Novel Gut-Restricted Bivalent Agonists Targeting Mucosal 5-HT4R: Design, Synthesis, and Biological Evaluation
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W Zhang, L Zhang, D Meng, K Zhang, Z Zhang…
European Journal of …, 2025
Elsevier
Chronic idiopathic constipation (CIC) is a prevalent gastrointestinal disorder with limited therapeutic options that balance efficacy and safety. Current therapies, such as the 5-HT 4 receptor (5-HT 4 R) agonist prucalopride, demonstrate efficacy but are often associated with systemic side effects, highlighting the need for gut-restricted alternatives. Herein, we report for the first time the rational design and synthesis of gut-restricted bivalent agonists targeting mucosal 5-HT 4 R by integrating pharmacophores of prucalopride and tenapanor. Structural …
