A muscarinic acetylcholine receptor antagonist
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Tolterodine (tartrate)

Item No. 15027

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 20 mg/mlEthanol: 0.1 mg/mlPBS (pH 7.2): 1 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $95

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    25 mg

    $178

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    50 mg

    $347

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    Product Description

    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.

    References & Product Citations
    Product Description References

    1. Jones, L.H., Randall, A., Napier, C., et al. Design and synthesis of a fluorescent muscarinic antagonist. Bioorg. 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 cells. Life 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 antagonist. Eur. J. Pharmacol. 605(1-3), 145-152 (2009).