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Effects of phosphodiesterase 5 inhibitors on sperm parameters and fertilizing capacity 被引量:11
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作者 F. Dimitriadis D. Giannakis +11 位作者 N. Pardalidis K. Zikopoulos E. Paraskevaidis N. Giotitsas V. Kalaboki P.Tsounapi D. Baltogiannis Georgiou M.Saito T.Watanabe I. Miyagawa N.Sofildtis 《Asian Journal of Andrology》 SCIE CAS CSCD 2008年第1期115-133,共19页
The aim of this review study is to elucidate the effects that phosphodiesterase 5 (PDE5) inhibitors exert on spermatozoa motility, capacitation process and on their ability to fertilize the oocyte. Second messenger ... The aim of this review study is to elucidate the effects that phosphodiesterase 5 (PDE5) inhibitors exert on spermatozoa motility, capacitation process and on their ability to fertilize the oocyte. Second messenger systems such as the cAMP/adenylate cyclase (AC) system and the cGMP/guanylate cyclase (GC) system appear to regulate sperm functions. Increased levels of intracytosolic cAMP result in an enhancement of sperm motility and viability. The stimulation of GC by low doses of nitric oxide (NO) leads to an improvement or maintenance of sperm motility, whereas higher concentrations have an adverse effect on sperm parameters. Several in vivo and in vitro studies have been carried out in order to examine whether PDE5 inhibitors affect positively or negatively sperm parameters and sperm fertilizing capacity. The results of these studies are controversial. Some of these studies demonstrate no significant effects of PDE5 inhibitors on the motility, viability, and morphology of spermatozoa collected from men that have been treated with PDE5 inhibitors. On the other hand, several studies demonstrate a positive effect of PDE5 inhibitors on sperm motility both in vivo and in vitro. In vitro studies of sildenafil citrate demonstrate a stimulatory effect on sperm motility with an increase in intracellular cAMP suggesting an inhibitory action of sildenafil citrate on a PDE isoform other than the PDE5. On the other hand, tadalafil's actions appear to be associated with the inhibitory effect of this compound on PDE11. In vivo studies in men treated with vardenafil in a daily basis demonstrated a significantly larger total number of spermatozoa per ejaculate, quantitative sperm motility, and qualitative sperm motility; it has been suggested that vardenafil administration enhances the secretory function of the prostate and subsequently increases the qualitative and quantitative motility of spermatozoa. The effect that PDE5 inhibitors exert on sperm parameters may lead to the improvement of the outcome of assisted reproductive technology (ART) programs. In the future PDE5 inhibitors might serve as adjunct therapeutical agents for the alleviation of male infertility. 展开更多
关键词 sperm fertilizing capacity phosphodiesterase 5 inhibitors SPERMATOZOA TESTIS male infertility
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Evaluation and diagnostic testing of erectile dysfunction in the era of phosphodiesterase type 5 inhibitors 被引量:1
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作者 Kenneth Jacobsohn Run Wang 《Asian Journal of Andrology》 SCIE CAS CSCD 2007年第1期3-7,共5页
自从安全、有效的口头的治疗的可获得性,可勃起的机能障碍的诊断和处理戏剧性地变化了。不幸地,不是都,人们能足够地这样被对待,并且可能要求诊断并且对待他们的机能障碍的特定的原因的更侵略的测试。这评论看测试和为不能被口头的... 自从安全、有效的口头的治疗的可获得性,可勃起的机能障碍的诊断和处理戏剧性地变化了。不幸地,不是都,人们能足够地这样被对待,并且可能要求诊断并且对待他们的机能障碍的特定的原因的更侵略的测试。这评论看测试和为不能被口头的治疗独自对待的人可得到的策略。 展开更多
关键词 磷酸二酯酶 男子性功能障碍 诊断方法 药物治疗
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Are phosphodiesterase type 5 inhibitors effective for the management of lower urinary symptoms suggestive of benign prostatic hyperplasia? 被引量:1
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作者 Li Tao Zhang Jong Kwan Park 《World Journal of Nephrology》 2015年第1期138-147,共10页
AIM: To review the efficacy of phosphodiesterase type 5 inhibitors(PDE5-Is) in lower urinary tract symptoms(LUTS) suggestive of benign prostate hyperplasia(LUTS/BPH). METHODS: A comprehensive research was conducted to... AIM: To review the efficacy of phosphodiesterase type 5 inhibitors(PDE5-Is) in lower urinary tract symptoms(LUTS) suggestive of benign prostate hyperplasia(LUTS/BPH). METHODS: A comprehensive research was conducted to identify all publications relating to benign prostate hyperplasia and treatment with sildenafil, vardenafil and tadalafil. To assess the efficacy, the changes in total international prostate symptom score(IPSS), IPSS subscore including voiding, storage and quality of life(Qo L), Benign prostatic hyperplasia Impact Index(BII), maximum urinary flow rate(Qmax) and the International Index of Erectile Function(IIEF) were extracted. A meta-analytical technique was used for the analysis of integrated data from the included studies to evaluate the mean difference in the results. RESULTS: Total IPSS score, IIEF and BII showed a significant improvement in trials in which LUTS/BPH with or without erectile dysfunction(ED) were compared with the placebo. For LUTS/BPH, the mean differences of total IPSS score, IIEF and BII are-2.17, 4.88 and-0.43, P < 0.00001, respectively. For LUTS/BPH with comorbid ED, the mean difference are-1.97, 4.54 and-0.52, P < 0.00001, respectively. PDE5-Is appear to improve IPSS storage, voiding and Qo L subscore(mean difference =-0.71,-1.23 and-0.33, P < 0.00001, respectively). Although four doses of tadalafil(2.5, 5, 10 and 20 mg) failed to reach significance in Qmax(mean difference = 0.22, P = 0.10), the 5 mg dose of tadalafil significantly improved the Qmax(mean difference = 0.33, P = 0.03).CONCLUSION: PED5-Is demonstrated efficacy for improving LUTS in BPH patients with or without ED and could be considered to be the first line treatment for LUTS/BPH. 展开更多
关键词 尿路 前列腺 治疗方法 临床分析
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Erectile potentials of a new phosphodiesterase type 5 inhibitor, DA-8159, in diet-induced obese rats 被引量:2
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作者 Jae-Young Yu Kyung-Koo Kang Moohi Yoo 《Asian Journal of Andrology》 SCIE CAS CSCD 2006年第3期325-329,共5页
Aim: To examine the changes in the erectile function in diet-induced obese rats and investigate the oral efficacy of DA-8159, a new phosphodiesterase type 5 (PDE5) inhibitor, on penile erection in obese rats. Meth... Aim: To examine the changes in the erectile function in diet-induced obese rats and investigate the oral efficacy of DA-8159, a new phosphodiesterase type 5 (PDE5) inhibitor, on penile erection in obese rats. Methods: The rats were fed a high-energy diet for 12 weeks and divided into three groups: an obesity-resistant (OR) control group, an obesity-prone (OP) control group, and an OP-DA-8159 treatment (DA-8159) group. The electrostimulation-induced erectile responses were measured in all groups. The body weight, plasma cholesterol, triglyceride and glucose levels were also measured. Results: In the OP control group, the maximum intracavernous pressure (ICP) and ICP/blood pressure (ICP/BP) ratio after electric stimulation were significantly lower than those in OR control group. The corresponding area under the curve (AUC) of the ICP/BP ratio, the detumescence time and the baseline cavernous pressure were also lower than those in the OR control group, but this difference was not significant. The body weight gain, plasma cholesterol and triglyceride level in the OP group were significantly higher than those in the OR group. After administering the DA-8159, a significant increase in the maximum ICP and the ICP/BP ratio were observed. The corresponding AUCs in the DA-8159 group were also higher than those in the two control groups. Furthermore, the detumescence time was significantly prolonged after treatment with DA-8159. Conclusion: These results demon- strate that diet-induced obesity affects the erectile function in rats and these erectile dysfunction (ED) can be improved by the treatment with DA-8159, indicating DA-8159 might be a treatment option for ED associated with obesity. 展开更多
关键词 phosphodiesterase type 5 inhibitor penile erection OBESITY DA-8159 intracavemous pressure
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The use of antimuscarinics,phosphodiesterase type Ⅴ inhibitors and phytotherapy for lower urinary tract symptoms in men 被引量:2
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作者 Kok Kit Ng Foo Cheong Ng 《Asian Journal of Urology》 2017年第3期191-194,共4页
Besides the mainstay of α-blockers and 5α-reductase inhibitors,other forms of medical therapy complete the armamentarium in the treatment of lower urinary tract symptoms(LUTS)in men.These treatments can target speci... Besides the mainstay of α-blockers and 5α-reductase inhibitors,other forms of medical therapy complete the armamentarium in the treatment of lower urinary tract symptoms(LUTS)in men.These treatments can target specific symptoms as well as associated symptoms that would affect the quality of life of the patients.Many patients are bothered by storage symptoms,more so than the voiding symptoms.Antimuscarinics are efficacious and safe,provided the patients do not have high post void residual urine.Many patients with LUTS also have erectile dysfunction,and phosphodiesterase type Ⅴ inhibitors are effective in relieving both LUTS as well as erectile dysfunction for such patients.Phytotherapy provides a popular and safe treatment for LUTS,however,the efficacy of the treatment has not been proven in well conducted prospective randomized controlled studies. 展开更多
关键词 Benign prostatic hyperplasia Erectile dysfunction Lower urinary tract symptoms Muscarinic antagonists phosphodiesterase 5 inhibitors PHYTOTHERAPY
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Effect of phosphodiesterase inhibitors in the bladder 被引量:1
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作者 Bilal Chughtai Aizaz Ali +1 位作者 Claire Dunphy Steven A.Kaplan 《Asian Journal of Urology》 2015年第1期33-37,共5页
Many aging men will experience lower urinary tract symptoms(LUTS).Phosphodiesterase type 5(PDE5)inhibitors have shown promise in treating LUTS in these patients.PDE5 inhibitors mediate their effects through several pa... Many aging men will experience lower urinary tract symptoms(LUTS).Phosphodiesterase type 5(PDE5)inhibitors have shown promise in treating LUTS in these patients.PDE5 inhibitors mediate their effects through several pathways including cAMP,NO/cGMP,Kchannel modulated pathways,and the L-cysteine/H2S pathway.PDE5 inhibitors exert their effect in muscle cells,nerve fibers,and interstitial cells(ICs).The use of PDE5 inhibitors led to improvement in LUTS.This included urodynamic parameters.PDE5 inhibitors may play a significant role in LUTS due to their effect on the bladder rather than the prostate. 展开更多
关键词 Lower urinary tract symptoms(LUTS) Overactive bladder syndrome(OAB) phosphodiesterase type 5 inhibitors NO/CGMP cAMP
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Statin, testosterone and phosphodiesterase 5-inhibitor treatments and age related mortality in diabetes
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作者 Geoffrey Hackett Peter W Jones +1 位作者 Richard C Strange Sudarshan Ramachandran 《World Journal of Diabetes》 SCIE CAS 2017年第3期104-111,共8页
AIM To determine how statins, testosterone(T) replacement therapy(TRT) and phosphodiesterase 5-inhibitors(PDE5I) influence age related mortality in diabetic men.METHODS We studied 857 diabetic men screened for the BLA... AIM To determine how statins, testosterone(T) replacement therapy(TRT) and phosphodiesterase 5-inhibitors(PDE5I) influence age related mortality in diabetic men.METHODS We studied 857 diabetic men screened for the BLAST study, stratifying them(mean follow-up = 3.8 years) into:(1) Normal T levels/untreated(total T > 12 nmol/L and free T > 0.25 nmol/L), Low T/untreated and Low T/treated;(2) PDE5I/untreated and PDE5I/treated; and(3) statin/untreated and statin/treated groups. The relationship between age and mortality, alone and with T/TRT, statin and PDE5 I treatment was studied using logistic regression. Mortality probability and 95%CI were calculated from the above models for each individual. RESULTS Age was associated with mortality(logistic regression, OR = 1.10, 95%CI: 1.08-1.13, P < 0.001). With all factors included, age(OR = 1.08, 95%CI: 1.06-1.11, P < 0.001), Low T/treated(OR = 0.38, 95%CI: 0.15-0.92, P = 0.033), PDE5I/treated(OR = 0.17, 95%CI: 0.053-0.56, P = 0.004) and statin/treated(OR = 0.59, 95%CI: 0.36-0.97, P = 0.038) were associated with lower mortality. Age related mortality was as described by Gompertz, r2 = 0.881 when Ln(mortality) was plotted against age. The probability of mortality and 95%CI(from logistic regression) of individuals, treated/untreated with the drugs, alone and in combination was plotted against age. Overlap of 95%CI lines was evident with statins and TRT. No overlap was evident with PDE5 I alone and with statins and TRT, this suggesting a change in the relationship between age and mortality. CONCLUSION We show that statins, PDE5 I and TRT reduce mortality in diabetes. PDE5 I, alone and with the other treatments significantly alter age related mortality in diabetic men. 展开更多
关键词 2 糖尿病 死亡 Gompertz-Makeham 方程 phosphodiesterase 5 禁止者 男性腺机能减退 STATINS 睾丸激素代替治疗
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磷酸二酯酶5在心力衰竭中作用的研究进展
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作者 杨洋 张雅茸 +2 位作者 杨红琴 王婧 赵红梅 《基础医学与临床》 CAS 2024年第5期724-728,共5页
磷酸二酯酶5(PDE5)是环磷酸鸟苷(cGMP)特异性水解酶,是由一氧化氮(NO)激活的可溶性鸟苷酸环化酶(sGC)靶向cGMP产生的。PDE5催化cGMP中磷酸二酯键的水解,从而将cGMP转化为无活性的5′-GMP形式,cGMP-PKG轴功能障碍将引起心脏重塑,是心力衰... 磷酸二酯酶5(PDE5)是环磷酸鸟苷(cGMP)特异性水解酶,是由一氧化氮(NO)激活的可溶性鸟苷酸环化酶(sGC)靶向cGMP产生的。PDE5催化cGMP中磷酸二酯键的水解,从而将cGMP转化为无活性的5′-GMP形式,cGMP-PKG轴功能障碍将引起心脏重塑,是心力衰竭(HF)的主要原因之一。但PDE5抑制剂治疗心力衰竭的临床疗效存在争议。本文总结了近年来PDE5在心力衰竭中的作用机制和研究进展,对未来临床应用PDE5靶向治疗心力衰竭具有重要的指导意义。 展开更多
关键词 心力衰竭 磷酸二酯酶5 磷酸二酯酶抑制剂 环磷酸鸟苷
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磷酸二酯酶-5型抑制剂与五羟色胺再摄取抑制剂治疗勃起功能障碍合并早泄疗效及安全性Meta分析 被引量:1
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作者 苗德雨 王祖龙 +1 位作者 张宸铭 万雯熙 《现代泌尿外科杂志》 CAS 2023年第10期888-893,共6页
目的评价单独使用磷酸二酯酶-5型(PDE5)抑制剂或联合五羟色胺再摄取抑制剂(SSRIs)对比单独应用SSRIs治疗勃起功能障碍(ED)与早泄(PE)共病的疗效与安全性。方法检索下述网站:知网、PubMed、Web of Science、Embase、万方、维普数据库、... 目的评价单独使用磷酸二酯酶-5型(PDE5)抑制剂或联合五羟色胺再摄取抑制剂(SSRIs)对比单独应用SSRIs治疗勃起功能障碍(ED)与早泄(PE)共病的疗效与安全性。方法检索下述网站:知网、PubMed、Web of Science、Embase、万方、维普数据库、中国生物医学文献服务系统、中华医学期刊,自建库起至2022年11月,单独使用PDE5抑制剂或联合SSRIs对比单独应用SSRIs治疗ED与PE共病的随机对照试验,用Revman 5.4.1软件分析阴道内射精潜伏期(IELT)、国际勃起功能指数5项问卷(IIEF-5)评分及不良反应率。结果最终纳入文献9篇,涉及793例患者。Meta分析显示:与单独应用SSRIs治疗ED与PE共病相比,单独使用PDE5抑制剂或联合SSRIs治疗后患者IELT更高[MD=1.99,95%CI(1.51~2.46),P<0.001]、IIEF-5评分更高[MD=4.61,95%CI(3.68~5.55),P<0.001],不良反应无统计学差异[RR=0.99,95%CI(0.74~1.31),P=0.92]。结论治疗ED与PE共病患者时,应优先治疗ED或同时治疗ED和PE,在ED和PE方面都能获得更好的治疗效果,同时不良反应也没有增加。 展开更多
关键词 勃起功能障碍 早泄 META分析 5型磷酸二酯酶抑制剂 五羟色胺再摄取抑制剂
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PDE-5i联合AVSS RigiScan检测对ED患者特征及PCDU综合评估的分析 被引量:1
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作者 黄十佳 马玲 《中国循证心血管医学杂志》 2023年第3期357-360,363,共5页
目的采用阴茎血流彩色多普勒超声(PCDU)对磷酸二酯酶5抑制剂(PDE-5i)联合听视觉性刺激(AVSS)阴茎硬度测量仪(RigiScan)检测异常的阴茎勃起功能障碍(ED)患者特征进行综合评估,探讨PCDU在ED评估中的临床价值。方法选择2014年1月至2021年1... 目的采用阴茎血流彩色多普勒超声(PCDU)对磷酸二酯酶5抑制剂(PDE-5i)联合听视觉性刺激(AVSS)阴茎硬度测量仪(RigiScan)检测异常的阴茎勃起功能障碍(ED)患者特征进行综合评估,探讨PCDU在ED评估中的临床价值。方法选择2014年1月至2021年10月就诊于中国中医科学院西苑医院男科诊断为ED且行PDE-5i联合AVSS的RigiScan检测结果为异常的患者共1477例,平均年龄(36.16±9.39)岁,平均病程(33±9.12)月,所有患者均完成PCDU检查。结果根据PCDU诊断标准将受检者分为四组:非血管性ED组611例(41%)、动脉性ED组266例(18%)、静脉性ED组375例(26%)和动静脉混合性ED组225例(15%),对四组患者一般特征及各项PCDU指标进行多组间比较。其中,除各组间病程无统计学差异外,各组间年龄、右侧阴茎海绵体动脉收缩期峰值流速(PSV)、右侧舒张末期流速(EDV)、右侧阻力指数(RI)、左侧PSV、左侧EDV、左侧RI比较均有统计学差异(P<0.05)。结论药物联合AVSS的RigiScan检测虽具有简便、可重复性等特点,但不能很好地区分非血管性ED和血管性ED,临床上仍需结合PCDU检查对血管性ED进一步诊断。年龄是血管性ED病情趋于加重的独立风险因素。 展开更多
关键词 勃起功能障碍 彩色多普勒超声 磷酸二酯酶5抑制剂 听视觉性刺激
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新型磷酸二酯酶5抑制剂CPD1对四氯化碳诱导的肝纤维化小鼠治疗作用 被引量:1
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作者 封文斌 杨建钦 +6 位作者 陈心慧 谢中莲 张莹莹 陈颖禧 赵子建 穆云萍 李芳红 《中国药理学通报》 CAS CSCD 北大核心 2023年第3期470-476,共7页
目的探讨新型磷酸二酯酶5抑制剂CPD1对四氯化碳(carbon tetrachloride,CCl 4)诱导的肝纤维化小鼠肝组织结构损伤和肝星状细胞(hepatic stellate cells,HSCs)活化的影响。方法SPF级雄性C57BL/6 J小鼠随机分为正常对照组、模型组、CPD1治... 目的探讨新型磷酸二酯酶5抑制剂CPD1对四氯化碳(carbon tetrachloride,CCl 4)诱导的肝纤维化小鼠肝组织结构损伤和肝星状细胞(hepatic stellate cells,HSCs)活化的影响。方法SPF级雄性C57BL/6 J小鼠随机分为正常对照组、模型组、CPD1治疗组、他达拉非治疗组,模型组和治疗组小鼠腹腔注射CCl 4(每周2次)。造模4周后治疗组分别给予CPD1(2 mg·kg^(-1)·d^(-1))、他达拉非(10 mg·kg^(-1)·d^(-1))灌胃治疗,持续4周。模型到期后,通过组织病理学染色、免疫荧光技术观察CPD1治疗对肝纤维化小鼠肝形态、组织结构损伤、胶原沉积及HSCs活化标志物α平滑肌肌动蛋白(α-smooth muscle actin,α-SMA)、人肝星状细胞系LX-2细胞中纤维连接蛋白(fibronectin)表达和分布的影响。结果与正常组相比,模型组小鼠肝组织出现肝细胞坏死,炎症细胞浸润增加,肝小叶结构破坏,汇管区出现胶原沉积,α-SMA表达和分布明显增加;CPD1治疗可明显减轻模型小鼠肝组织损伤程度,减少肝细胞坏死和炎症细胞浸润,减轻胶原纤维的沉积,降低α-SMA的表达及分布,且治疗效果优于他达拉非;同时CPD1明显抑制LX-2细胞中转化生长因子-β1(TGF-β1)诱导的fibronectin和PAI-1蛋白的表达。结论磷酸二酯酶5抑制剂CPD1通过抑制HSCs的激活,减少肝组织中胶原纤维蛋白的产生,延缓肝纤维化的进展。 展开更多
关键词 磷酸二酯酶5抑制剂 CPD1 肝纤维化 肝星状细胞 四氯化碳 激活
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新型磷酸二酯酶5抑制剂CPD1对单侧输尿管梗阻引起的肾间质纤维化小鼠治疗作用 被引量:1
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作者 刘傲璐 任倩 +6 位作者 封文斌 李斌 陈心慧 李思蓉 赵子建 穆云萍 李芳红 《中国药理学通报》 CAS CSCD 北大核心 2023年第1期147-152,共6页
目的探讨新型磷酸二酯酶5抑制剂CPD1对单侧输尿管梗阻(unilateral ureteric obstruction,UUO)诱导的肾纤维化小鼠肾脏组织结构损伤及间质纤维化的影响。方法8周龄♂C57BL/6 J小鼠随机分为假手术组、模型组、CPD1治疗组,手术结扎模型组... 目的探讨新型磷酸二酯酶5抑制剂CPD1对单侧输尿管梗阻(unilateral ureteric obstruction,UUO)诱导的肾纤维化小鼠肾脏组织结构损伤及间质纤维化的影响。方法8周龄♂C57BL/6 J小鼠随机分为假手术组、模型组、CPD1治疗组,手术结扎模型组和治疗组小鼠左侧输尿管,假手术组仅分离输尿管而不结扎。造模2 h后,给予CPD1(5 mg·kg^(-1)·d^(-1))灌胃治疗,持续7 d。通过组织病理学染色和Western blot,观察CPD1治疗对UUO小鼠患侧肾脏组织结构病变和纤维化标志蛋白:纤维连接蛋白(fibronectin,FN)、α平滑肌肌动蛋白(α-SMA)、Ⅰ型胶原(collagen-Ⅰ)、肾损伤分子-1(kidney injury molecule 1,Kim-1)表达及分布的影响。结果与假手术组相比,UUO组小鼠患侧肾组织中肾小管扩张,可见明显空泡变性,炎症浸润增加,FN、α-SMA、collagen-I及Kim-1蛋白的表达明显增加(P<0.05);CPD1可明显改善UUO模型小鼠患侧肾脏的结构,降低胶原纤维蛋白的沉积,纤维化标志蛋白FN、α-SMA、collagen-I及Kim-1的表达均得到明显抑制(P<0.05)。结论磷酸二酯酶5抑制剂CPD1通过下调细胞外基质ECM的沉积,减少Kim-1介导的肾损伤,改善输尿管梗阻诱导的肾间质纤维化,其具体的作用机制还有待进一步研究。 展开更多
关键词 磷酸二酯酶5抑制剂 CPD1 肾间质纤维化 单侧输尿管梗阻 胶原沉积 肾损伤
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新型磷酸二酯酶5抑制剂CPD1对百草枯诱导的肺纤维化大鼠治疗作用
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作者 高洁 杨建钦 +5 位作者 邱浩恒 张静 赵子建 李芳红 穆云萍 吴健 《中国药理学通报》 CAS CSCD 北大核心 2023年第6期1136-1142,共7页
目的探讨新型磷酸二酯酶5抑制剂CPD1对百草枯(paraquat,PQ)诱导的肺纤维化大鼠肺组织病理结构损伤和上皮-间质转化(epithelial-mesenchymal transition,EMT)的影响。方法模型组和治疗组大鼠腹腔注射PQ(30 mg·kg^(-1)),2 h后分别灌... 目的探讨新型磷酸二酯酶5抑制剂CPD1对百草枯(paraquat,PQ)诱导的肺纤维化大鼠肺组织病理结构损伤和上皮-间质转化(epithelial-mesenchymal transition,EMT)的影响。方法模型组和治疗组大鼠腹腔注射PQ(30 mg·kg^(-1)),2 h后分别灌胃CPD1(5 mg·kg^(-1)·d^(-1))、尼达尼布(50 mg·kg^(-1)·d^(-1)),持续4周。观察CPD1治疗对肺纤维化大鼠肺组织病理结构损伤、胶原沉积及EMT标志物α平滑肌肌动蛋白(α-SMA)和E-钙黏蛋白(E-cadherin)表达的影响。结果模型组大鼠肺组织指数明显增大,肺泡塌陷和扩张弥漫性分布,肺泡壁及肺泡间隔均增厚,肺间质胶原沉积增多,E-cadherin表达降低,而α-SMA和纤维连接蛋白表达增加(P<0.01);CPD1治疗可明显减轻模型大鼠肺组织病理结构损伤程度,减少肺泡塌陷和扩张,减轻胶原纤维的沉积,上调E-cadherin表达,降低α-SMA和fibronectin的表达(P<0.01)。结论CPD1可能通过抑制EMT和炎症,减少肺组织间质胶原纤维的产生,减缓PQ引起的肺纤维化进展。 展开更多
关键词 磷酸二酯酶5抑制剂 CPD1 肺纤维化 肺泡上皮细胞 上皮-间质转化 百草枯
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保健食品中西地那非等PDE-5i检测方法研究进展
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作者 李少元 接强 +5 位作者 栾玉静 董颖 崔冠峰 黄健 孙晓宇 王芳琳 《刑事技术》 2023年第3期221-227,共7页
5型磷酸二酯酶(PDE-5)是生物体内专一水解细胞内环磷酸鸟苷(cGMP)的关键因子,具有调节血管张力、传导视觉信号、调控能量代谢等作用。5型磷酸二酯酶抑制剂(PDE-5i)作为选择性抑制磷酸二酯酶活性的一类药物,可用于改善勃起功能障碍、治... 5型磷酸二酯酶(PDE-5)是生物体内专一水解细胞内环磷酸鸟苷(cGMP)的关键因子,具有调节血管张力、传导视觉信号、调控能量代谢等作用。5型磷酸二酯酶抑制剂(PDE-5i)作为选择性抑制磷酸二酯酶活性的一类药物,可用于改善勃起功能障碍、治疗肺动脉高压等疾病,在临床上广泛应用。一些不法商家向保健食品中非法添加PDE-5i及其类似物以达到其声称的保健效果,严重危害消费者健康。本文综述了保健食品中非法添加PDE-5i及其类似物的常用检测方法,包括理化快速筛查法、酶联免疫法、胶体金免疫层析法、近红外光谱法、拉曼光谱法、离子迁移谱法、薄层色谱及其联用法、液相色谱法、液相色谱-质谱联用法等,并介绍了各个方法的特点,为市场监管部门和公安机关打击食品药品违法犯罪行为提供技术支撑。 展开更多
关键词 保健食品 5型磷酸二酯酶抑制剂(PDE-5i) 西地那非 检测方法
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Influence of erectile dysfunction course on its progress and efficacy of treatment with phosphodiesterase type 5 inhibitors 被引量:4
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作者 LIU De-feng JIANG Hui HONG Kai ZHAO Lian-ming TANG Wen-hao MA Lu-lin 《Chinese Medical Journal》 SCIE CAS CSCD 2010年第22期3258-3261,共4页
Background Erectile dysfunction (ED) is a common impairment among older men, and the prevalence rates increase sharply after age of 60 years. Most studies have focused on the prevalence rate or dangerouse factors. T... Background Erectile dysfunction (ED) is a common impairment among older men, and the prevalence rates increase sharply after age of 60 years. Most studies have focused on the prevalence rate or dangerouse factors. The aim of this study was to investigate the basic epidemiologic data about ED patients with different ED courses. The purpose of this researth was to understand the therapeutic effect of phosphodiesterase type 5 inhibitor (PDE5-1) and see how and why the ED course impact the progress of ED and the therapeutic effect of PDE5-1 treatment. Methods From June 2008 to June 2009, 4252 questionnaires (Quality of Erection Questionnaire, QEQ) were gathered from 46 centers by urology or andrology doctors all around China. Patients with ED (age 〉 20 years) filled in first half of the questionnaires when they came for the first time, and then completed the second half 4 weeks after PDE5-1 therapy. Results ED courses of most patients were less than 5 years (〈5 years, 74.0%; 5-10 years 20.8%; 〉10 years, 5.2%). As ED course increasing, the incidence of the risk factors of ED, such as smoking, drinking, hypertension, diabetes, heart disease and hyperlipidemia also increase (P 〈0.01). PDES-I was effective in improving the quality of sexual activities (P 〈0.01). Administration of PDE5-1 improves satisfaction, enjoyment and frequency of sexual activities. The longer the ED course, the worse the therapeutic effect (〈5 years, 96.1%; 5-10 years, 94.9%; 〉10 years, 89.0%) (P 〈0.01). Conclusions The ED course greatly affected the therapeutic effect of PDE5-1, the patients with ED should consult doctor at early stage of the disease. Admistration of PDE5-1 effectively improves the penile erection and the quality of sexual life of the patients hence should be considered as first-line medicine in the treatment of ED. 展开更多
关键词 erectile dysfunction course phosphodiesterase type 5 inhibitor international index oferectile function
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Clinical and preclinical treatment of urologic diseases with phosphodiesterase isoenzymes 5 inhibitors: an update 被引量:2
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作者 Wen-Hao Zhang Xin-Hua Zhang 《Asian Journal of Andrology》 SCIE CAS CSCD 2016年第5期723-731,共9页
Phosphodiesterase isoenzymes 5 inhibitors (PDE5-1s) are the first-line therapy for erectile dysfunction (ED). The constant discoveries of nitric oxide (NO)/cyclic guanosine monophosphate (cGMP) cell-signaling ... Phosphodiesterase isoenzymes 5 inhibitors (PDE5-1s) are the first-line therapy for erectile dysfunction (ED). The constant discoveries of nitric oxide (NO)/cyclic guanosine monophosphate (cGMP) cell-signaling pathway for smooth muscle (SM) control in other urogenital tracts (UGTs) make PDE5-1s promising pharmacologic agents against other benign urological diseases. This article reviews the literature and contains some previously unpublished data about characterizations and activities of PDE5 and its inhibitors in treating urological disorders. Scientific discoveries have improved our understanding of cell-signaling pathway in NO/cGMP-mediated SM relaxation in UGTs. Moreover, the clinical applications of PDE5-1s have been widely recognized. On-demand PDE5-1s are efficacious for most cases of ED, while daily-dosing and combination with testosterone are recommended for refractory cases. Soluble guanylate cyclase (sGC) stimulators also have promising role in the management of severe ED conditions. PDE5-1s are also the first rehabilitation strategy for postoperation or postradiotherapy ED for prostate cancer patients. PDE5-1s, especially combined with (z-adrenoceptor antagonists, are very effective for benign prostatic hyperplasia (BPH) except on maximum urinary flow rate (Qmax) with tadalafil recently proved for BPH with/without ED. Furthermore, PDE5-1s are currently under various phases of clinical or preclinical researches with promising potential for other urinary and genital illnesses, such as priapism, premature ejaculation, urinary tract calculi, overactive bladder, Peyronie's disease, and female sexual dysfunction. Inhibition of PDE5 is expected to be an effective strategy in treating benign urological diseases. However, further clinical studies and basic researches investigating mechanisms of PDE5-1s in disorders of UGTs are required. 展开更多
关键词 benign prostatic hyperplasia erectile dysfunction overactive bladder phosphodiesterase isoenzymes 5 inhibitor PRIAPISM smooth muscle
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Systematic review and meta-analysis on phosphodiesterase 5 inhibitors and α-adrenoceptor antagonists used alone or combined for treatment of LUTS due to BPH 被引量:1
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作者 Xing-Huan Wang Xiao Wang Ming-Jun Shi Sheng Li Tao Liu Xin-Hua Zhang 《Asian Journal of Andrology》 SCIE CAS CSCD 2015年第6期1022-1032,I0012,共12页
The aim of this systematic review is to determine the comparative effectiveness and safety of phosphodiesterase 5 inhibitors (PDE5-1s) and (x-blockers used alone or combined for the treatment of lower urinary tract... The aim of this systematic review is to determine the comparative effectiveness and safety of phosphodiesterase 5 inhibitors (PDE5-1s) and (x-blockers used alone or combined for the treatment of lower urinary tract symptoms (LUTS) due to benign prostatic hyperplasia (BPH). An electronic search of PubMed, Cochrane Library and Embase up to January 2014 was performed to identify randomized controlled trials comparing the efficacy and safety of PDE5-Is and (x-blockers for treatment of lower urinary tract symptoms due to benign prostatic hyperplasia, which assessed IPSS score, maximum flow rate, postvoided residual urine, quality of life and Erectile Function (IIEF) score as outcomes. Data were analyzed by fixed or random effect models using Cochrane Collaboration review manager software. A total of 12 studies were included, Our novel data demonstrated that there was a trend that (x-blockers were more efficacious than PDE5-Is on decreasing IPSS score and increasing maximum flow rate. (x-blockers were significantly more effective than PDE5-Is on reduction of postvoided residual urine with a mean difference of 3.67 (95% CI 1.56 to 5.77, P = 0.0006) and PDE5-Is showed greater effect than (x-blockers on increasing IIEF score with a mean difference of 9.82 (95% CI 3.80 to 15.85, P = 0.001). In conclusion, our novel data demonstrated that PDE5-Is plus ABs ranked the highest on the improvement of LUTS/BPH. PDE5-Is monotherapy was also effective in this kind of disorder except less reduction of PVR than ABs, In addition, both combined- or mono-therapy were safe. 展开更多
关键词 benign prostatic hyperplasia lower urinary tract symptoms META-ANALYSIS phosphodiesterase 5 inhibitors -adrenoceptorantagonists
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A meta-regression evaluating the effectiveness and prognostic factors of oral phosphodiesterase type 5 inhibitors for the treatment of erectile dysfunction
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作者 Jin-Qiu Yuan Chen Mao +3 位作者 Zu-Yao Yang Xiao-Hong Fu Samuel Y Wong Jin-Ling Tang 《Asian Journal of Andrology》 SCIE CAS CSCD 2016年第1期60-65,共6页
The effectiveness of phosphodiesterase type 5 inhibitors (PDE5-1s) for erectile dysfunction (ED) varies considerably among trials, but available studies investigating the factors that affect the effectiveness are ... The effectiveness of phosphodiesterase type 5 inhibitors (PDE5-1s) for erectile dysfunction (ED) varies considerably among trials, but available studies investigating the factors that affect the effectiveness are few and findings are not consistent. A systematic search was performed in PubMed, Cochrane Library, and EMBASE to identify randomized controlled trials comparing PDE5-1s with placebo for the treatment of ED. The methodological quality of included studies was assessed by the Cochrane Collaboration's tool for assessing risk of bias. The associations between prespecified study-level factors and effectiveness were tested by a random effects meta-regression model. This study included 93 trials with 26 139 patients. When all PDE5-1s were grouped together, Caucasian ethnicity was associated with 15.636% (95% confidence interval [CI]: 0.858% to 32.579%) increase in risk ratio (RR) for Global Assessment Questionnaire question-1 (GAQ-1), and 1.473 (95% CI: 0.406 to 2.338) score increase in mean difference (MD) for posttreatment International Index of Erectile Function-Erectile Function domain score (IIEF-EF), compared to Asian ethnicity. A one-score increase in baseline IIEF-EF was associated with -5.635% (95% CI: -9.120% to -2.017%) reduction in RR for GAQ-1, and -0.229 (95% CI: -0.425 to -0.042) score decrease in MD for posttreatment IIEF-EF. In conclusion, PDE5-1s are more effective in Caucasians than Asians, and in patients with more severe ED. 展开更多
关键词 erectile dysfunction META-REGRESSION phosphodiesterase type 5 inhibitors systematic review
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糖尿病勃起功能障碍患者服用PDE5抑制剂的疗效及安全性Meta分析 被引量:15
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作者 刘庆 蔡健 +2 位作者 林礼彰 李澄棣 武志刚 《中华男科学杂志》 CAS CSCD 北大核心 2015年第5期447-457,共11页
目的:系统评价磷酸二酯酶5(PDE5)抑制剂治疗糖尿病患者勃起功能障碍的临床疗效及安全性,为其治疗提供临床证据。方法:通过计算机检索2013年12月以前Medline、Embase、Cocbrane Library、中国学术期刊全文数据库(CNKI)、万方数据库、维... 目的:系统评价磷酸二酯酶5(PDE5)抑制剂治疗糖尿病患者勃起功能障碍的临床疗效及安全性,为其治疗提供临床证据。方法:通过计算机检索2013年12月以前Medline、Embase、Cocbrane Library、中国学术期刊全文数据库(CNKI)、万方数据库、维普数据库(VIP)、浙江省高校数字图书馆(ZADL),并阅读检索文章及参考文献,纳入PDE5抑制剂治疗糖尿病患者勃起功能障碍的随机对照试验(RCT)。对纳入研究的方法学用Jadad量表评价,以国际勃起功能指数(IIEF-EF)、IIEF第3问题(IIEF-Q3)、IIEF第4问题(IIEF-Q4)、阴茎插入成功率(SEP-2)、完成性交成功率(SEP-3)及GAQ总体评价问卷为主要疗效评价指标。采用Review manager 5.1.0软件进行Meta分析。结果:共有13篇研究被纳入,所有纳入研究Jadad评分均为3分以上高质量试验。10篇文献IIEF-EF评分采用固定效应模型Meta分析,合并WMD=5.79,95%CI为(4.91,6.66),P<0.001。6篇文献IIEF-Q3评分采用固定效应模型Meta分析,合并WMD=0.96,95%CI为(0.83,1.08),P<0.001。6篇文献IIEF-Q4评分采用固定效应模型Meta分析,合并WMD=1.11,95%CI为(0.98,1.25),P<0.001。2篇文献SEP-2评分采用固定效应模型Meta分析,合并WMD=20.08,95%CI为(13.76,26.04),P<0.001。5篇文献SEP-3评分采用固定效应模型Meta分析,合并WMD=25.56,95%CI为(22.24,28.80),P<0.001。11篇文献GAQ评分采用随机效应模型Meta分析,OR=6.20,95%CI为(3.65,10.52),P<0.001。11个试验药物不良反应采用随机效应模型Meta分析,OR=7.43,95%CI为(4.11,13.44),P<0.001。结论:PDE-5抑制剂能安全有效地改善男性糖尿病患者的勃起功能。 展开更多
关键词 磷酸二酯酶5抑制剂 糖尿病 勃起功能障碍 META分析
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5型磷酸二酯酶抑制剂治疗勃起功能障碍的疗效和安全性 被引量:17
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作者 沈周俊 余燕岚 《中华男科学杂志》 CAS CSCD 2005年第8期631-634,共4页
5型磷酸二酯酶抑制剂使用方便、高效、不良反应小,是治疗勃起功能障碍的一线药物。西地那非自1998年面世以来,是目前研究最透彻的5型磷酸二酯酶抑制剂。临床试验主要针对不同患者群体,包括合并有心血管疾病、糖尿病、抑郁症、前列腺根... 5型磷酸二酯酶抑制剂使用方便、高效、不良反应小,是治疗勃起功能障碍的一线药物。西地那非自1998年面世以来,是目前研究最透彻的5型磷酸二酯酶抑制剂。临床试验主要针对不同患者群体,包括合并有心血管疾病、糖尿病、抑郁症、前列腺根治术后和透析治疗等特殊人群,进行疗效和安全性研究。不良反应多为轻中度,主要表现为头痛、面部潮红、消化不良和短暂的视觉障碍。本文就5型磷酸二酯酶抑制剂治疗勃起功能障碍的疗效和安全性作一综述。 展开更多
关键词 勃起功能障碍 5型磷酸二酯酶抑制剂 西地那非 有效性 安全性
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