Drofenine (hydrochloride)

Drofenine is an antagonist of M1 muscarinic acetylcholine receptors (mAChRs). It inhibits carbachol-induced inositol phosphate accumulation in isolated guinea pig cortical slices, which endogenously express M1 muscarinic receptors (pA2 = 8.15). Drofenine also inhibits butyrylcholinesterase (BChE) isolated from human serum (Ki = 3 µM). It induces inward currents in whole-cell patch-clamp assays using HEK293 cells overexpressing transient receptor potential vanilloid 3 (TRPV3, EC50 = 205 µM). Drofenine (5 mg/kg twice per week) increases hepatic levels of alpha-smooth muscle actin (alpha-Sma) and collagen I in a mouse model of hepatic fibrosis induced by carbon tetrachloride (CCl4).. Solulibility: DMSO: Soluble: =10 mg/ml: Ethanol: Soluble: =10 mg/ml.