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. 2022 Mar 1:59:128554.
doi: 10.1016/j.bmcl.2022.128554. Epub 2022 Jan 18.

Discovery of DS-3801b, a non-macrolide GPR38 agonist with N-methylanilide structure

Narihiro Toda  1 , Takeshi Shida  2 , Rieko Takano  2 , Takahiro Katagiri  2 , Masakazu Hirouchi  2 , Manabu Abe  2 , Kaori Soma  2 , Yasuhiro Nakagami  2 , Mami Yamazaki  2
Affiliations

Discovery of DS-3801b, a non-macrolide GPR38 agonist with N-methylanilide structure

Narihiro Toda et al. Bioorg Med Chem Lett. .

Abstract

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.

Keywords: Constipation; DS-3801; GPR38; Motilin; Motilin receptor agonist.

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