Imidafenacin - CAS 170105-16-5
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Not Intended for Therapeutic Use. For research use only.
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Molecular Weight:
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).
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KRP-197; ONO-8025
1.Comparative Influence of Imidafenacin and Oxybutynin on Voiding Function in Rats with Functional Urethral Obstruction.
Fukata A1, Yamazaki T1. Drug Res (Stuttg). 2016 Mar 15. [Epub ahead of print]
An antimuscarinic therapy may increase the risk of voiding dysfunction. However, it is unclear whether the relative risk of voiding dysfunction is different among antimuscarinics. Therefore we determined the potencies both in enhancing the bladder capacity (BC), effectiveness, and in decreasing the maximum urinary flow rate (Qmax), voiding dysfunction, to compare their therapeutic indices.Under urethane anesthesia, urinary flow rate was measured at distal urethra using an ultrasonic flow meter in female Sprague-Dawley rats with functional urethral obstruction induced by a continuous i. v. infusion of α1-adrenoceptor agonist A-61603 (0.03 μg/kg/min). In a separate group of urethane-anesthetized rats without urethral obstruction, an intermittent cystometry was performed to determine BC.Intravenous imidafenacin and oxybutynin produced a significant dose-dependent decrease in Qmax with the minimum doses of 0.03 and 1 mg/kg, respectively. Imidafenacin and oxybutynin markedly increased BC, with minimum doses of 0.
2.Selective inhibitory effect of imidafenacin and 5-hydroxymethyl tolterodine on capsaicin sensitive C fibers of the primary bladder mechanosensitive afferent nerves in the rat.
Aizawa N1, Ito H1, Sugiyama R1, Fujimura T1, Suzuki M1, Fukuhara H1, Homma Y1, Igawa Y2. J Urol. 2015 Apr;193(4):1423-32. doi: 10.1016/j.juro.2014.09.005. Epub 2014 Sep 16.
PURPOSE: Imidafenacin and fesoterodine are used to treat overactive bladder. Imidafenacin, fesoterodine and its active metabolite 5-hydroxymethyl tolterodine are muscarinic receptor antagonists. It is believed that these agents act on afferent nerves in addition to smooth muscle. We investigated the effects of imidafenacin and 5-hydroxymethyl tolterodine on single unit afferent activity of mechanosensitive capsaicin sensitive and insensitive primary bladder afferent nerve fibers in rats.
3.Comparative functional selectivity of imidafenacin and propiverine, antimuscarinic agents, for the urinary bladder over colon in conscious rats.
Muraki Y1. Naunyn Schmiedebergs Arch Pharmacol. 2015 Nov;388(11):1171-8. doi: 10.1007/s00210-015-1155-9. Epub 2015 Jul 28.
Antimuscarinics are the first-line choice of treatment for overactive bladder (OAB). Imidafenacin distributes in the bladder more selectively than in the submaxillary gland and colon, and hence, this drug is considered more useful for OAB than other antimuscarinics. However, the examination of imidafenacin selectivity to bladder over colon using in vivo models is limited. Thus, the author examined whether imidafenacin could induce more selective blockade of the bladder over colon in conscious rats using two pharmacological indices (colonic transit and neostigmine-induced fecal pellet output) and compared its bladder selectivity with propiverine. In the bladder study, the inhibitory doses of antimuscarinics were calculated using the area under the curve of the distension-induced rhythmic contraction in conscious rats. The relative bladder selectivity of imidafenacin to propiverine was 50-fold and 61-fold, respectively, in a dye marker colonic transit model and in a neostigmine-induced fecal pellet output model.
4.Cognitive Safety and Overall Tolerability of Imidafenacin in Clinical Use: A Long-Term, Open-Label, Post-Marketing Surveillance Study.
Sakakibara R1, Hamano H2, Yagi H3. Low Urin Tract Symptoms. 2014 Sep;6(3):138-44. doi: 10.1111/luts.12068. Epub 2014 Jul 28.
OBJECTIVES: To assess the effect of imidafenacin on cognitive function, including the conversion rate of mild cognitive impairment (MCI) to dementia, in a period of one year.
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CAS 170105-16-5 Imidafenacin

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