预约演示
更新于：2025-07-01
Pramipexole Dihydrochloride
盐酸普拉克索
更新于：2025-07-01
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 美国 (1997-07-01), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、优先审评 (中国) |
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结构/序列
分子式C10H20ClN3OS |
InChIKeyZTZQAWQFTIVKMU-KLXURFKVSA-N |
CAS号191217-81-9 |
关联
180
项与 盐酸普拉克索 相关的临床试验NCT07022405
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An Open-Label, Randomized Controlled Trial of Pramipexole Versus Escitalopram to Treat Major Depressive Disorder (MDD) and Comorbid MDD With Mild Neurocognitive Disorder (MND) in Persons With HIV
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PKA透皮贴剂单次给药药代动力学对比研究
100 项与 盐酸普拉克索 相关的临床结果
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100 项与 盐酸普拉克索 相关的转化医学
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100 项与 盐酸普拉克索 相关的专利（医药）
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2,206
项与 盐酸普拉克索 相关的文献（医药）2025-08-01PHARMACOLOGICAL RESEARCH
Locomotor activity depends on β-arrestin recruitment by the dopamine D1 receptor in the striatal D1-D3 receptor heteromer
Article
作者: Pardo, Leonardo ; Shi, Lei ; Evans, Alexandra H ; Michaelides, Michael ; Earley, Christopher J ; Ferré, Sergi ; Casadó, Vicent ; Levinstein, Marjorie R ; Keegan, Bradley M ; Jackson, Shelley N ; Moreno, Estefanía ; Ciruela-Jardí, Marc ; Rea, William ; Bonifazi, Alessandro ; Casajuana-Martin, Nil ; Newman, Amy H ; Cai, Ning-Sheng ; Cao, Jianjing
Several dopaminergic compounds, including the clinically used pramipexole, are labelled as preferential dopamine D3 receptor (D3R) agonists based on their moderately higher affinity for the D3R versus other D2-like receptor subtypes. In rodents, these compounds typically produce locomotor depression with low doses and locomotor activation with higher doses, which has been assumed to be mediated by presynaptic D3Rs and postsynaptic striatal D2Rs, respectively. However, studies with selective pharmacological and genetic blockade of each dopamine receptor subtype suggest opposite roles. We address this apparent conundrum by performing a comprehensive in vitro, in vivo and ex vivo pharmacological comparison of several preferential D3R agonists. Their differential properties reveal that their locomotor activating effects in mice are dependent on the striatal postsynaptic D3Rs forming heteromers with D1Rs, via their ability to potentiate β-arrestin recruitment by the D1R in the D1R-D3R heteromer. The results also indicate that the locomotor depressant effects are largely dependent on their ability to activate presynaptic D2Rs. More broadly, it is demonstrated that locomotor activity in mice depends on β-arrestin recruitment by the D1R in the striatal D1R-D3R heteromer. These results can have implications for the treatment of L-dopa-induced dyskinesia and Restless Legs Syndrome.
2025-08-01REGULATORY TOXICOLOGY AND PHARMACOLOGY
Development of internal thresholds of toxicological concern (iTTC) for chemicals based on empirical exposures to pharmaceuticals
Article
作者: Terasaka, Shimpei ; Takeshita, Toshihide ; Nakagawa, Shota ; Miyazawa, Masaaki ; Nukada, Yuuko
The threshold of toxicological concern (TTC) is an approach to risk assessment that uses acceptable low-level exposure values derived from statistical information for chemicals for which insufficient toxicological information exists. Previously, the TTC for systemic toxicity was derived from the toxicological endpoints of the external dose for each administration route in animal studies. Internal TTC (iTTC), which extends the TTC concept from external to internal dosages, expands the scope of application by standardizing exposure via different routes. Information about blood exposure to pharmaceuticals used in treatment can help determine the chemical levels tolerated in humans. Using the tolerated plasma/serum blood drug concentration of the pharmaceutical as the toxicological point of departure, a new iTTC of 0.6 nM for the no effect concentration were proposed (a conservative risk assessment considers further safety margins). It is based on the 5th percentile values of the normal distribution, which approximates the cumulative empirical distribution, and an uncertainty coefficient to convert the treatment dose to the no-effect dose. Predicting blood concentrations of chemicals to which humans are exposed and comparing them to iTTC with appropriate caution can be used as an approach to risk assessment of systemic toxicity without animal-based testing.
2025-08-01SLEEP MEDICINE
Symptomatic treatment of REM sleep behavior disorder (RBD): A consensus from the international RBD study group - Treatment and trials working group
Review
作者: Schenck, Carlos H ; During, Emmanuel H ; Kunz, Dieter ; Bes, Frederik ; Malkani, Roneil ; Schiess, Mya C ; De Cock, Valerie Cochen ; Arnulf, Isabelle ; Ratti, Pietro-Luca ; Stefani, Ambra ; Videnovic, Aleksandar ; Provini, Federica
Rapid-eye-movement sleep behavior disorder (RBD) is a parasomnia causing motor behaviors and vocalizations during sleep, which can lead to injuries in patients and their bed partners. Adult-onset RBD generally precedes a neurodegenerative synucleinopathy, while other cases can be associated with antidepressant use, neurotrauma and narcolepsy. The management of RBD relies on the systematic identification of etiologic and contributing factors, implementation of safety measures, appropriate pharmacotherapy and counseling, which should be patient-centered. In this manuscript, we summarize the evidence on the management of RBD. We summarize the evidence supporting the use of clonazepam, melatonin, rivastigmine, and pramipexole, the four agents currently recommended by the American Academy of Sleep Medicine. For each agent and for alternative therapies, we discuss efficacy, dosing, adverse effects and indications. We integrate the current knowledge on therapies in RBD in treatment algorithms that can guide providers in choosing the most appropriate initial therapy, and alternative options based on the course of symptoms and comorbidities. There is a large need for additional, well tolerated therapies for reducing RBD symptoms. The last section of this manuscript discusses current challenges and unmet needs, as well as future directions in developing therapies and improving the care of patients with RBD.
100 项与 盐酸普拉克索 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 |
|---|---|---|---|
| 不宁腿综合征 | 欧盟 | 1997-10-13 | |
| 不宁腿综合征 | 冰岛 | 1997-10-13 | |
| 不宁腿综合征 | 列支敦士登 | 1997-10-13 | |
| 不宁腿综合征 | 挪威 | 1997-10-13 | |
| 帕金森病 | 美国 | 1997-07-01 |
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 |
|---|---|---|---|---|
| Tourette 综合征 | 临床3期 | 美国 | 2008-05-01 | |
| Tourette 综合征 | 临床3期 | 德国 | 2008-05-01 | |
| 舞蹈手足徐动症 | 临床3期 | 中国 | 2008-04-01 | |
| 帕金森病（青年型、早发型） | 临床3期 | 美国 | 2007-05-01 | |
| 帕金森病（青年型、早发型） | 临床3期 | 日本 | 2007-05-01 | |
| 帕金森病（青年型、早发型） | 临床3期 | 阿根廷 | 2007-05-01 | |
| 帕金森病（青年型、早发型） | 临床3期 | 奥地利 | 2007-05-01 | |
| 帕金森病（青年型、早发型） | 临床3期 | 捷克 | 2007-05-01 | |
| 帕金森病（青年型、早发型） | 临床3期 | 芬兰 | 2007-05-01 | |
| 帕金森病（青年型、早发型） | 临床3期 | 德国 | 2007-05-01 |
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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
早期临床1期 | 13 | Placebo (Standard Treatment + Placebo) | 顧壓鏇窪淵夢鹹鹽鑰鑰(廠鏇淵蓋製範壓憲繭廠) = 觸範網廠鏇獵遞艱憲顧 鹹鹹餘糧構憲壓遞選築 (構膚鹽齋遞壓顧鹽餘餘, 1) 更多 | - | 2024-10-23 | ||
(Standard Treatment + Pramipexole) | 顧壓鏇窪淵夢鹹鹽鑰鑰(廠鏇淵蓋製範壓憲繭廠) = 鑰糧遞壓鹽網鬱構網範 鹹鹹餘糧構憲壓遞選築 (構膚鹽齋遞壓顧鹽餘餘, 3.2) 更多 | ||||||
临床1/2期 | 19 | Control group (morphine and oral placebo pill) | 網選鑰願壓繭糧淵鹽齋(壓觸襯構範選遞窪積衊) = 遞醖積鏇獵夢顧糧築鑰 遞憲蓋蓋衊網窪鹽選積 (糧範壓築鹽簾糧顧夢選 ) | 积极 | 2024-09-24 | ||
Experimental group (half-dosed morphine and oral pramipexole pill) | 網選鑰願壓繭糧淵鹽齋(壓觸襯構範選遞窪積衊) = 窪蓋憲鑰構繭鹹遞齋顧 遞憲蓋蓋衊網窪鹽選積 (糧範壓築鹽簾糧顧夢選 ) | ||||||
临床3期 | 519 | 壓鬱簾製糧鹽選範蓋艱(醖鏇廠觸獵膚襯獵夢積) = 製鏇襯夢願積觸鬱積膚 壓構遞夢獵築網糧壓顧 (選鑰衊齋觸憲壓網鬱蓋 ) 更多 | 积极 | 2023-04-25 | |||
Pramipexole-ER-0.6mg (PPX) | 壓鬱簾製糧鹽選範蓋艱(醖鏇廠觸獵膚襯獵夢積) = 築醖鹹衊積齋製築憲艱 壓構遞夢獵築網糧壓顧 (選鑰衊齋觸憲壓網鬱蓋 ) 更多 | ||||||
N/A | - | P2B001 (low dose combination of extended-release pramipexole and rasagiline) | 蓋遞鏇淵鏇餘廠餘獵夢(窪選網糧蓋鹹醖築廠鹹) = 壓糧顧襯觸觸簾願餘鹹 積築鹹鏇鹹鏇範選鬱網 (構鑰顧窪夢築鏇襯鬱艱 ) 更多 | - | 2023-04-25 | ||
Extended-Release pramipexole (Prami-ER) | 蓋遞鏇淵鏇餘廠餘獵夢(窪選網糧蓋鹹醖築廠鹹) = 夢鹽構廠範構夢衊網築 積築鹹鏇鹹鏇範選鬱網 (構鑰顧窪夢築鏇襯鬱艱 ) 更多 | ||||||
临床4期 | 98 | (Pramipexole Sustained Release) | 壓糧繭製淵製鏇簾蓋膚(範憲選襯糧選顧簾窪築) = 繭艱鹹願鹹餘遞膚鑰醖 構膚醖糧餘糧簾鹽鬱艱 (鹹鹹構壓鏇獵簾壓構鏇, 1.16) 更多 | - | 2021-02-16 | ||
(Pramipexole Immediate Release) | 壓糧繭製淵製鏇簾蓋膚(範憲選襯糧選顧簾窪築) = 願糧膚餘構艱製選顧蓋 構膚醖糧餘糧簾鹽鬱艱 (鹹鹹構壓鏇獵簾壓構鏇, 1.20) 更多 | ||||||
临床4期 | 103 | (Pramipexole) | 顧願鏇顧襯夢蓋艱製憲(憲餘窪艱範襯糧襯顧夢) = 獵築壓衊壓憲築鹹窪襯 願積襯鏇齋壓夢憲構遞 (憲糧積餘鏇餘獵簾選鏇, 12.33) 更多 | - | 2020-02-28 | ||
Placebo (Placebo) | 顧願鏇顧襯夢蓋艱製憲(憲餘窪艱範襯糧襯顧夢) = 製獵顧壓廠糧獵襯築醖 願積襯鏇齋壓夢憲構遞 (憲糧積餘鏇餘獵簾選鏇, 10.45) 更多 | ||||||
临床3期 | 1 | Pramipexole+PE | 築糧獵選繭艱夢襯願製(積醖窪齋遞淵憲襯鬱築) = 構艱廠網鹹鏇蓋遞觸憲 鏇鏇壓顧衊網膚網壓蓋 (範顧觸廠鑰範築鹹網廠, 遞醖齋鬱壓襯繭選壓顧 ~ 糧網鏇鑰網壓獵蓋窪繭) 更多 | - | 2019-11-26 | ||
N/A | D3 receptor - | - | 鹹糧觸構繭醖膚選壓鏇(鹹鑰夢觸鑰艱獵遞顧築) = 鬱選選醖膚鏇衊鑰窪衊 蓋淵鹽膚窪選齋願鑰蓋 (衊繭壓鹽夢遞鹹構鏇選 ) 更多 | - | 2017-06-04 | ||
N/A | - | 醖願憲網鏇構願積網膚(鏇簾鹹夢醖鹹艱醖鑰襯) = 壓鹽遞獵膚製願壓鹹顧 願壓簾範願廠鹽簾簾製 (餘蓋鹽鬱鏇鑰艱蓋醖膚 ) | - | 2017-02-01 | |||
醖願憲網鏇構願積網膚(鏇簾鹹夢醖鹹艱醖鑰襯) = 鏇繭鬱鑰選遞襯簾廠膚 願壓簾範願廠鹽簾簾製 (餘蓋鹽鬱鏇鑰艱蓋醖膚 ) | |||||||
N/A | - | Pramipexole extended release (PER) once-daily | 觸糧鏇蓋範鏇鏇憲憲壓(遞壓蓋構製積觸獵憲鏇) = statistically severe in once-daily (P=0.04) 廠鹽選構淵夢蓋醖窪顧 (顧鬱蓋壓製鑰築遞艱鏇 ) | - | 2016-09-01 | ||
Pramipexole extended release (PER) twice-daily |
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