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Darifenacin hydrobromide

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Chemical Structure| 133099-07-7 同义名 : UK-88525 hydrobromide;Darifenacin (hydrobromide);UK 88525-04;UK-88525;Darifenacin HBr
CAS号 : 133099-07-7
货号 : A211196
分子式 : C28H31BrN2O2
纯度 : 98%
分子量 : 507.462
MDL号 : -
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(68.97 mM)，配合低频超声助溶，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
靶点

  • mAChR

    M3 mAChR, pKi:8.9
描述 Darifenacin hydrobromide is a selective M3 muscarinic receptor antagonist with pKi of 8.5[3]. Concentration-dependent increases in ATPase activity was observed in P-gp (P-glycoprotein) membranes following darifenacin exposure (0-10 µM) with an estimated ED50 value of 1.6 μM[4]. Darifenacin (0.1 mg/kg i.v.) reduces bladder afferent activity in both Aδ and C fibers in female Sprague-Dawley rats, the decrease in afferent spikes in C fibers may be more pronounced than that in Aδ fibers[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.97mL

0.39mL

0.20mL

9.85mL

1.97mL

0.99mL

19.71mL

3.94mL

1.97mL
参考文献

[1]Miller DW, Hinton M, Chen F. Evaluation of drug efflux transporter liabilities of darifenacin in cell culture models of the blood-brain and blood-ocular barriers. Neurourol Urodyn. 2011 Nov;30(8):1633-8.

[2]Hegde SS, Choppin A, et al. Functional role of M2 and M3 muscarinic receptors in the urinary bladder of rats in vitro and in vivo. Br J Pharmacol. 1997 Apr;120(8):1409-18.

[3]Hegde SS, Choppin A, Bonhaus D, Briaud S, Loeb M, Moy TM, Loury D, Eglen RM. Functional role of M2 and M3 muscarinic receptors in the urinary bladder of rats in vitro and in vivo. Br J Pharmacol. 1997 Apr;120(8):1409-18.

[4]Miller DW, Hinton M, Chen F. Evaluation of drug efflux transporter liabilities of darifenacin in cell culture models of the blood-brain and blood-ocular barriers. Neurourol Urodyn. 2011 Nov;30(8):1633-8.

[5]Iijima K, De Wachter S, Wyndaele JJ. Effects of the M3 receptor selective muscarinic antagonist darifenacin on bladder afferent activity of the rat pelvic nerve. Eur Urol. 2007 Sep;52(3):842-7.