Alfuzosin HCl

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Chemical Structure| 81403-68-1 同义名 : 阿夫唑嗪盐酸盐 ;SL 77499-10; Alfuzosin(hydrochloride); Uroxatral; SL 77499 HCl; Alfuzosin hydrochloride
CAS号 : 81403-68-1
货号 : A272742
分子式 : C19H28ClN5O4
纯度 : 98%
分子量 : 425.91
MDL号 : MFCD00879135
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: 25 mg/mL(58.7 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

H2O: 50 mg/mL(117.4 mM)，配合低频超声助溶
生物活性
靶点

  • α-adrenergic receptor
描述 Alfuzosin hydrochloride is a selective and competitive α1-adrenoceptor antagonist for the treatment of symptomatic BPH (benign prostatic hyperplasia)[3]. In the pithed rat, alfuzosin (0.03-0.3 mg kg-1, i.v.) markedly inhibited pressor responses produced by the alpha 1-selective agonist; alfuzosin (1 mg kg-1, i.v.) had minimal effects against responses mediated by stimulation of prejunctional alpha 2-receptors[4]. Moreover, Alfuzosin hydrochloride is an appropriate candidate drug to prepare a gastro-retention controlled release dosage form[5].
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
NCT01685658 Renal Colic A... 展开 >>cute Renal Colic 收起 << Phase 4 Suspended(same study already p... 展开 >>ublished) 收起 << March 2018 France ... 展开 >> CH d'Alès Alès, France, 30103 CHU de Nîmes - Hôpital Universitaire Carémeau Nîmes Cedex 9, France, 30029 收起 <<
NCT01323998 - Completed - -
NCT01332487 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.35mL

0.47mL

0.23mL

11.74mL

2.35mL

1.17mL

23.48mL

4.70mL

2.35mL
参考文献

[1]Lacerda AE, Kuryshev YA, et al. Alfuzosin delays cardiac repolarization by a novel mechanism. J Pharmacol Exp Ther. 2008 Feb;324(2):427-33.

[2]Palea S, Barras M. Comparison of the relaxant effects of alfuzosin, phentolamine and sildenafil on rabbit isolated corpus cavernosum. BJU Int. 2003 Jun;91(9):873-7.

[3]Fahmy RH. Statistical approach for assessing the influence of calcium silicate and HPMC on the formulation of novel alfuzosin hydrochloride mucoadhesive-floating beads as gastroretentive drug delivery systems. AAPS PharmSciTech. 2012 Sep;13(3):990-1004.

[4]Lefèvre-Borg F, O'Connor SE, Schoemaker H, Hicks PE, Lechaire J, Gautier E, Pierre F, Pimoule C, Manoury P, Langer SZ. Alfuzosin, a selective alpha 1-adrenoceptor antagonist in the lower urinary tract. Br J Pharmacol. 1993 Aug;109(4):1282-9.

[5]Gong L, Sun Y, Yu M, Gao Y, Zou M, Cheng G. Development and Evaluation of Compression Coating Gastro-Floating Tablet of Alfuzosin Hydrochloride for Zero-Order Controlled Release. AAPS PharmSciTech. 2018 Oct;19(7):3277-3286.