Darifenacin

Darifenacin (UK-88525) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin inhibits tumor growth in colorectal cancer cells and has anti-tumor effects^{[1][2][3][4][5][6]}. In Vitro:Darifenacin (0.01-100 μM; 5 min) inhibits the Kv currents in concentration-dependent manners with an IC₅₀ value of 0.34 μM and a Hill coefficient of 0.84 in coronary arterial smooth muscle cells^[2].
Darifenacin (0.01-10 μM; 1-48 h) inhibits cell viability, invasion and MMP-1 expression in colorectal cancer cells, and inhibits the phosphorylation of p38, ERK1/2 and Akt induced by muscarinic acetylcholine ^[3]. In Vivo:Darifenacin (2.5 mg/kg; Intraperitoneal injection; 42 days) has an antitumor effect in a xenograft mouse model of colorectal cancer^[3].
Darifenacin (0.1 mg/kg; Intravenous injection; Single dose) decreases the afferent activity of bladder Aδ and C fibers in female rats^[4].
Darifenacin (3 mg/kg/day; Subcutaneous osmotic pump; 14 weeks) increases the severity of liver damage caused by Azoxymethane (HY-111375)^[5].