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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
包装与价格:
包装价格(元)
500 mg电议
1 g电议
1 mL*10 mM(in DMSO)电议

产品名称
BM-15275
KT-611
萘哌地尔
产品介绍
Naftopidil 是一种选择性的 alpha1-肾上腺素受体 (α1-adrenoceptor) 拮抗剂,对克隆的人类 α1a、α1b和 α1d亚型肾上腺素受体的亲和力Ki分别为 3.7 nM、20 nM 、1.2 nM。它具有抗增殖活性,可用于研究前列腺增生。

产品描述

Naftopidil (INN, marketed under the brand name Flivas), an antihypertensive medicine, is used as a selective α1-adrenergic receptor antagonist or α-blocker.

体外活性

Naftopidil is selective for the alpha1d-adrenoceptor with approximately 3- and 17-fold higher affinity than for the alpha1a- and alpha1b-adrenoceptor subtypes, respectively. [1] Naftopidil has growth inhibitory effect in androgen-sensitive and -insensitive human prostate cancer cell lines. Naftopidil induces p21(cip1) but not p27(kip1) in PC-3 cells. [2] Naftopidil induces apoptosis in all the investigated malignant mesothelioma cells, and a similar effect is obtained with prazosin, another α1-adrenoceptor blocker. Naftopidil-induced reduction in cell viability is inhibited by GF109203X, while prazosin-induced in cell viability is less affected. [3] Naftopidil, an alpha 1-adrenoreceptor antagonist produces a concentration-dependent inhibition ofcollagen-induced Ca2+ mobilization, maximum inhibition (22.9%) occurring with 40 mM Naftopidil. Naftopidil also inhibits the adrenaline-induced rise in [Ca2+]i in a concentration-dependent manner (30 mM doxazosin), significant inhibitions of platelet aggregation also being produced. [4] Naftopidil (0.3, 1, and 3 μM) inhibits 5-HT-induced bladder contraction in a concentration-dependent manner. Naftopidil inhibits both the 5-HT(2A) and 5-HT(2) receptor agonists-induced bladder contractions. Naftopidil binds to the human 5-HT(2A) and 5-HT(2B) receptors with pKi values of 6.55 and 7.82, respectively. [5]

体内活性

Naftopidil selectively inhibits the phenylephrine-induced increase in prostatic pressure compared with mean blood pressure in the anesthetized dog model. [1] Naftopidil inhibits 5-HT-induced bladder contraction via blockade of the 5-HT(2A) and 5-HT(2B) receptors in rats. [5]

Cas No.

57149-07-2

分子式

C24H28N2O3

分子量

392.499

别名

BM-15275;KT-611;萘哌地尔

储存和溶解度

H2O:<1 mgml
DMSO:73 mg/mL (186 mM)
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years