1246911-91-0

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] LYN H. JONES . Design and synthesis of a fluorescent muscarinic antagonist[J]. Bioorganic & Medicinal Chemistry Letters, 2008, 18 2: Pages 825-827. DOI: 10.1016/j.bmcl.2007.11.022
[2] SEIJI KOBAYASHI  Keiji M  Ken Ikeda. 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[J]. Life sciences, 2004, 74 7: Pages 843-853. DOI: 10.1016/j.lfs.2003.07.019
[3] ALEXANDER MCNAMARA . Pharmacological properties of TD-6301, a novel bladder selective muscarinic receptor antagonist[J]. European journal of pharmacology, 2009, 605 1: Pages 145-152. DOI: 10.1016/j.ejphar.2008.12.043