Tarafenacin

Tarafenacin (SVT-40776) is an orally active, selective M3 muscarinic receptor (M3 muscarinic receptor) antagonist with 203-fold selectivity over the M2 muscarinic receptor. Tarafenacin does not affect atrial contraction, arterial blood pressure or arterial pressure at high doses. Tarafenacin can be used in the research of overactive bladder^[1][2][3]. In Vitro:Tarafenacin (3-1000 nmol/L; 60 min) potently inhibits carbachol-induced contractions in mouse isolated urinary bladder detrusor smooth muscle^[1].
Tarafenacin (0.1-10 μmol/L; 60 min) inhibits Carbachol (HY-B1208)-induced negative chronotropism in mouse isolated atrial tissue, exhibiting a 199-fold functional selectivity for mouse urinary bladder over atrial tissue^[1].
Tarafenacin (20 min) potently inhibits Carbachol-induced inositol phosphate accumulation in mouse bladder smooth muscle with a K_i of 0.19 nM, and shows 23-fold greater selectivity over mouse salivary glands^[2]. In Vivo:Tarafenacin (1-3000 nmol/kg (log dose); i.v.; cumulative bolus; 15 min between doses) potently inhibits spontaneous guinea pig bladder contractions with an ED₂₅ of 6.97 mg/kg, and exhibits greater than 175-fold bladder versus vascular selectivity, with no observed effects on arterial blood pressure^[1].