Propiverine is an antagonist of muscarinic acetylcholine receptors (mAChRs).1 It binds to M1 and M2 mAChRs in rat bladder and submaxillary gland, respectively (Kis = 0.3 and 0.19 ?M, respectively), and inhibits carbachol-induced contraction of bladder strips isolated from patients with normal bladder activity and detrusor overactivity associated with benign prostatic hyperplasia (pA2s = 7.7 and 7.6, respectively).2 Formulations containing propiverine have been used in the treatment of overactive bladder.
1.Yamada, S., Ito, Y., Taki, Y., et al.The N-oxide metabolite contributes to bladder selectivity resulting from oral propiverine: Muscarinic receptor binding and pharmacokineticsDrug Metab. Dispos.38(8)1314-1321(2010) 2.Yamanishi, T., Kaga, K., Fuse, M., et al.The role of muscarinic receptor subtypes on carbachol-induced contraction of normal human detrusor and overactive detrusor associated with benign prostatic hyperplasiaJ. Pharmacol. Sci.128(2)65-70(2015)