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HU 210: A Potent Tool for Investigations of the Cannabinoid System HU 210:研究大麻酚系统的有效工具
CNS drug reviews Pub Date : 2006-06-07 DOI: 10.1111/j.1527-3458.2001.tb00192.x
Alessandra Ottani, Daniela Giuliani
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引用次数: 51
GV150526: A Neuroprotective Agent GV150526:一种神经保护剂
CNS drug reviews Pub Date : 2006-06-07 DOI: 10.1111/j.1527-3458.2000.tb00142.x
Fabio Bordi, Manolo Mugnaini, Andrea Terron, Robert Barnaby, Angelo Reggiani
{"title":"GV150526: A Neuroprotective Agent","authors":"Fabio Bordi,&nbsp;Manolo Mugnaini,&nbsp;Andrea Terron,&nbsp;Robert Barnaby,&nbsp;Angelo Reggiani","doi":"10.1111/j.1527-3458.2000.tb00142.x","DOIUrl":"https://doi.org/10.1111/j.1527-3458.2000.tb00142.x","url":null,"abstract":"<div>\u0000 \u0000 <p>Thromboembolic stroke is a severe, disabling disease characterized by an abrupt reduction of cerebral blood flow, which leads to deprivation of oxygen and nutrients to neuronal tissue, followed by permanent brain damage. Evidence has been accumulated to implicate excitotoxicity in the pathogenesis of ischemic brain injury. Overstimulation of excitatory amino acid receptors becomes deleterious for neuronal cell survival. Glutamate antagonists can ameliorate the ischemic injury by any of several mechanisms. Because blockade of the glycine site of the <i>N</i>-methyl-D-aspartate (NMDA) receptor seems to offer a better side-effect profile, glycine antagonists are attractive targets for blocking excitotoxicity following stroke.</p>\u0000 <p>GV150526 is a selective and potent glycine antagonist at the NMDA receptor complex. It binds to the glycine site with both high affinity and high selectivity in <i>in vitro</i> binding studies. <i>In vivo</i> studies have shown that GV150526 significantly reduces infarct volume in the middle cerebral artery occlusion model of stroke. This effect remained statistically significant, even if treatment was delayed for as long as 6 h post-occlusion. GV150526 showed no evidence of adverse effects usually associated with NMDA receptor blockers, such as neuronal vacuolization in standard assays or cognitive impairment in behavioral tests. GV150526 had no significant treatment-related respiratory or cardiovascular effects or effects on behavior, body temperature, or blood pressure in mice or rats. Pharmacokinetic studies indicated that GV150526 has low clearance and volume of distribution in both the rat and the dog. Preclinical toxicology studies have shown that the compound is well tolerated in both species. Phase I/II studies were undertaken to assess the safety, tolerability, and pharmacokinetics of GV150526 in healthy volunteers and acute stroke patients, and from these a dose was selected to be studied in Phase III clinical trials. These efficacy studies have now completed recruitment and data reconciliation is ongoing. GV150526 has the potential to be an effective therapy for acute ischemic stroke.</p>\u0000 </div>","PeriodicalId":94307,"journal":{"name":"CNS drug reviews","volume":"6 2","pages":"135-152"},"PeriodicalIF":0.0,"publicationDate":"2006-06-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1111/j.1527-3458.2000.tb00142.x","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71942758","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 2
29th Annual Meeting of New England Pharmacologists Brown University, Providence, RI January 28–29, 2000 新英格兰药理学专家第29届年会布朗大学,普罗维登斯,RI 2000年1月28日-29日
CNS drug reviews Pub Date : 2006-06-07 DOI: 10.1111/j.1527-3458.2000.tb00145.x
Alexander Scriabine
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引用次数: 0
SB-236057-A: A Selective 5-HT1B Receptor Inverse Agonist SB-236057-A:一种选择性5-HT1B受体反向激动剂
CNS drug reviews Pub Date : 2006-06-07 DOI: 10.1111/j.1527-3458.2001.tb00209.x
Claire Roberts, Jeanette Watson, Gary W. Price, Derek N. Middlemiss
{"title":"SB-236057-A: A Selective 5-HT1B Receptor Inverse Agonist","authors":"Claire Roberts,&nbsp;Jeanette Watson,&nbsp;Gary W. Price,&nbsp;Derek N. Middlemiss","doi":"10.1111/j.1527-3458.2001.tb00209.x","DOIUrl":"https://doi.org/10.1111/j.1527-3458.2001.tb00209.x","url":null,"abstract":"<div>\u0000 \u0000 <p>5-HT<sub>1B</sub> autoreceptors are involved in the control of extracellular 5-HT levels from both the terminal and cell body regions of serotonergic neurons. In this manuscript we review the pharmacological and pharmacokinetic data available for the selective and potent 5-HT<sub>1B</sub> receptor inverse agonist, SB-236057-A (1′-ethyl-5-(2′-methyl-4′-(5-methyl-1,3,4-oxadiazolyl-2-yl)biphenyl-4-carbonyl)-2,3,6,7-tetrahydrospiro (furo[2,3-f]indole-3,4′-piperidine) hydrochloride). SB 236057-A has been shown to have high affinity for human 5-HT<sub>1B</sub> receptors (p<i>K</i><sub>i</sub>= 8.2) and displays 80 or more fold selectivity for the human 5-HT<sub>1B</sub> receptor over other 5-HT receptors and a range of additional receptors, ion channels and enzymes. In functional studies at human 5-HT<sub>1B</sub> receptors SB-236057-A displayed inverse agonism (pA<sub>2</sub>= 8.9) using [<sup>35</sup>S]GTPγS binding, and silent antagonism (pA<sub>2</sub>= 9.2) using cAMP accumulation. SB-236057-A also acted as an antagonist at the 5-HT terminal autoreceptor as measured by [<sup>3</sup>H]5-HT release from electrically stimulated guinea pig and human cortical slices.</p>\u0000 <p>In the guinea pig, pharmacokinetic analysis demonstrated that SB-236057-A was bioavailable and according to <i>in vivo</i> pharmacodynamic assays it enters brain and has a long duration of action. Importantly no side effect liability was evident at relevant doses from anxiogenic, cardiovascular, sedative or migraine viewpoints.</p>\u0000 <p> <i>In vivo</i> microdialysis studies demonstrated that SB-236057-A is an antagonist in the guinea pig cortex but has no effect on extracellular 5-HT levels <i>per se.</i> In contrast, SB-236057-A increased extracellular 5-HT levels in the guinea pig dentate gyrus. This increase in 5-HT release was comparable to that observed after 14 days of paroxetine administration.</p>\u0000 <p>SB-236057-A has been a useful tool in confirming that, in either guinea pigs or humans, the terminal 5-HT autoreceptor is of the 5-HT<sub>1B</sub> subtype. It appears that acute 5-HT<sub>1B</sub> receptor blockade, by virtue of increased 5-HT release in the dentate gyrus, may provide a rapidly acting antidepressant.</p>\u0000 </div>","PeriodicalId":94307,"journal":{"name":"CNS drug reviews","volume":"7 4","pages":"433-444"},"PeriodicalIF":0.0,"publicationDate":"2006-06-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1111/j.1527-3458.2001.tb00209.x","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71951192","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 17
ACKNOWLEDGMENT OF REVIEWERS 评审员认可
CNS drug reviews Pub Date : 2006-06-07 DOI: 10.1111/j.1527-3458.2001.tb00212.x
{"title":"ACKNOWLEDGMENT OF REVIEWERS","authors":"","doi":"10.1111/j.1527-3458.2001.tb00212.x","DOIUrl":"https://doi.org/10.1111/j.1527-3458.2001.tb00212.x","url":null,"abstract":"","PeriodicalId":94307,"journal":{"name":"CNS drug reviews","volume":"7 4","pages":"485"},"PeriodicalIF":0.0,"publicationDate":"2006-06-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1111/j.1527-3458.2001.tb00212.x","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71953161","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Phenibut (β-Phenyl-GABA): A Tranquilizer and Nootropic Drug Phenibut(β-苯基GABA):一种镇静剂和益智药
CNS drug reviews Pub Date : 2006-06-07 DOI: 10.1111/j.1527-3458.2001.tb00211.x
Izyaslav Lapin
{"title":"Phenibut (β-Phenyl-GABA): A Tranquilizer and Nootropic Drug","authors":"Izyaslav Lapin","doi":"10.1111/j.1527-3458.2001.tb00211.x","DOIUrl":"https://doi.org/10.1111/j.1527-3458.2001.tb00211.x","url":null,"abstract":"<div>\u0000 \u0000 <p>Phenibut (β-phenyl-γ-aminobutyric acid HCl) is a neuropsychotropic drug that was discovered and introduced into clinical practice in Russia in the 1960s. It has anxiolytic and nootropic (cognition enhancing) effects. It acts as a GABA-mimetic, primarily at GABA<sub>B</sub> and, to some extent, at GABA<sub>A</sub> receptors. It also stimulates dopamine receptors and antagonizes β-phenethylamine (PEA), a putative endogenous anxiogenic. The psychopharmacological activity of phenibut is similar to that of baclofen, a <i>p</i>-Cl-derivative of phenibut. This article reviews the structure-activity relationship of phenibut and its derivatives. Emphasis is placed on the importance of the position of the phenyl ring, the role of the carboxyl group, and the activity of optical isomers. Comparison of phenibut with piracetam and diazepam reveals similarities and differences in their pharmacological and clinical effects. Phenibut is widely used in Russia to relieve tension, anxiety, and fear, to improve sleep in psychosomatic or neurotic patients; as well as a pre- or post-operative medication. It is also used in the therapy of disorders characterized by asthenia and depression, as well as in post-traumatic stress, stuttering and vestibular disorders.</p>\u0000 </div>","PeriodicalId":94307,"journal":{"name":"CNS drug reviews","volume":"7 4","pages":"471-481"},"PeriodicalIF":0.0,"publicationDate":"2006-06-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1111/j.1527-3458.2001.tb00211.x","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71953162","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 143
Immunophilin Ligands and Anti-inflammatory Drugs Regulate Amyloid Precursor Protein Synthesis and Metabolism 免疫亲蛋白配体和抗炎药调节淀粉样前体蛋白的合成和代谢
CNS drug reviews Pub Date : 2006-06-07 DOI: 10.1111/j.1527-3458.2000.tb00169.x
Robert K. K. Lee
{"title":"Immunophilin Ligands and Anti-inflammatory Drugs Regulate Amyloid Precursor Protein Synthesis and Metabolism","authors":"Robert K. K. Lee","doi":"10.1111/j.1527-3458.2000.tb00169.x","DOIUrl":"https://doi.org/10.1111/j.1527-3458.2000.tb00169.x","url":null,"abstract":"","PeriodicalId":94307,"journal":{"name":"CNS drug reviews","volume":"6 s1","pages":"20-21"},"PeriodicalIF":0.0,"publicationDate":"2006-06-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1111/j.1527-3458.2000.tb00169.x","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71953164","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Fourth Hungarian Conference on Alzheimer's Disease and Related Disorders Szeged, Hungary, October 7–9, 1998 第四届匈牙利阿尔茨海默病及相关疾病会议,1998年10月7日至9日,匈牙利塞格德
CNS drug reviews Pub Date : 2006-06-07 DOI: 10.1111/j.1527-3458.1999.tb00088.x
Peter Kasa
{"title":"Fourth Hungarian Conference on Alzheimer's Disease and Related Disorders Szeged, Hungary, October 7–9, 1998","authors":"Peter Kasa","doi":"10.1111/j.1527-3458.1999.tb00088.x","DOIUrl":"10.1111/j.1527-3458.1999.tb00088.x","url":null,"abstract":"","PeriodicalId":94307,"journal":{"name":"CNS drug reviews","volume":"5 1","pages":"70-76"},"PeriodicalIF":0.0,"publicationDate":"2006-06-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1111/j.1527-3458.1999.tb00088.x","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73157386","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Melatonin after Four Decades: An Assessment of its Potential Hamburg, Germany, August 11–19, 1998 四十年后的褪黑素:对其潜力的评估汉堡,德国,1998年8月11-19日
CNS drug reviews Pub Date : 2006-06-07 DOI: 10.1111/j.1527-3458.1999.tb00086.x
James Olcese
{"title":"Melatonin after Four Decades: An Assessment of its Potential Hamburg, Germany, August 11–19, 1998","authors":"James Olcese","doi":"10.1111/j.1527-3458.1999.tb00086.x","DOIUrl":"10.1111/j.1527-3458.1999.tb00086.x","url":null,"abstract":"","PeriodicalId":94307,"journal":{"name":"CNS drug reviews","volume":"5 1","pages":"59-63"},"PeriodicalIF":0.0,"publicationDate":"2006-06-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1111/j.1527-3458.1999.tb00086.x","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80334115","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 6
LY3 54740: A Systemically Active mGlu2/mGlu3 Receptor Agonist LY3 54740:一种系统活性mGlu2/mGlu3受体激动剂
CNS drug reviews Pub Date : 2006-06-07 DOI: 10.1111/j.1527-3458.1999.tb00082.x
Darryle D. Schoepp, James A. Monn, Gerard J. Marek, George A Ghajanian, Bita Moghaddam
{"title":"LY3 54740: A Systemically Active mGlu2/mGlu3 Receptor Agonist","authors":"Darryle D. Schoepp,&nbsp;James A. Monn,&nbsp;Gerard J. Marek,&nbsp;George A Ghajanian,&nbsp;Bita Moghaddam","doi":"10.1111/j.1527-3458.1999.tb00082.x","DOIUrl":"10.1111/j.1527-3458.1999.tb00082.x","url":null,"abstract":"","PeriodicalId":94307,"journal":{"name":"CNS drug reviews","volume":"5 1","pages":"1-12"},"PeriodicalIF":0.0,"publicationDate":"2006-06-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1111/j.1527-3458.1999.tb00082.x","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88350327","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 16
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