Naftopidil (hydrochloride)
(Synonyms: KT-611 hydrochloride; BM-15275 hydrochloride) 目录号 : GC44311
An α1-adrenergic receptor antagonist
Cas No.:1164469-60-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Naftopidil is an α1-adrenergic receptor antagonist that competitively inhibits α-adrenoceptor-mediated contractions induced by noradrenaline with pA2 values of 6.73-8.15 in various blood vessels from dog, rabbit, guinea pig, and rat. It binds to the cloned human α1-adrenergic receptors with Ki values of 3.7, 20, and 1.2 nM for α1A, α1B and α1D, respectively. Clinical formulations of naftopidil are used in the treatment of benign prostatic hyperplasia in Japan. Naftopidil also exhibits antiproliferative activity, inhibiting the growth of androgen-sensitive LNcaP cells and androgen-insensitive PC-3 cancer cell lines with IC50 values of 22.2 and 33.2 µM, respectively.
| Cas No. | 1164469-60-6 | SDF | |
| 别名 | KT-611 hydrochloride; BM-15275 hydrochloride | ||
| Canonical SMILES | COC1=C(N2CCN(CC(COC3=CC=CC4=C3C=CC=C4)O)CC2)C=CC=C1.Cl | ||
| 分子式 | C24H28N2O3•HCl | 分子量 | 429 |
| 溶解度 | DMF: 10 mg/mL,DMF:PBS (pH 7.2) (1:4): 0.2 mg/mL,DMSO: 3 mg/mL | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.331 mL | 11.655 mL | 23.31 mL |
| 5 mM | 0.4662 mL | 2.331 mL | 4.662 mL |
| 10 mM | 0.2331 mL | 1.1655 mL | 2.331 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Naftopidil for the treatment of lower urinary tract symptoms compatible with benign prostatic hyperplasia
Cochrane Database Syst Rev 2009 Oct 7;(4):CD007360.PMID:19821408DOI:10.1002/14651858.CD007360.pub2.
Background: Benign prostatic hyperplasia (BPH) is a common condition in aging men causing lower urinary tract symptoms (LUTS). Treatment aims are to relieve symptoms and prevent disease progression. Of the different alpha-1 adrenergic receptors (ARs) in the prostate, alpha-1a receptors are known to be central to prostatic smooth-muscle contraction. Recent studies have shown that patients with BPH may also have a predominance of alpha-1d receptors. Objectives: To evaluate the efficacy and adverse effects of Naftopidil, a selective alpha-1d oral alpha-blocking agent for the treatment of LUTS associated with BPH. Search strategy: Systematic review of trials published January 1950 to January 2009. Sources included MEDLINE and bibliographies of retrieved articles and review articles. Selection criteria: Eligible trials included: men diagnosed with symptomatic BPH; compared Naftopidil to placebo, control, or combination therapy; evaluated clinically relevant outcomes between randomized groups; had at least 4-weeks follow up; and were published in English language. Data collection and analysis: Participant demographics and comorbidities, enrollment criteria, outcomes, adverse events, numbers and reasons for dropouts were extracted onto standardized extraction forms by one reviewer. The mean change and per cent improvement from baseline in AUA (American Urological Association Symptom Score) and IPSS (International Prostate Symptom Score) scores and other efficacy outcomes for treatment and control groups were calculated. If feasible, the efficacy outcomes and adverse events data were pooled. Main results: Eight trials were eligible (N = 744 participants). All trials were conducted in Japan. Study duration ranged from 4 to 17 weeks. The mean age of participants was 68 years; pretreatment mean IPSS = 17.8 and mean peak urine flow (Qmax) = 9.5 mL/s (milliliters/second). No trials compared Naftopidil to placebo. In 5 trials (N = 419), Naftopidil in doses of 25 to 75 mg/d (milligrams/day) showed a mean IPSS improvement similar to low-dose tamsulosin (0.2 mg/d) (8.4 versus 8.9 points). Compared to a phytotherapy preparation (eviprostat), Naftopidil significantly improved total IPSS (-5.9 versus 0.4; P < 0.0002). In one trial, the addition of anticholinergic drugs (oxybutynin or propiverine hydrochloride) to Naftopidil did not offer any significant improvement for IPSS or Qmax in comparison to treatment with Naftopidil alone. Although IPSS did not significantly differ between high- (75 mg/d) and low-dose (25mg/d) Naftopidil, high dose significantly improved Qmax compared to low dose (1.2 mL/s versus 0.2 mL/s). Adverse events reported were few, mild and similar to those seen with 0.2 mg/d tamsulosin. Authors' conclusions: There are no data from placebo controlled trials regarding the efficacy of Naftopidil in men with symptomatic BPH. Limited information suggests that treatment with Naftopidil provides short-term improvement in urinary symptom-scale scores (total IPSS/AUA), QoL (quality of life) score, and urinary symptoms from baseline comparable to low-dose tamsulosin. Adverse effects due to Naftopidil were few and usually mild.
Naftopidil and propiverine hydrochloride for treatment of male lower urinary tract symptoms suggestive of benign prostatic hyperplasia and concomitant overactive bladder: a prospective randomized controlled study
Scand J Urol Nephrol 2009;43(4):307-14.PMID:19396723DOI:10.1080/00365590902836740.
Objective: To assess the efficacy and safety of propiverine hydrochloride (antimuscarinic), Naftopidil (alpha(1)-adrenoceptor antagonist) or both in patients with male lower urinary tract symptoms (LUTS) suggestive of benign prostatic hyperplasia and concomitant overactive bladder (OAB). Material and methods: Men aged at least 50 years who had a total International Prostate Symptom Score (IPSS) of 8 or higher and bladder dairy documenting micturition frequency (more than eight micturitions/24 h) and urgency (more than one episode/24 h), with or without urgency urinary incontinence were randomized into three groups: group N, Naftopidil (50 mg once daily) only; group P, propiverine hydrochloride (20 mg once daily); and group NP, Naftopidil (50 mg once daily) plus propiverine hydrochloride (20 mg once daily) for a 4-week treatment regimen. Results: A total of 66 men, including 20 in group N, 23 in group P and 23 in group NP, were treated and 58 (87.9%) completed the 4 weeks of treatment. IPSS improved significantly in groups N and NP. Urinary frequency improved significantly in groups P and NP. Postvoid residual urine volume increased significantly in groups P and NP. Significant improvements in urgency episodes were noted in each group. One patient in group P required catheterization owing to acute urinary retention and another stopped medication because of difficulty in voiding. Conclusion: These results suggest that each treatment showed effectiveness for male LUTS with OAB. However, there are some possibilities of adverse effects with propiverine hydrochloride monotherapy.
Naftopidil versus tamsulosin hydrochloride for lower urinary tract symptoms associated with benign prostatic hyperplasia with special reference to the storage symptom: a prospective randomized controlled study
Int J Urol 2008 Dec;15(12):1049-54.PMID:19120513DOI:10.1111/j.1442-2042.2008.02169.x.
Objectives: In order to compare the clinical efficacy of Naftopidil (Naf) and tamsulosin hydrochloride (Tam), which differ in their selectivity to alpha receptor subtypes, we performed a multi-center prospective randomized controlled study. Methods: Men complaining of lower urinary tract symptoms due to benign prostatic hypertrophy, were randomized into two treatment groups: one receiving 50 mg Naftopidil daily (Naf group, n = 31 pts), and one receiving 0.2 mg Tam once daily (Tam group, n = 28 pts). Baseline symptom scores were compared to those at 2 weeks and at the end of the observation period (6-8 weeks). Results: In the Naf group at 2 weeks, the score of the daytime frequency significantly improved from 3.5 to 2.2 (P = 0.03), and the score of nocturia improved significantly from 3.5 to 2.2 (P = 0.0004), respectively. In the Tam group at 2 weeks, however, no significant improvement was noted in the increased score of daytime frequency (P = 0.1) or nocturia (P = 0.2). At 2 weeks, the storage symptom score of the frequency to the combined score of daytime frequencies and the score of nocturia was better in the Naf group (improved from 7.0 to 4.4, P = 0.0017) than in the Tam group (from 6.8 to 4.9, P = 0.08) (P < 0.05). At 6-8 weeks, the effects of the two drugs on lower urinary tract symptoms were comparable. Conclusions: Naf demonstrated a significant early response to improve storage symptoms at 2 weeks, including daytime frequency and nocturia, compared with Tam.
A comparison of the efficacy of Naftopidil and tamsulosin hydrochloride in medical treatment of benign prostatic enlargement
Urol Ann 2015 Jan-Mar;7(1):74-8.PMID:25657550DOI:10.4103/0974-7796.148624.
Introduction: Lower urinary tract symptoms in men, over age of 50 years is suggestive of benign prostatic enlargement (BPE). Different alpha-blockers have been evaluated for the treatment of benign prostatic hyperplasia for over last 30 years. This study was conducted in a tertiary care institution during the period of year between June 2011 and August 2013 to compare the effect of Naftopidil and tamsulosin in reducing the obstructive and irritable symptoms of BPE. Subjects and methods: A prospective randomized comparative study was carried on 60 patients of BPE by assigning half of them to treatment with tamsulosin and rest with Naftopidil. Pre- and post-treatment uroflowmetry (UFM), post-void residue (PVR), International Prostate Symptoms Score (IPSS), were obtained at 15 and 30 days after starting treatment. Results: The age of patients ranged from 51 to 78. At base line there was no statistical difference between UFM parameter, PVR and IPSS in the two groups. UFM and PVR showed significantly better response at both intervals with Naftopidil. Comparison of IPSS showed better improvement in Group A both at 15 and 30 days. It was seen that the obstructive symptoms showed a significantly better response with tamsulosin and symptoms of irritability was seen better response with Naftopidil. Conclusion: It was seen that during the period of follow-up of 30 days Naftopidil had a better effect on UFM, PVR, IPSS compared with tamsulosin. In general, obstructive symptoms showed better improvement in tamsulosin and irritative symptoms showed better improvement in Naftopidil.
Naftopidil for the treatment of urinary symptoms in patients with benign prostatic hyperplasia
Ther Clin Risk Manag 2011;7:227-38.PMID:21753885DOI:10.2147/TCRM.S13883.
Naftopidil, approved only in Japan, is an α1-adrenergic receptor antagonist (α1-blocker) used to treat lower urinary tract symptoms (LUTS) suggestive of benign prostatic hyperplasia (BPH). Different from tamsulosin hydrochloride and silodosin, in that it has higher and extremely higher affinity respectively, for the α1A-adrenergic receptor subtype than for the α1D type, Naftopidil has distinct characteristics because it has a three times greater affinity for the α1D-adrenergic receptor subtype than for the α1A subtype. Although well-designed large-scale randomized controlled studies are lacking and the optimal dosage of Naftopidil is not always completely determined, previous reports from Japan have shown that Naftopidil has superior efficacy to a placebo and comparable efficacy to other α1-blockers such as tamsulosin. On the other hand, the incidences of ejaculatory disorders and intraoperative floppy iris syndrome induced by Naftopidil may be lower than for tamsulosin and silodosin having high affinity for the α1A-adrenergic receptor subtype. However, it remains unknown if the efficacy and safety of Naftopidil in Japanese is applicable to white, black and Hispanic men having LUTS/BPH in western countries.