Discovery of novel diarylamides as orally active diuretics targeting urea transporters

Urea transporters (UT) play a vital role in the mechanism of urine concentration and are recognized as novel targets for the development of salt-sparing diuretics. Thus, UT inhibitors are promising for development as novel diuretics. In the present study, a novel UT inhibitor with a diarylamide scaffold was discovered by high-throughput screening. Optimization of the inhibitor led to the identification of a promising preclinical candidate,

Novel compound FLZ alleviates rotenone-induced PD mouse model by suppressing TLR4/MyD88/NF-

Parkinson's disease (PD) is the second most common neurodegenerative disease, but none of the current treatments for PD can halt the progress of the disease due to the limited understanding of the pathogenesis. In PD development, the communication between the brain and the gastrointestinal system influenced by gut microbiota is known as microbiota-gut-brain axis. However, the explicit mechanisms of microbiota dysbiosis in PD development have not been well elucidated yet. FLZ, a novel squamosamide derivative, has been proved to be effective in many PD models and is undergoing the phase I clinical trial to treat PD in China. Moreover, our previous pharmacokinetic study revealed that gut microbiota could regulate the absorption of FLZ

Optimizing Preparation Technics of Sodium Carboxylmethylcellulose Mucilage by Orthogonal Test / 中国药房

OBJECTIVE:To study the preparation technique for CMC-Na mucilage.METHODS:The factors including kinds of solvents,the prescription dosage of CMC-Na and its adding way,the preferable prescription of and preparation for the above were inspected using orthogonal test of3factors and levels.RESULTS:The preferable technique was that2.5%CMC-Na was spreaded into the hot purified water solution under its stirring.CONCLUSIONS:The prescription and preparation for CMC-Na mucilage selected by the orthogonal test is consistent with Chinese Hospital's Preparation Standards.