstract
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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