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Naftopidil
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Naftopidil图片
CAS NO:57149-07-2

Naftopidil (KT-611) 是一种选择性 alpha1-adrenoceptor 拮抗剂,对克隆的人 α1a-、α1b- 和 α1d-adrenoceptor 亚型的 Kis 分别为 3.7 nM、20 nM 和 1.2 nM。
Cas No.57149-07-2
别名萘哌地尔; KT-611; BM-15275
化学名1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol
Canonical SMILESCOC1=CC=CC=C1N2CCN(CC2)CC(COC3=CC=CC4=CC=CC=C43)O
分子式C24H28N2O3
分子量392.49
溶解度≥ 19.6245mg/mL in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Naftopidil (Flivas), a selective α1-adrenergic receptor antagonist or alpha blocker, is an antihypertensive drug.Target: α1-Adrenergic ReceptorNaftopidil significantly improved the overall international prostatic symptom score ; from 19.2±7.9 to 11.7±5.8 in the M group and from 19.4±6.4 to 12.3±6.8 in the E group (p<0.0001), QOL score from 4.9±0.8 to 3.2±1.4 in the M group and from 5.0±0.8 to 3.6±1.3 in the E group (p<0.0001), and OAB symptom score from 7.8±2.6 to 5.0±2.5 in the M group (p<0.0001) and from 8.6±2.9 to 5.8± 3.3 in the E group (p<0.0001). naftopidil improves storage symptoms as well as voiding symptoms regardless of timing of administration [1]. The selectivity of naftopidil for prostatic pressure was the most potent among the test compounds. In addition, using cloned human alpha1-adrenoceptor subtypes, naftopidil was selective for the alpha1d-adrenoceptor with approximately 3- and 17-fold higher affinity than for the alpha1a- and alpha1b-adrenoceptor subtypes, respectively. The selectivity of naftopidil for prostatic pressure may be attributable to its high binding affinity for alpha1a- and alpha1d-adrenoceptor subtypes [2].

References:
[1]. Sakai, H., et al., [Efficacy of naftopidil in patients with overactive bladder associated with benign prostatic hyperplasia: prospective randomized controlled study to compare differences in efficacy between morning and evening medication]. Hinyokika Kiyo, 2011. 57(1): p. 7-13.
[2]. Takei, R., et al., Naftopidil, a novel alpha1-adrenoceptor antagonist, displays selective inhibition of canine prostatic pressure and high affinity binding to cloned human alpha1-adrenoceptors. Jpn J Pharmacol, 1999. 79(4): p. 447-54.

 
 
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