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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
规格:≥98%
包装与价格:
包装价格(元)
1g电议
2g电议
5g电议
10g电议
25g电议
50g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)392.49
FormulaC24H28N2O3
CAS No.57149-07-2
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 79 mg/mL (201.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Chemical Name1-(4-(2-methoxyphenyl)piperazin-1-yl)-3-(naphthalen-1-yloxy)propan-2-ol diHCl
SynonymsKT-611; BM-15275; KT611; BM 15275; KT 611; BM15275; KT611; Flivas
实验参考方法
In Vitro

In vitro activity: Naftopidil is selective for the alpha1d-adrenoceptor with approximately 3- and 17-fold higher affinity than for the alpha1a- and alpha1b-adrenoceptor subtypes, respectively. 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. 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. 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. 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.

In VivoNaftopidil selectively inhibits the phenylephrine-induced increase in prostatic pressure compared with mean blood pressure in the anesthetized dog model. Naftopidil inhibits 5-HT-induced bladder contraction via blockade of the 5-HT(2A) and 5-HT(2B) receptors in rats.
Animal modelRats and dogs
Formulation & DosageN/A
References

Jpn J Pharmacol. 1999 Apr;79(4):447-54; Eur J Pharmacol. 2013 Jan 30;700(1-3):194-200.