Tolterodine (tartrate)

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). It reduces intracellular calcium mobilization induced by carbachol (carbamoylcholine, Cay-14486) in bladder smooth muscle cells and submandibular gland cells isolated from cynomolgus monkeys (Kis = 3.16 and 2 nM, respectively). Tolterodine inhibits volume-induced bladder contractions and oxotremorine-induced salivation in rats (ID50s = 0.025 and 0.12 mg/kg, respectively). Formulations containing tolterodine have been used in the treatment of overactive bladder.Formal Name: 2-[(1R)-3-[bis(1-methylethyl)amino]-1-phenylpropyl]-4-methyl-phenol, 2R,3R-dihydroxybutanedioate. CAS Number: 124937-52-6. Synonyms: PNU 200583E. Molecular Formula: C22H31NO . C4H6O6. Formula Weight: 475.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 20 mg/ml, Ethanol: 0.1 mg/ml, PBS (pH 7.2): 1 mg/ml. lambdamax: 284 nm. SMILES: OC1=C([C@@H](C2=CC=CC=C2)CCN(C(C)C)C(C)C)C=C(C)C=C1.O[C@H]([C@@H](O)C(O)=O)C(O)=O. InChi Code: InChI=1S/C22H31NO.C4H6O6/c1-16(2)23(17(3)4)14-13-20(19-9-7-6-8-10-19)21-15-18(5)11-12-22(21)24,5-1(3(7)8)2(6)4(9)10/h6-12,15-17,20,24H,13-14H2,1-5H3,1-2,5-6H,(H,7,8)(H,9,10)/t20-,/m1./s1. InChi Key: TWHNMSJGYKMTRB-VEIFNGETSA-N.