A Novel Bifunctional μOR Agonist and σR Antagonist with Potent Analgesic Responses and Reduced Adverse Effects.

Bifunctional ligands possessing both μOR agonism and σR antagonism have shown promise in producing strong analgesic effects with reduced opioid-related side effects. However, the μOR agonism activity of most dual ligands diminishes compared with classical opioids, raising concern about their effectiveness in managing nociceptive pain. In this study, a new class of dual μOR agonist/σR antagonist was reported.

MiR-299-3p Inhibits Nasopharyngeal Carcinoma Cell Proliferation and Migration by Targeting MMP-2.

Purpose: Nasopharyngeal carcinoma (NPC) is a type of squamous cell carcinoma that originated from the epithelial cells of the nose and throat, and its incidence ranks the first among head and neck tumors. However, NPC has a unique and complex etiology that is not completely understood. MiR-299-3p was discovered to be abnormally expressed in cancers.

Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.

A series of novel procaine derivatives for intravenous anesthesia were prepared and evaluated by physicochemical properties and pharmacodynamic experiments in vivo and in vitro. Systematic optimization of procaine led to the identification of 6f, 6g, 6h, 6o, 6p and 6q with higher TI value and moderate log D. Compared with procaine (TI = 1.