rac-Tolterodine-d14 is intended for use as an internal standard for the quantification of tolterodine by GC- or LC-MS. Tolterodine is an antagonist of muscarinic acetylcholine receptors (Kis = 1.4, 2.7, 3.6, 3.1, and 2.2 nM for M1-5 receptors, respectively).1 It reduces intracellular calcium mobilization induced by carbachol in bladder smooth muscle cells and submandibular gland cells isolated from cynomolgus monkeys (Kis = 3.16 and 2 nM, respectively).2 Tolterodine inhibits volume-induced bladder contractions and oxotremorine-induced salivation in rats (ID50s = 0.025 and 0.12 mg/kg, respectively).3 Formulations containing tolterodine have been used in the treatment of overactive bladder.
1.Jones, L.H., Randall, A., Napier, C., et al.Design and synthesis of a fluorescent muscarinic antagonistBioorg. Med. Chem. Lett.18(2)825-827(2008) 2.Kobayashi, S., Ikeda, K., and Miyata, K.Comparison of in vitro selectivity profiles of solifenacin succinate (YM905) and current antimuscarinic drugs in bladder and salivary glands: A Ca2+ mobilization study in monkey cellsLife Sci.74(7)843-853(2004) 3.McNamara, A., Pulido-Rios, M.T., Sweazey, S., et al.Pharmacological properties of TD-6301, a novel bladder selective muscarinic receptor antagonistEur. J. Pharmacol.605(1-3)145-152(2009)