Imidafenacin

Imidafenacin (KRP-197; ONO-8025) is an orally active inhibitor of muscarinic (mAChR) M₁ and M₃ receptors. Imidafenacin potently inhibits bladder contraction in vivo and exerts an antidiuretic effect by enhancing the signaling pathway of vasopressin (antidiuretic hormone). Imidafenacin can be used in research related to overactive bladder^[1][2]. In Vivo:Imidafenacin (3-300 μg/kg; i.v.; single dose) dose-dependently suppresses urine production in orally water-loaded female Sprague-Dawley rats, with a maximum 50% inhibition of vehicle group urine volume at 100 μg/kg, and exerts its antidiuretic effect by enhancing components of the vasopressin signaling pathway^[1].
Imidafenacin (0.05-0.2 mg/kg; p.o.; single dose) dose-dependently prevents carbamylcholine-induced reductions in bladder capacity in conscious female rats with an ID₅₀ of 0.055 mg/kg, and significantly lowers maximum intravesical pressure at doses of 0.05, 0.1, and 0.2 mg/kg^[2].
Imidafenacin (0.0625-1 mg/kg; p.o.; singe dose) dose-dependently inhibits distention-induced rhythmic bladder contractions in conscious male rats with an ID₃₀ of 0.17 mg/kg, with effects peaking 30-50 minutes post-dosing and lasting at least 120 minutes^[2].
Imidafenacin (0.3-2.4 mg/kg; p.o.; single dose) dose-dependently inhibits carbamylcholine-induced salivary secretion in conscious male rats with an ID₅₀ of 1.5 mg/kg^[2].
Imidafenacin (1-10 mg/kg; p.o.; daily; 7 days) does not impair spatial learning or memory in male rats tested in the Morris water maze task^[2].