Idrugs最新文献 - Book学术

Neurodegenerative diseases. 神经退行性疾病。

Idrugs Pub Date : 2023-03-21 DOI: 10.5772/45957

A. Hannan

引用次数: 0

Edotecarin. Edotecarin。

Idrugs Pub Date : 2020-02-07 DOI: 10.32388/69tw8h

W. Denny

引用次数: 2

Tesaglitazar.

Idrugs Pub Date : 2020-02-07 DOI: 10.32388/g73iem

N. Kamber, Timothy M. Davis

引用次数: 0

Anti-inflammatory drugs 抗炎药

Idrugs Pub Date : 2013-09-27 DOI: 10.1007/978-1-349-10705-6_51

高橋季之, 太砂田, 砂田太, 永井秀忠, 英二依田, 依田英二

引用次数: 51

Dexpramipexole, the R(+) enantiomer of pramipexole, for the potential treatment of amyotrophic lateral sclerosis. 右普拉克索，普拉克索的R(+)对映体，用于肌萎缩性侧索硬化的潜在治疗。

Idrugs Pub Date : 2010-12-01

Benjamin C Cheah, Matthew C Kiernan

{"title":"Dexpramipexole, the R(+) enantiomer of pramipexole, for the potential treatment of amyotrophic lateral sclerosis.","authors":"Benjamin C Cheah, Matthew C Kiernan","doi":"","DOIUrl":"","url":null,"abstract":"Dexpramipexole (KNS-760704), the R(+) enantiomer of pramipexole, is under development by Knopp Neurosciences and Biogen Idec as a potential neuroprotective therapy for amyotrophic lateral sclerosis (ALS), a universally fatal neurodegenerative disease. Pramipexole, exclusively the S(-) enantiomer, is a non-ergot dopaminergic autoreceptor agonist that is currently marketed for use in the treatment of Parkinson's disease and restless legs syndrome. Pramipexole has been proposed to exert a broad spectrum of neuroprotective properties, primarily through antioxidant effects, inhibiting apoptotic enzymes and preserving mitochondrial structure and activity. More recent work has suggested that pramipexole possesses anti-excitotoxic properties, raising the possibility of beneficial effects in patients with ALS. However, pramipexole has high intrinsic dopaminergic receptor activity and, consequently, dose-limiting side effects, including orthostatic hypotension and hallucination, are frequent. Dexpramipexole exhibits significantly lower affinity for dopaminergic receptors, thereby making it unlikely to be associated with dopaminergic side effects. In clinical trials to date, dexpramipexole has been safe and well tolerated at doses up to 67-fold higher than the maximum recommended daily dose of pramipexole in patients with Parkinson's disease, and has demonstrated signs of neuroprotective benefit. This report summarizes the chemical and pharmacological properties of dexpramipexole and describes the potential utility of the drug in the pharmaceutical development pipeline.","PeriodicalId":55031,"journal":{"name":"Idrugs","volume":"13 12","pages":"911-20"},"PeriodicalIF":0.0,"publicationDate":"2010-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"29532530","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

LX-1031, a tryptophan 5-hydroxylase inhibitor that reduces 5-HT levels for the potential treatment of irritable bowel syndrome. LX-1031，一种色氨酸5-羟化酶抑制剂，可降低5-羟色胺水平，用于肠易激综合征的潜在治疗。

Idrugs Pub Date : 2010-12-01

Michael Camilleri

引用次数: 0

Remimazolam, a short-acting GABA(A) receptor agonist for intravenous sedation and/or anesthesia in day-case surgical and non-surgical procedures. 雷马唑仑，一种短效GABA(a)受体激动剂，用于日间手术和非手术过程中的静脉镇静和/或麻醉。

Idrugs Pub Date : 2010-12-01

William Kirke Rogers, Thomas S McDowell

{"title":"Remimazolam, a short-acting GABA(A) receptor agonist for intravenous sedation and/or anesthesia in day-case surgical and non-surgical procedures.","authors":"William Kirke Rogers, Thomas S McDowell","doi":"","DOIUrl":"","url":null,"abstract":"Remimazolam (CNS-7056) is a short-acting GABA(A) receptor agonist, under development by PAION, in collaboration with Japanese licensee Ono Pharmaceutical, as an intravenous sedative agent for potential use in day-case procedures, and the induction and maintenance of anesthesia. A member of the benzodiazapene class of drugs, the structure of remimazolam was modified to produce a drug that displays organ-independent metabolism. The incorporation of a carboxylic ester moiety into the benzodiazapene core of remimazolam renders it susceptible to non-specific tissue esterases and it is rapidly metabolized into its pharmacologically inactive metabolite CNS-7054. Preclinical studies in sheep demonstrated that remimazolam produced a more rapid onset of action, and a shorter duration of action, compared with midazolam. In a phase IIa clinical trial evaluating remimazolam as a procedural sedative for upper gastrointestinal endoscopy in patients, the time to recovery from sedation was shorter and more consistent with remimazolam, relative to midazolam. Because of its organ-independent metabolism and rapid and predictable onset and recovery, remimazolam appears to have potential advantages over other currently available short-acting sedatives.","PeriodicalId":55031,"journal":{"name":"Idrugs","volume":"13 12","pages":"929-37"},"PeriodicalIF":0.0,"publicationDate":"2010-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"29532532","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Lu-AA21004, a multimodal serotonergic agent, for the potential treatment of depression and anxiety. Lu-AA21004，一种多模式血清素能剂，用于治疗抑郁和焦虑。

Idrugs Pub Date : 2010-12-01

Albert Adell

{"title":"Lu-AA21004, a multimodal serotonergic agent, for the potential treatment of depression and anxiety.","authors":"Albert Adell","doi":"","DOIUrl":"","url":null,"abstract":"Lu-AA21004, an oral, multimodal serotonergic agent, is currently under development by H Lundbeck and Takeda Pharmaceutical, for the potential treatment of depression and anxiety. Lu-AA21004 belongs to a novel chemical class of antidepressant agents, the bisarylsulfanyl amines, and possesses a novel pharmacological profile, with activity at serotonergic receptors 5-HT3, 5-HT7 and 5-HT1A, and also at the 5-HT transporter. Acute administration of Lu-AA21004 in rats inhibited the firing activity of serotonergic neurons of the dorsal raphe nucleus through 5-HT3 receptor blockade, with rapid recovery of firing activity upon cessation of treatment compared with an antidepressant of the SSRI class. Results from phase II clinical trials have reported improvement in depression and anxiety symptoms after 6 weeks of treatment. Lu-AA21004 was generally well tolerated, with adverse events related to sexual dysfunction occurring in a lower number of patients receiving Lu-AA21004 compared with venlafaxine. Phase III clinical trials with Lu-AA21004 in patients with major depressive disorder are underway and phase III trials in patients with generalized anxiety disorder have been completed. If initial outcomes from these clinical trials prove positive, Lu-AA21004 may pave the way for new multimodal therapies for the treatment of depression and anxiety.","PeriodicalId":55031,"journal":{"name":"Idrugs","volume":"13 12","pages":"900-10"},"PeriodicalIF":0.0,"publicationDate":"2010-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"29532529","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Targeted molecular therapy for preventing heart failure and sudden cardiac death. 28 September 2010, New York, NY, USA. 靶向分子治疗预防心力衰竭和心源性猝死。2010年9月28日，美国纽约。

Idrugs Pub Date : 2010-12-01

Martin Schwarz

引用次数: 0

Strategies for conducting ADME studies during lead generation in the drug discovery process. 在药物发现过程的先导物生成过程中进行ADME研究的策略。

Idrugs Pub Date : 2010-12-01

Jeffrey W Cramer, Brian E Mattioni, Kenneth A Savin

引用次数: 0