Flavoxate HCl

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Chemical Structure| 3717-88-2 同义名 : Rec-7-0040; DW61; Flavoxate HCl, Flavoxate hydrochloride, DW-61, Rec-7-0040; Rec 7/0040; Flavoxate (hydrochloride); NSC-114649; Flavoxate hydrochloride
CAS号 : 3717-88-2
货号 : A666517
分子式 : C24H26ClNO4
纯度 : 99%
分子量 : 427.92
MDL号 : MFCD00072099
存储条件：

Pure form Inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 3 mg/mL(7.01 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

H2O: 5 mg/mL(11.68 mM)，配合低频超声助溶
生物活性
靶点

  • mAChR

    mAChR, IC50:12.2 μM
描述 Flavoxate Hydrochloride is a muscarinic AChR antagonist. It has been reported that flavoxate causes a concentration-dependent relaxation of the tension elicited by muscarinic stimulation (IC50=35 μM) or 5 mM extracellular Ca2+ (IC50=83 μM) in rat detrusor. And flavoxate caused a concentration-dependent relaxation of human urinary bladder precontracted by K+ with much higher potency (IC50=2 μM)[3]. Flavoxate (10-8-10-5 M) inhibited cAMP formation in a concentration-dependent manner. Flavoxate (3 mg/kg, i.v.) completely abolished rhythmic bladder contractions in vehicle-pretreated rats, but not in PTX-pretreated (pertussis toxin ) rats[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00440739 Pain Phase 4 Completed - Thailand ... 展开 >> Faculty of Medicine Siriraj Hospital, Mahidol University Bangkok, Thailand, 10700 收起 <<
NCT00992238 Healthy Phase 1 Completed - United States, North Dakota ... 展开 >> PRACS Institute, Ltd Fargo, North Dakota, United States, 58104 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.34mL

0.47mL

0.23mL

11.68mL

2.34mL

1.17mL

23.37mL

4.67mL

2.34mL
参考文献

[1]Dansette PM, Jaoen M, et al. HMG-CoA reductase activity in human liver microsomes: comparative inhibition by statins. Exp Toxicol Pathol. 2000 May;52(2):145-8.

[2]Kimura Y, Sasaki Y, et al. Mechanisms of the suppression of the bladder activity by flavoxate. Int J Urol. 1996 May;3(3):218-27.

[3]Tomoda T, Aishima M, Takano N, Nakano T, Seki N, Yonemitsu Y, Sueishi K, Naito S, Ito Y, Teramoto N. The effects of flavoxate hydrochloride on voltage-dependent L-type Ca2+ currents in human urinary bladder. Br J Pharmacol. 2005 Sep;146(1):25-32.

[4]Oka M, Kimura Y, Itoh Y, Sasaki Y, Taniguchi N, Ukai Y, Yoshikuni Y, Kimura K. Brain pertussis toxin-sensitive G proteins are involved in the flavoxate hydrochloride-induced suppression of the micturition reflex in rats. Brain Res. 1996 Jul 15;727(1-2):91-8.