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rac-Tolterodine-d14 is intended for use as an internal standard for the quantification of tolterodine (Item No. 15027) 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 (carbamoylcholine; Item No. 14486) 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.
WARNING This product is not for human or veterinary use.
1. Design and synthesis of a fluorescent muscarinic antagonist. Bioorg. Med. Chem. Lett. 18(2), 825-827 (2008).
2. 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 cells. Life Sci. 74(7), 843-853 (2004).
3. Pharmacological properties of TD-