TAK-259

TAK-259 is an orally active α1D-adrenergic receptor antagonist with a K_i value of 1.1 nM for human α1D-adrenergic receptors. TAK-259 can inhibit the contraction of isolated bladder strips in rats with bladder outlet obstruction, reduce non-voiding bladder contractions, and improve urinary frequency symptoms. TAK-259 can be used in research related to overactive bladder^[1]. In Vitro:TAK-259 (Compound 9u) (60 min) potently binds to human α₁D-adrenergic receptor in a cell membrane-free binding assay, with a K_i value of 1.1 nM^[1].
TAK-259 (10 μM; 5 min at 32°C) exhibits low inhibitory activity against hERG K⁺ channels in cell-based patch-clamp assays (16% inhibition at 10 μM)^[1]. In Vivo:TAK-259 (i.v.) reduces non-voiding bladder contractions in rats with bladder outlet obstruction in a dose-dependent manner, with an IC₃₀ of 12 nM and an ID₅₀ of 1.3 µg/kg^[1].
TAK-259 (10 µg/kg; p.o.) reduces micturition frequency in Cyclophosphamide (HY-17420)-induced cystitis rats when administered at the minimum effective dose of 10 µg/kg^[1].