| Literature DB >> 18557609 |
Zhi-Cai Shi1, Arokiasamy Devasagayaraj, Kunjian Gu, Haihong Jin, Brett Marinelli, Lakshman Samala, Sheldon Scott, Terry Stouch, Ashok Tunoori, Ying Wang, Yi Zang, Chengmin Zhang, S David Kimball, Alan J Main, Weimei Sun, Qi Yang, Amr Nouraldeen, Xiang-Qing Yu, Eric 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.Entities:
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Year: 2008 PMID： 18557609 DOI： 10.1021/jm800338j
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446