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Imidafenacin

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Chemical Structure| 170105-16-5 同义名 : KRP-197;ONO-8025
CAS号 : 170105-16-5
货号 : A204562
分子式 : C20H21N3O
纯度 : 98%
分子量 : 319.4
MDL号 : MFCD09833703
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(93.93 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Imidafenacin (KRP-197) is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors (IC50=4.13 nM). 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[3]. A single oral dose of imidafenacin 0.1 mg or 0.2 mg may contribute to the improvement of pulmonary function with excellent safety and tolerability in patients with chronic obstructive pulmonary disease[4]. 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[5]. Imidafenacin is a safe drug that may improve the urodynamic parameters of patients with SCI, and it possibly alleviates bladder complications[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.13mL

0.63mL

0.31mL

15.65mL

3.13mL

1.57mL

31.31mL

6.26mL

3.13mL
参考文献

[1]Yamazaki T, Fukata A, et al. Imidafenacin exerts the antidiuretic effect by enhancing vasopressin-related responses in orally water-loaded rats. Eur J Pharmacol. 2016 Nov 15;791:72-77.

[2]Yoshida A, Kuraoka S, et al. Muscarinic receptor binding of the novel radioligand, [3h] imidafenacin in the human bladder and parotid gland. J Pharmacol Sci. 2014;124(1):40-6.

[3]Miyachi H, Kiyota H, Uchiki H, Segawa M. Synthesis and antimuscarinic activity of a series of 4-(1-Imidazolyl)-2,2-diphenylbutyramides: discovery of potent and subtype-selective antimuscarinic agents. Bioorg Med Chem. 1999 Jun;7(6):1151-61

[4]Machida K, Kawayama T, Kinoshita M, Ichinose M, Tsuda T, Takata S, Koto H, Yoshida M, Ashihara Y, Kawashima M, Suna H, Inoue H. Imidafenacin, An Orally Active Muscarinic Receptor Antagonist, Improves Pulmonary Function In Patients With Chronic Obstructive Pulmonary Disease: A Multicenter, Randomized, Double-Blind, Placebo-Controlled 3×3 Crossover Phase II Trial. Int J Chron Obstruct Pulmon Dis. 2019 Sep 19;14:2175-2184

[5]Yamazaki T, Fukata A. Imidafenacin has no influence on learning in nucleus basalis of Meynert-lesioned rats. Naunyn Schmiedebergs Arch Pharmacol. 2013 Dec;386(12):1095-102

[6]Sugiyama H, Uemura O, Mori T, Okisio N, Unai K, Liu M. Effect of imidafenacin on the urodynamic parameters of patients with indwelling bladder catheters due to spinal cord injury. Spinal Cord. 2017 Feb;55(2):187-191