lubiprostone

Lubiprostone (RU-0211), an activator of ClC-2 chloride channels, is used in the therapy of idiopathic chronic constipation.

Lubiprostone (hemiketal) (RU-0211 (hemiketal)), a selective activator of the chloride channel 2 (CLCN2), facilitates the treatment of chronic idiopathic constipation and opioid-induced constipation. It functions by enhancing CLCN2 channel activity, which boosts chloride ion secretion in the intestines, subsequently increasing fluid secretion and improving intestinal peristalsis. Additionally, Lubiprostone (hemiketal) may be utilized in research related to chronic constipation and cancer.

Prostaglandin E1 (PGE1), synthesized through cyclooxygenase-mediated metabolism of dihomo-γ-linolenic acid (DGLA), functions by inhibiting platelet aggregation (IC50= 40 nM) and enhancing vasodilation. Its analog, 13,14-dihydro-16,16-difluoro PGE1, and the metabolite, 13,14-dihydro PGE1, both retain similar anti-aggregatory properties to the original compound. The inclusion of two electron-withdrawing fluorine atoms in 13,14-dihydro-16,16-difluoro PGE1 is believed to increase molecular stability and potentially extend bioavailability by resisting hydrolytic degradation.