Description: Lubiprostone (RU-0211), an activator of ClC-2 chloride channels, is used in the therapy of idiopathic chronic constipation. Target: Chloride channel. Smiles: CCCCC(F)(F)C(=O)CC[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(O)=O. References: Bijvelds MJ, et al. Gastroenterology, 2009, 137(3), 976-1985.

Lubiprostone is an activator of chloride channel protein 2 (ClC-2) and a bicyclic derivative of prostaglandin E1 (PGE1, Cay-13010). It induces chloride currents in HEK293 cells expressing recombinant human ClC-2 (EC50 = ~17 nM), but not CFTR, chloride channels. Lubiprostone (1 µM) induces short-circuit currents, a...