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Parathyroid‐Hormone‐Related Protein is a Neuroprotective Endogenous Regulator of L‐Type Calcium Channels 甲状旁腺激素相关蛋白是L型钙通道的神经保护性内源性调节剂
Pub Date : 2006-06-07 DOI: 10.1111/J.1527-3458.2000.TB00185.X
O. Chatterjee, I. Nakchbandi, W. Philbrick, L. Kaczmarek, M. Brines, A. Broadus
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引用次数: 0
Neuroimaging in Alzheimer's Disease: Relevance for the Development of Therapeutic Agents 阿尔茨海默病的神经影像学:与治疗剂开发的相关性
Pub Date : 2006-06-07 DOI: 10.1111/J.1527-3458.2000.TB00172.X
C. Dyck
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引用次数: 0
Alzheimer's Association International Conference on Prevention of Dementia Washington, D.C., USA June 18–21, 2005 2005年6月18日至21日在美国华盛顿特区举行的阿尔茨海默病协会预防痴呆症国际会议
Pub Date : 2006-06-07 DOI: 10.1111/J.1527-3458.2005.TB00050.X
A. Scriabine
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引用次数: 0
Mapping Cortical and Hippocampal Activation with an AMPA Receptor Potentiator in the Rat Brain Using c-fos Immunocytochemistry and [14C]2-deoxyglucose Autoradiography 利用c-fos免疫细胞化学和[14C]2-脱氧葡萄糖放射自显影技术,用AMPA受体增强剂定位大鼠脑皮层和海马的激活
Pub Date : 2006-06-07 DOI: 10.1111/J.1527-3458.2004.TB00016.X
Jill H. Fowler, K. Whalley, T. Murray, M. O'Neill, J. Mcculloch
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引用次数: 0
Evidence for Neuropathology in Transgenic Mice Overexpressing p25, an Activator of cdk5 过表达cdk5激活因子p25转基因小鼠的神经病理学证据
Pub Date : 2006-06-07 DOI: 10.1111/J.1527-3458.2000.TB00178.X
M. Ahlijanian
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引用次数: 0
Immunophilin Ligands and Anti‐inflammatory Drugs Regulate Amyloid Precursor Protein Synthesis and Metabolism 亲免疫蛋白配体和抗炎药物调节淀粉样蛋白前体蛋白的合成和代谢
Pub Date : 2006-06-07 DOI: 10.1111/J.1527-3458.2000.TB00169.X
Robert K. K. Lee
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引用次数: 0
Discovery of Selective Inhibitors of Neuronal Nitric Oxide Synthase for Neuroprotection 神经元一氧化氮合酶选择性抑制剂的神经保护作用
Pub Date : 2006-06-07 DOI: 10.1111/J.1527-3458.2000.TB00182.X
D. Reif
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引用次数: 0
Antiaging compounds: (-)deprenyl (selegeline) and (-)1-(benzofuran-2-yl)-2-propylaminopentane, [(-)BPAP], a selective highly potent enhancer of the impulse propagation mediated release of catecholamine and serotonin in the brain. 抗衰老化合物:(-)去戊烯基(selegeline)和(-)1-(苯并呋喃-2-基)-2-丙基氨基戊烷,[(-)BPAP],一种选择性的高效增强剂,可促进脑内冲动传播介导的儿茶酚胺和血清素的释放。
Pub Date : 2006-06-07 DOI: 10.1111/J.1527-3458.2001.TB00202.X
J. Knoll
Hundreds of millions of people now die over the age of 80 years primarily due to twentieth century progress in hygiene, chemotherapy, and immunology. With a longer average lifespan, the need to improve quality of life during the latter decades is more compelling. "Aging--The Epidemic of the New Millenium," a recent international conference (Monte Carlo, June 17-18, 2000), showed with peculiar clarity that a safe and efficient drug strategy to slow the age-related decay of brain performance is still missing. This review summarizes the physiologic and pharmacologic arguments in favor of a peculiar lifelong prophylactic medication with reasonable chances to keep in check brain aging and decrease the precipitation of age-related neurological diseases.
现在有数亿人在80岁以上死亡,这主要是由于20世纪卫生、化疗和免疫学的进步。随着平均寿命的延长,提高晚年生活质量的需求更加迫切。“衰老——新千年的流行病”,最近的一次国际会议(蒙特卡洛,2000年6月17日至18日),以一种特别清晰的方式表明,一种安全有效的药物策略来减缓与年龄相关的大脑功能衰退仍然缺失。本文综述了支持一种特殊的终身预防性药物的生理和药理学论据,这种药物具有合理的机会来控制大脑衰老并减少与年龄相关的神经系统疾病的发生。
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引用次数: 35
Abstracts from the Sixth International Conference on Progress in Alzheimer's and Parkinson's Diseases. May 8-12, 2003. Seville, Spain. 第六届阿尔茨海默病和帕金森病国际进展会议摘要2003年5月8日至12日。西班牙塞维利亚。
Pub Date : 2004-01-01
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引用次数: 0
Negative allosteric modulation of AMPA-preferring receptors by the selective isomer GYKI 53784 (LY303070), a specific non-competitive AMPA antagonist. 选择性异构体GYKI 53784 (LY303070)对AMPA偏好受体的负变构调节,一种特异性的非竞争性AMPA拮抗剂。
Pub Date : 2002-01-01
Jérôme Ruel, Matthieu J Guitton, Jean-Luc Puell

GYKI 53784 or LY303070 [(-)1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-4,5-dihydro-3-methylcarbamoyl-2,3-benzodiazepine] belongs to a new family of 2,3-benzodiazepine compounds (also called homophtalazines) selective and non-competitive antagonists at alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionate (AMPA) receptors. These compounds include the original GYKI-52466, its more potent derivative GYKI 53655 and the active isomer of the latter, GYKI 53784. This review summarizes current knowledge of this novel AMPA antagonist: GYKI 53784. GYKI 53784 is the most potent of the compounds in the 2,3-benzodiazepine class, blocking AMPA receptor-mediated responses. In contrast to the compounds of the quinoxalinedione family, that block AMPA as well as kainate receptors, GYKI 53784 does not block the activation of kainate receptors. Furthermore, GYKI 53784 does not act at the same receptor site as positive AMPA modulators (i.e., cyclothiazide, BDP-12, 1-BCP or aniracetam). GYKI 53784 is a powerful neuroprotective agent in both in vitro and in vivo models of AMPA receptor-mediated excitotoxicity. In contrast to NMDA receptor antagonists, whose favorable clinical actions are compromised by important side effects such as the impairment of memory functions, the selective AMPA antagonist, GYKI 53784, may be of potential clinical value, both in acute (stroke and trauma) and chronic (Alzheimer's disease, epilepsy) neurological disorders.

GYKI 53784或LY303070[(-)1-(4-氨基苯基)-4-甲基-7,8-亚甲二氧基-4,5-二氢-3-甲基氨基甲酰-2,3-苯二氮卓]属于2,3-苯二氮卓类化合物(也称为同苯丙嗪)的新家族,具有α -氨基-3-羟基-5-甲基-4-异恶唑-丙酸(AMPA)受体的选择性和非竞争性拮抗剂。这些化合物包括原始的GYKI-52466,其更有效的衍生物GYKI 53655和后者的活性异构体GYKI 53784。本文综述了目前对新型AMPA拮抗剂GYKI 53784的了解。GYKI 53784是2,3-苯二氮卓类药物中最有效的化合物,可阻断AMPA受体介导的反应。与喹啉二酮家族的化合物相比,阻断AMPA和盐酸盐受体,GYKI 53784不阻断盐酸盐受体的激活。此外,GYKI 53784不作用于与AMPA阳性调节剂(即环噻嗪、BDP-12、1-BCP或阿尼西坦)相同的受体位点。GYKI 53784在体外和体内AMPA受体介导的兴奋性毒性模型中都是一种强大的神经保护剂。与NMDA受体拮抗剂相比,选择性AMPA拮抗剂GYKI 53784可能在急性(中风和创伤)和慢性(阿尔茨海默病、癫痫)神经系统疾病中具有潜在的临床价值,而NMDA受体拮抗剂的良好临床作用受到记忆功能损害等重要副作用的影响。
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引用次数: 0
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CNS drug reviews
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