Naftopidil 2HCl

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Chemical Structure| 57149-08-3 同义名 : BM-15275 dihydrochloride;KT-611 dihydrochloride;Naftopidil DiHCl;Naftopidil dihydrochloride
CAS号 : 57149-08-3
货号 : A127685
分子式 : C24H30Cl2N2O3
纯度 : 99%
分子量 : 465.413
MDL号 : MFCD00153845
存储条件：

Pure form Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：

0.5% CMC+water 30 mg/mL suspension

生物活性
靶点

  • α-adrenergic receptor

    α1-adrenergic receptor, IC50:0.2 μM
描述 Naftopidil (Dihydrochloride), a selective α1-adrenergic receptor antagonist or alpha blocker, is an antihypertensive drug. Naftopidil significantly improved the overall international prostatic symptom score[3]. The intravenous administration of each of Naftopidil dose-dependently inhibited phenylephrine-induced increases in prostatic pressure and mean blood pressure, the selectivity index was 3.76 [4]. Moreover, Naftopidil induces apoptosis and autophagy of HGC27 cells (human gastric cancer cell line), however, autophagy is considered to inhibit apoptosis[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.21mL

10.74mL

2.15mL

1.07mL

21.49mL

4.30mL

2.15mL
参考文献

[1]Kanda H, Ishii K, et al. Naftopidil, a selective alpha-1 adrenoceptor antagonist, inhibits growth of human prostate cancer cells by G1 cell cycle arrest. Int J Cancer. 2008 Jan 15;122(2):444-51.

[2]Borbe HO, Metzenauer P, Szelenyi I. 5-HT1A-agonistic properties of naftopidil, a novel antihypertensive drug. Eur J Pharmacol. 1991 Nov 19;205(1):105-7.

[3]Sakai H, Igawa T, Onita T, Furukawa M, Hakariya T, Hayashi M, Matsuya F, Shida Y, Nishimura N, Yogi Y, Tsurusaki T, Takehara K, Nomata K, Shiraishi K, Shono T, Aoki D, Kanetake H. [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 Jan;57(1):7-13. Japanese.

[4]Takei R, Ikegaki I, Shibata K, Tsujimoto G, Asano T. 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 Apr;79(4):447-54. doi: 10.1254/jjp.79.447. PMID: 10361884.

[5]Nakamura A, Matsunaga W, Gotoh A. Autophagy Induced by Naftopidil Inhibits Apoptosis of Human Gastric Cancer Cells. Anticancer Res. 2018 Feb;38(2):803-809.