期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 59, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2022.128554
关键词
Motilin; Motilin receptor agonist; GPR38; Constipation; DS-3801
Motilin is a gastrointestinal hormone that regulates GI motility by binding to the motilin receptor GPR38 on smooth muscle cells in the GI tract. A series of N-methylanilide derivatives were identified as novel candidates for gastrointestinal prokinetic agents.
Motilin is a 22-amino-acid gastrointestinal (GI) hormone and is involved in the regulation of GI motility through binding to GPR38, the motilin receptor which is expressed on smooth muscle cells in the GI tract. Therefore, GPR38 agonists are expected to be novel gastrointestinal prokinetic agents for the treatment of functional gastrointestinal disorders such as gastroparesis and chronic constipation. We identified a series of N-methylanilide derivatives as novel non-macrolide GPR38 agonists. Among them, 12 di-L-tartrate (DS-3801b) was selected as a clinical candidate for further evaluation.
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