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Naftopidil Dihydrochloride

产品号 S1387 公司名称 Selleck Chemicals
CAS号 57149-08-3 公司网站 http://www.selleckchem.com
分子式 C24H30Cl2N2O3 电 话 (877) 796-6397
分子量 465.4126 传 真 (832) 582-8590
纯 度 电子邮件 sales@selleckchem.com
保 存 -20°C Chembase数据库ID: 72654

产品价格信息

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产品别名

标题
Naftopidil Dihydrochloride
IUPAC标准名
1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-(naphthalen-1-yloxy)propan-2-ol dihydrochloride
IUPAC传统名
flivas dihydrochloride
别名
Flivas
KT-611
BM-15275
Avishot

产品登记号

CAS号 57149-08-3

产品性质

作用靶点 adrenergic receptor
成盐信息 Dihydrochloride
保存条件 -20°C

产品详细信息

详细说明 (English)
Research Area
Description Cardiovascular Disease
Biological Activity
Description Naftopidil DiHCl is a selective 5-HT1A and α1-adrenergic receptor antagonist with IC50 of 0.1 μM and 0.2 μM, respectively.
Targets 5-HT1A receptor α1-adrenergic receptor
IC50 0.1 μM 0.2 μM [1]
In Vitro Naftopidil diHCl possesses 5-HT1A agonistic properties in addition to being an α1-adrenoceptor antagonist. [1] Naftopidil has growth inhibitory effect in androgen-sensitive and -insensitive human prostate cancer cell lines. Naftopidil inhibits the growth of androgen-sensitive LNCaP cells and androgen-insensitive PC-3 cells with IC50 of 22.2 μM and 33.2 μM, respectively. Cell growth inhibition by Naftopidil is due to the arrest of the G1 cell cycle. Expressions of p27kip1 and p21cip1 are significantly increased in LNCaP cells treated with Naftopidil. In PC-3 cells, Naftopidil induces p21cip1 but not p27kip1. [2] Naftopidil produces a concentration-dependent inhibition of collagen-induced Ca2+ mobilization, maximum inhibition (22.9%) occurring with 40 μM Naftopidil. The adrenaline-induced rise in [Ca2+]i is inhibited dose dependently by Naftopidil. [3] Naftopidil is significantly more effective than tamsulosin in relieving nocturia. [4] Naftopidil induces G(1) cell-cycle arrest in both PCa cells and PrSC. In Naftopidil-treated PrSC, total interleukin-6 protein is significantly reduced with increased suppression of cell proliferation. [5]
In Vivo Oral administration of Naftopidil to nude mice inhibits the growth of PC-3 tumors as compared to vehicle-treated controls. Naftopidil improves bladder capacity and relaxed voiding via inhibition of afferent nerve activity. [2] Naftopidil (0.1 μg–30 μg) transiently abolishes isovolumetric rhythmic bladder contraction. The amplitude of bladder contraction is decreased by intrathecal injection of naftopidil (3 μg–30 μg). [6] Naftopidil selectively inhibits the phenylephrine-induced increase in prostatic pressure compared with mean blood pressure in the anesthetized dog model. [7]
Clinical Trials
Features Higher selectivity for the -1A and -1D subtypes.
Protocol
Cell Assay [2]
Cell Lines LNCaP and PC-3 cell lines
Concentrations 20 μM, 40 μM
Incubation Time 24 hours
Methods Cell cycle analysis is performed by flow cytometry. Cells are treated with either 20 μM Naftopidil (LNCaP), 40 μM Naftopidil (PC-3) or vehicle (0.1% DMSO) for 24 hours, then trypsinized and washed once with phosphate-buffer saline (PBS), fixed in 70% ethanol and stored at 4 °C for subsequent cell cycle analysis. Fixed cells are washed with PBS and incubated with PBS containing 20 μg/mL RNaseA and 0.3% NP-40 for 30 minutes at 37 °C, then stained with 50 μg/mL propidium iodide (PI) for 30 minutes at 4 °C in the dark. The DNA content of 1 × 106 stained cells is analyzed on a FACS Caliburflow cytometer. The fractions of cells in the G0/G1, S and G2/M phases are calculated using Cell Quest software.
Animal Study [2]
Animal Models Athymic nude mice bearing PC-3 cells
Formulation 0.5% carboxymethylcellulose
Doses 10 mL/kg/day
Administration Orally
References
[1] Borbe HO, et al. Eur J Pharmacol, 1991, 205(1), 105-107.
[2] Kanda H, et al. Int J Cancer, 2008, 122(2), 444-451.
[3] Alarayyed NA, et al. Br J Clin Pharmacol, 1997, 43(4), 415-420.
[4] Nishino Y, et al. BJU Int, 2006, 97(4), 747-751.
[5] Hori Y, et al. Cancer Prev Res (Phila), 2011, 4(1), 87-96.
[6] Sugaya K, et al. Neurosci Lett, 2002, 328(1), 74-76.
[7] Takei R, et al. Jpn J Pharmacol, 1999, 79(4), 447-454.