Tolterodine

Tolterodine ((R)-(+)-Tolterodine) is a mAChR inhibitor and substrate for cytochrome P450 enzymes. Tolterodine competitively binds acetylcholine, reduces sympathetic excitation, and inhibits involuntary bladder muscle contraction. Tolterodine restores the Nrf2/NF-κB signaling pathway, mediates protection against inflammatory response and ferroptosis. Tolterodine ameliorates LPS (HY-D1056)-induced reactive oxygen species production and lipid oxidation. Tolterodine can be used for the research of urinary tract infections and overactive bladder^[1][2][3]. In Vitro:Tolterodine (0-500 μM; 4 h) induced a concentration-dependent reduction in viability of HepG2-CYP3A4 cells, with a TC₅₀ of 414 μM^[1].
Tolterodine (20-40 μM; 24 h, co-treated with 10 mg/L LPS) dose-dependently ameliorates LPS-induced oxidative stress in hBEC 5637 cells by reducing intracellular ROS and lipid oxidation (MDA) levels after 24 h of co-treatment with LPS^[2].
Tolterodine (20-40 μM; 24 h, co-treated with 10 mg/L LPS) dose-dependently inhibits LPS-induced production of IL-6, IL-1β, and TNF-α in hBEC 5637 cells after 24 h of co-treatment with LPS^[2].
Tolterodine (20-40 μM; 24 h, co-treated with 10 mg/L LPS) reduces LPS-induced intracellular Fe²⁺ accumulation and reverses dysregulated iron homeostasis markers (Ferritin, TFR1) in hBEC 5637 cells after 24 h of co-treatment with LPS^[2].
Tolterodine (20-40 μM; 24 h, co-treated with 10 mg/L LPS) dose-dependently attenuates LPS-induced ferroptosis in hBEC 5637 cells by normalizing ferroptosis marker levels and restoring cell viability after 24 h of co-treatment with LPS^[2].
Tolterodine (20-40 μM; 24 h, co-treated with 10 mg/L LPS) restores the Nrf2/NF-κB signaling balance in LPS-challenged hBEC 5637 cells after 24 h of co-treatment with LPS^[2]. In Vivo:Tolterodine (04-40 mg/kg; oral gavage, oral, intravenous tail vein infusion; single dose, daily for 5 days, daily for 3 months, daily for 7 days) demonstrates rapid, almost complete oral absorption, extensive metabolism with dose-dependent metabolite profiles, rapid elimination (half-life <2 h), and primarily faecal/urinary excretion in CD-1 mice, with no evidence of reduced serum levels with 3 months of repeat dosing^[3].