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CAS No. : 170105-16-5
Biological Activity：Imidafenacin(KRP-197; ONO-8025) is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM).
IC50 value: 0.3 nM(M3) 
in vitro: KRP-197 showed equipotent anti-M2 and anti-M3 activity and decreased subtype-selectivity .
in vivo: Intraduodenal administration of
KRP-197 (0.04±0.30 mg/kg) inhibited bladder contraction dose-dependently, and the ED30 value was 0.11 mg/kg. The inhibitory action of KRP-197 on the bladder contraction was 19 times as potent as that of oxybutynin. KRP-197 showed preventive action against
the decrease in bladder capacity induced by carbachol
(ED50 0.074 mg/kg, intragastric administration), and
the potency of the inhibitory action was 15-fold greater
than that of oxybutynin . The learning-inhibitory doses of intravenous oxybutynin hydrochloride and tolterodine tartrate were 0.3 and 3 mg/kg in sham-operated rats and 0.1 and 1 mg/kg in nbM-lesioned rats, respectively. Thus, the learning impairments by those antimuscarinics were more sensitive in nbM-lesioned rats than in sham-operated rats. On the other hand, intravenous administration of imidafenacin had no influence on learning in either case of the rats. In normal rats, however, intracerebroventricular administration of imidafenacin impaired learning to the same degree as that of oxybutynin hydrochloride .
Research Area：Neurological Disease
Related Screening Libraries:Drug Repurposing Compound Library Plus;FDA-Approved Drug Library Plus;FDA-Approved Drug Library Mini;Bioactive Compound Library Plus;GPCR/G Protein Compound Library;Neuronal Signaling Compound Library;FDA-Approved Drug Library;Drug Repurposing Compound Library;Anti-COVID-19 Compound Library;Neurotransmitter Receptor Compound Library;FDA Approved & Pharmacopeial Drug Library;Anti-Parkinson’s Disease Compound Library;Neurodegenerative Disease-related Compound Library;Human Metabolite Library;
Related Small Molecules:VU0357017 hydrochloride;TBPB;Sabcomeline;MK-6884;Brompheniramine-d6 maleate;Navafenterol saccharinate;DREADD agonist 21;Cyclobuxine D;Brompheniramine maleate;Dexetimide;Anisodamine hydrobromide;Anisotropine bromide;PD 102807;Nebracetam hydrochloride;Muscarine-d9 iodide;Mazaticol;VU0455691;Arborine;Oxitropium Bromide;Propiverine hydrochloride;VU0152099;MHP 133;YM-58790;Elucaine;Rispenzepine;Phenglutarimid;Rapacuronium bromide;Ambutonium bromide;Temiverine hydrochloride;Procyclidine;M4 mAChR agonist-1;Camylofine
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