Tarafenacin (D-tartrate)

Tarafenacin (SVT-40776) (D-tartrate) is an orally active, selective M3 muscarinic receptor (M3 muscarinic receptor) antagonist with 203-fold selectivity over the M2 muscarinic receptor. Tarafenacin (D-tartrate) does not affect atrial contraction, arterial blood pressure or arterial pressure at high doses. Tarafenacin (D-tartrate) can be used in the research of overactive bladder^[1][2][3]. In Vitro:Tarafenacin (D-tartrate) (3-1000 nmol/L; 60 min) potently inhibits carbachol-induced contractions in mouse isolated urinary bladder detrusor smooth muscle^[1].
Tarafenacin (D-tartrate) (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 (D-tartrate) (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 (D-tartrate) (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].