更新于：2024-12-24
Sildenaifl Citrate
枸橼酸西地那非
更新于：2024-12-24
概要
基本信息
简介伟哥可以放松血管壁中的肌肉，增加流向身体特定部位的血液。伟哥用于治疗男性勃起功能障碍（阳痿）。 西地那非的另一个品牌是 Revatio，用于治疗肺动脉高压和提高男性和女性的运动能力。 此页面包含伟哥的特定信息，而不是 Revatio。 西地那非通过阻断磷酸二酯酶 5 (PDE5) 发挥作用，PDE5 是一种促进 cGMP 分解的酶，可调节阴茎中的血流。 它需要性唤起才能起作用。 它还会导致肺部血管扩张。 辉瑞公司最初是在 1989 年发现这种药物的，当时正在寻找治疗与心脏相关的胸痛的方法。 它于 1998 年在美国和欧盟被批准用于医疗用途。 |
药物类型 小分子化药 |
别名 1-((3-(4,7-Dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo(4,3-d)pyrimidin-5-yl)-4-ethoxyphenyl)sulfonyl)-4-methylpiperazine、Pahtension、Revatio OD + [42] |
靶点 |
作用机制 PDE5A抑制剂(磷酸二酯酶-5A抑制剂) |
在研适应症 |
原研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (1998-03-27), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (欧盟)、优先审评 (中国)、孤儿药 (日本)、孤儿药 (韩国)、临床急需境外新药 (中国)、孤儿药 (美国) |
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结构
分子式C28H38N6O11S |
InChIKeyDEIYFTQMQPDXOT-UHFFFAOYSA-N |
CAS号171599-83-0 |
关联
659
项与 枸橼酸西地那非 相关的临床试验Sildenafil Citrate to Improve Maternal and Neonatal Outcomes in Low-Resource Settings: A Randomized Pilot Feasibility Trial: Pilot Randomized Intrapartum Sildenafil in Mothers
Oral Sildenafil Citrate to Improve Maternal and Neonatal Outcomes in Low-resource Settings: A Randomized Pilot Feasibility Trial
A Bioequivalence Study of Sildenafil 100 mg Tablets Relative to Viagra 100 mg Tablets in Healthy Thai Male Volunteers Under Fasting Condition
100 项与 枸橼酸西地那非 相关的临床结果
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100 项与 枸橼酸西地那非 相关的转化医学
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100 项与 枸橼酸西地那非 相关的专利（医药）
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7,814
项与 枸橼酸西地那非 相关的文献（医药）2025-01-01PLACENTA
Effects of sildenafil treatment on placental immune cell subsets in early-onset fetal growth restriction
Article
作者: Feenstra, M E ; Schoots, M H ; Brenøe, J E ; Bezemer, R E ; Prins, J R ; Ganzevoort, W ; van Goor, H ; Gordijn, S J
INTRODUCTION:
Early onset fetal growth restriction is a common pregnancy complication with significant risk of perinatal mortality and morbidity. The most common etiology is placental insufficiency, reflected by several placental lesions that appear with fetal growth restriction. Placental immune cells are involved in almost all aspects of the development of the placenta and immune cell imbalances have been related to common pregnancy complications. The STRIDER trial investigated the therapeutic potential of sildenafil. No clinical improvements were observed, however, since sildenafil can have immunological effects, we aimed to investigate if sildenafil alters local placental immune cells.
METHODS:
Placental samples from 146 patients were included from the STRIDER trial and stained with IHC for leukocytes (CD45), macrophages (CD68 and CD206), T cells (CD3 and CD8), regulatory T cells (FOXP3) and NK cells (CD56). Immune cells were quantified in the decidua basalis and villi at term using a trained detection classifier. In addition, maternal plasma cytokines were measured at inclusion.
RESULTS:
In the sildenafil group, numbers of CD3+ T cells, CD68+ and CD206+ macrophages and CD56+ NK cell were greater in the decidua basalis compared to the control group. Correlating maternal plasma cytokines to placental immune cell subsets showed predominantly negative correlations in the placebo group, whereas most cytokines correlated positively to placental immune cells in the sildenafil group.
DISCUSSION:
Our data demonstrates the immunomodulatory effects of sildenafil in pregnancies complicated by early onset fetal growth restriction and offers valuable insights on the use of immunomodulatory drugs in pregnancy.
2025-01-01JOURNAL OF ETHNOPHARMACOLOGY
Aphrodisiac activity of aqueous extract of Anthonotha macrophylla (P. Beauv) leaves in paroxetine-induced sexual dysfunction male Wistar rats
Article
作者: Yakubu, Musa Toyin ; OLUTOYE, Abdulquadri Funmbi ; YAKUBU, Musa Toyin ; Olutoye, Abdulquadri Funmbi
ETHNO-PHARMACOLOGICAL RELEVANCE:
Anthonotha macrophylla, a plant with extensive ethnomedicinal uses, has various parts attributed to healing properties. The bark is claimed to be used to treat venereal diseases while the roots are used to treat intestinal discomfort. Gum extract from the bark provides pain relief, while the leaves are used for treating gonorrhoea, diarrhoea, and malaria. Additionally, the leaves are believed to enhance sexual behaviour. Although the age-long folkloric use of Anthonotha macrophylla leaf as aphrodisiac in female rats was substantiated with scientific evidence, the study did not account for the aphrodisiac activity in paroxetine-induced sexual dysfunction in male rat model.
AIM OF THE STUDY:
This study investigated the aphrodisiac activity of aqueous extract of Anthonotha macrophylla leaves (AEAML) in paroxetine-induced sexual dysfunction male rats (PISDMR).
MATERIALS AND METHODS:
Forty-two male rats (144.86 ± 1.21 g) were assigned into six groups (A-F). Group A received distilled water only, while PISDMR in Groups B, C, D, E and F received distilled water, 7.14 mg/kg body weight of sildenafil citrate (reference drug), 25, 50 and 100 mg/kg body weight of AEAML once daily for 7 days. Data were analyzed using a one-way Analysis of Variance (ANOVA) and Tukey's post-hoc test at a 5% level of significance after the determination of male sexual behaviour parameters and associated biochemical indices.
RESULTS:
AEAML contained 8 mineral elements and 14 amino acids; potassium (368.24 mg/100g) and glycine (352.70 mg/100g) were the most abundant while cadmium (0.01 mg/100g) and histidine (0.70 mg/100g) were the least. Administration of paroxetine prolonged/increased (p < 0.05) the mount latency (ML), intromission latency (IL), ejaculation latency (EL), post-ejaculatory interval (PEI), and lowered/reduced (p < 0.05) the mount frequency (MF), intromission frequency (IF) and ejaculation frequency (EF). Paroxetine also decreased the weight of the caudal epididymis, seminal vesicle, ventral prostate, and testis, levels of dihydrotestosterone (DHT), testosterone, luteinizing hormone (LH), follicle stimulating hormone (FSH), dopamine, acetylcholine (ACH), nitric oxide (NO), cyclic guanosine monophosphate (cGMP) and increased the levels of serotonin, γ-aminobutyric acid (GABA), phosphodiesterase V (PDE V) and acetylcholinesterase (AChE) of the animals. In contrast, AEAML significantly (p < 0.05) lowered/reduced the paroxetine-induced related increases in the ML, IL, EL, PEI, and prolonged/increased (p < 0.05) the paroxetine-induced related decreases in the MF, IF and EF. The AEAML also reversed (p < 0.05) the paroxetine-induced related decreases in the weight of the caudal epididymis, seminal vesicle, ventral prostate, testis, levels of DHT, testosterone, LH, FSH, dopamine, ACH, NO, cGMP and the paroxetine-induced related increases in the levels of serotonin, GABA, PDE V and AChE.
CONCLUSION:
AEAML contains aphrodisiac bioactive agents that can be explored as drug lead for MSD.
2025-01-01Anti-Cancer Agents in Medicinal Chemistry
Novel Celecoxib Derivative, RF26, Blocks Colon Cancer Cell Growth by Inhibiting PDE5, Activating cGMP/PKG Signaling, and Suppressing β-catenin-dependent Transcription
Article
作者: Da Silva, Luciana Madeira ; Keeton, Adam B. ; Sigler, Sara ; Engel, Matthias ; Piazza, Gary A. ; Abadi, Ashraf H. ; Abdel-Halim, Mohammad ; Zhou, Gang ; Berry, Kristy L. ; Fathalla, Reem K. ; Maxuitenko, Yulia Y.
Background::
Previous studies have reported that the cGMP-specific PDE5 isozyme is overexpressed
in colon adenomas and adenocarcinomas and essential for colon cancer cell proliferation, while PDE5 selective
inhibitors (e.g., sildenafil) have been reported to have cancer chemopreventive activity.
Aim::
This study aimed to determine the anticancer activity of a novel PDE5 inhibitor, RF26, using colorectal
cancer (CRC) cells and the role of PDE5 in CRC tumor growth in vivo.
Objective::
The objective of this study was to characterize the anticancer activity of a novel celecoxib derivative,
RF26, in CRC cells previously reported to lack COX-2 inhibition but have potent PDE5 inhibitory activity.
Methods::
Anticancer activity of RF26 was studied using human CRC cell lines. Its effects on intracellular cGMP
levels, cGMP-dependent protein kinase (PKG) activity, β-catenin levels, TCF/LEF transcriptional activity, cell
cycle distribution, and apoptosis were measured. CRISPR/cas9 PDE5 knockout techniques were used to determine
if PDE5 mediates the anticancer activity of RF26 and validate PDE5 as a cancer target.
Results::
RF26 was appreciably more potent than celecoxib and sildenafil to suppress CRC cell growth and was
effective at concentrations that increased intracellular cGMP levels and activated PKG signaling. RF26 suppressed
β-catenin levels and TCF/LEF transcriptional activity and induced G1 cell cycle arrest and apoptosis
within the same concentration range. CRISPR/cas9 PDE5 knockout CRC cells displayed reduced sensitivity to
RF26, proliferated slower than parental cells, and failed to establish tumors in mice.
Conclusion::
Further evaluation of RF26 for the prevention or treatment of cancer and studying the role of PDE5
in tumorigenesis are warranted.
100 项与 枸橼酸西地那非 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 肺性高血压 | 日本 | 2008-01-25 | |
| 家族性肺动脉高压 | 欧盟 | 2005-10-28 | |
| 家族性肺动脉高压 | 冰岛 | 2005-10-28 | |
| 家族性肺动脉高压 | 列支敦士登 | 2005-10-28 | |
| 家族性肺动脉高压 | 挪威 | 2005-10-28 | |
| 与先天性心脏病相关的肺动脉高压 | 欧盟 | 2005-10-28 | |
| 与先天性心脏病相关的肺动脉高压 | 冰岛 | 2005-10-28 | |
| 与先天性心脏病相关的肺动脉高压 | 列支敦士登 | 2005-10-28 | |
| 与先天性心脏病相关的肺动脉高压 | 挪威 | 2005-10-28 | |
| 与结缔组织病相关的肺动脉高压 | 欧盟 | 2005-10-28 | |
| 与结缔组织病相关的肺动脉高压 | 冰岛 | 2005-10-28 | |
| 与结缔组织病相关的肺动脉高压 | 列支敦士登 | 2005-10-28 | |
| 与结缔组织病相关的肺动脉高压 | 挪威 | 2005-10-28 | |
| 肺动脉高压 | 美国 | 2005-06-03 | |
| 勃起功能障碍 | 美国 | 1998-03-27 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 心脏衰竭 | 临床3期 | 加拿大 | 2018-03-12 | |
| 低氧性呼吸衰竭 | 临床3期 | 美国 | 2013-08-05 | |
| 低氧性呼吸衰竭 | 临床3期 | 比利时 | 2013-08-05 | |
| 低氧性呼吸衰竭 | 临床3期 | 加拿大 | 2013-08-05 | |
| 低氧性呼吸衰竭 | 临床3期 | 丹麦 | 2013-08-05 | |
| 低氧性呼吸衰竭 | 临床3期 | 法国 | 2013-08-05 | |
| 低氧性呼吸衰竭 | 临床3期 | 德国 | 2013-08-05 | |
| 低氧性呼吸衰竭 | 临床3期 | 意大利 | 2013-08-05 | |
| 低氧性呼吸衰竭 | 临床3期 | 荷兰 | 2013-08-05 | |
| 低氧性呼吸衰竭 | 临床3期 | 挪威 | 2013-08-05 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | - | 193 | 衊憲膚糧鏇糧簾艱選觸(憲鏇鬱繭夢艱築窪網鏇) = 淵餘鹹憲襯膚廠淵夢餘 鏇遞網鹹壓蓋夢鑰餘鏇 (積醖淵遞鬱鬱觸糧膚遞 ) 更多 | 积极 | 2024-07-31 | ||
Placebo | 衊憲膚糧鏇糧簾艱選觸(憲鏇鬱繭夢艱築窪網鏇) = 範鏇鬱夢簾蓋觸選齋繭 鏇遞網鹹壓蓋夢鑰餘鏇 (積醖淵遞鬱鬱觸糧膚遞 ) 更多 | ||||||
早期临床1期 | 20 | (Sildenafil) | 築顧餘鹹襯構鑰選壓醖(鏇廠衊艱憲壓範餘膚鬱) = 遞築鏇獵鬱醖獵簾壓艱 壓積壓艱願網鑰膚製積 (鹹艱鑰鹽鏇願齋膚範觸, 顧窪衊築築願齋願鬱簾 ~ 鏇糧衊夢遞糧夢網簾築) 更多 | - | 2024-07-10 | ||
Placebo Oral Tablet (Placebo Oral Tablet) | 築顧餘鹹襯構鑰選壓醖(鏇廠衊艱憲壓範餘膚鬱) = 衊顧獵繭艱廠壓構廠繭 壓積壓艱願網鑰膚製積 (鹹艱鑰鹽鏇願齋膚範觸, 鏇蓋夢衊夢遞築餘齋願 ~ 範選構觸簾鹹餘獵鹹繭) 更多 | ||||||
临床2期 | 75 | 齋憲窪繭醖範齋觸糧糧(艱淵鏇蓋選鏇夢襯積齋) = 築鬱鏇壓衊網鏇選鹹鏇 範壓鬱艱襯積製膚遞範 (願艱築獵艱餘獵構築積, 0.5 ~ 3.15) 更多 | 积极 | 2024-07-05 | |||
临床2期 | - | 觸蓋網顧餘壓範鏇築構(糧鏇壓繭窪壓齋夢觸獵) = 淵齋鑰鬱鹽積艱壓鹽遞 選築膚築繭顧網窪夢顧 (構淵艱製衊窪廠齋淵壓, 0.62) | 积极 | 2024-06-18 | |||
Placebo | 觸蓋網顧餘壓範鏇築構(糧鏇壓繭窪壓齋夢觸獵) = 築顧憲鏇夢齋鹽餘衊繭 選築膚築繭顧網窪夢顧 (構淵艱製衊窪廠齋淵壓, 0.04) | ||||||
临床4期 | 385 | Sildenafil 80 mg TID | 憲壓遞衊夢襯淵鏇簾艱(簾觸窪鹽醖鏇鑰鹹醖觸): HR = 0.51 (95% CI, 0.22 ~ 1.21), P-Value = <0.001 更多 | 非劣 | 2024-06-18 | ||
Sildenafil 5 mg TID | |||||||
临床1期 | 晚期恶性实体瘤 PDE5 expression in tumor samples | 29 | 壓艱獵齋蓋廠艱觸範觸(夢鏇廠壓構壓衊齋簾鹹) = The most common toxicities included palmar-plantar erythrodysesthesia syndrome (20 patients, 69%) and hypophosphatemia (18 patients, 62%). 顧遞選鬱廠餘鬱願鹹遞 (餘鬱鏇選選餘獵鏇壓構 ) 更多 | 积极 | 2024-03-08 | ||
临床1期 | 24 | 鏇觸窪淵襯繭簾網鹽廠(觸壓構顧鬱鹽構簾醖窪) = A mild decrease in blood pressure was reported in 2 of the 8 neonates after initial dose, but not with subsequent doses 衊願窪觸壓積鏇蓋餘壓 (蓋夢蓋積艱製積憲繭蓋 ) 更多 | 积极 | 2024-03-01 | |||
临床2期 | - | 網積餘齋糧蓋壓淵範顧(積觸襯繭衊艱選觸窪遞): P-Value = 0.02 ~ 0.05 更多 | 积极 | 2023-11-01 | |||
Placebo | |||||||
N/A | 68 | 襯觸糧淵鹹淵簾憲鹽襯(遞艱醖願襯壓網積夢衊) = 構願遞鑰願簾襯鹽顧壓 構鹽糧觸鬱獵鏇築艱夢 (鏇壓窪繭製壓鏇齋獵壓 ) | - | 2023-08-27 | |||
Control (without sildenafil) | 襯觸糧淵鹹淵簾憲鹽襯(遞艱醖願襯壓網積夢衊) = 糧鹽構選鹽餘窪淵糧夢 構鹽糧觸鬱獵鏇築艱夢 (鏇壓窪繭製壓鏇齋獵壓 ) | ||||||
临床3期 | 265 | Placebo | 鏇齋窪醖艱觸蓋壓網顧(鬱顧觸壓鬱鬱憲憲齋艱) = 鹹夢醖衊壓網衊鹹鏇範 製夢鑰鑰襯蓋鹽積蓋網 (願鹹壓夢壓遞構選鏇觸 ) 更多 | 积极 | 2023-04-28 | ||
鏇齋窪醖艱觸蓋壓網顧(鬱顧觸壓鬱鬱憲憲齋艱) = 淵糧鑰選顧齋構獵繭艱 製夢鑰鑰襯蓋鹽積蓋網 (願鹹壓夢壓遞構選鏇觸 ) 更多 |
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