Delving into the Latest Updates on Parke Davis Pharmaceutical Research Div Warner Lambert Co with Synapse

概览

疾病领域	数量

感染	2

排名前五的药物类型	数量

小分子化药	2

排名前五的靶点	数量

Top II(拓扑异构酶II)	2

关联

5

项与 Parke Davis Pharmaceutical Research Div Warner Lambert Co 相关的药物

PD-131628

靶点

Top II

作用机制

Top II抑制剂

在研机构

Parke Davis Pharmaceutical Research Div Warner Lambert Co

原研机构

Pfizer Inc.

在研适应症

细菌感染

非在研适应症-

最高研发阶段临床前

首次获批国家/地区-

首次获批日期-

CI-990

靶点

Top II

作用机制

Top II抑制剂

在研机构

Parke Davis Pharmaceutical Research Div Warner Lambert Co

原研机构

Pfizer Inc.

在研适应症

细菌感染

非在研适应症-

最高研发阶段临床前

首次获批国家/地区-

首次获批日期-

Phenytoin sodium

苯妥英钠

靶点

SCNA

作用机制

SCNA阻滞剂

在研机构-

原研机构

Parke Davis Pharmaceutical Research Div Warner Lambert Co

在研适应症-

非在研适应症

癫痫发作 [+1]

最高研发阶段撤市

首次获批国家/地区

美国

首次获批日期1956-03-01

100 项与 Parke Davis Pharmaceutical Research Div Warner Lambert Co 相关的临床结果

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0 项与 Parke Davis Pharmaceutical Research Div Warner Lambert Co 相关的专利（医药）

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47

项与 Parke Davis Pharmaceutical Research Div Warner Lambert Co 相关的文献（医药）

2011-04-12·Journal of Pharmacy and Pharmacology3区 · 医学

Brain Extracellular Levels of the Putative Antipsychotic CI-1007 and Its Effects on Striatal and Nucleus Accumbens Dopamine Overflow in the Awake Rat

3区 · 医学

Article

作者: Davis, M Duff ; Giordani, Anne B ; Iyer, Raj N ; Juneau, Paul L

AbstractThe compound CI-1007 (R-(+)-1,2,3,6-tetrahydro-4-phenyl-1[(3-phenyl-3-cyclohexen-1-yl)methyl]pyridine maleate) has been identified as a partial dopamine agonist and putative antipsychotic in in-vitro and in-vivo neurochemical, neurophysiological and behavioural tests.By use of microdialysis in conjunction with high-performance liquid chromatography (HPLC) with electrochemical detection, the effects of the drug on brain dopamine release, previously observed in anaesthetized animals, were shown to occur in awake animals also. Detection of peripherally administered CI-1007 in the brain, i.e. evidence of the drug’s ability to penetrate the blood-brain barrier, was achieved by use of in-vivo brain microdialysis in awake, freely moving rats and capillary HPLC in combination with tandem mass spectrometry (HPLC/MS/MS). Intravenous administration of CI-1007 (40 mg kg−1) significantly inhibits dopamine release in the nucleus accumbens, a region associated with dopamine hyperactivity in schizophrenia, while having a non-significant impact on the striatal dopamine neurotransmission which is critical to regular motor function.The differential neurochemical profile of the drug indicates its potential usefulness in treating positive disease symptoms and implies that its extrapyramidal side effects are lower than those of typical antipsychotics.

2001-09-01·Diabetes1区 · 医学

Calpains Play a Role in Insulin Secretion and Action

1区 · 医学

Article

作者: Zhou, Yun-Ping ; Burant, Charles F. ; Polonsky, Kenneth S. ; Ostrega, Diane M. ; Horikawa, Yukio ; Pugh, William ; Fox, Aaron P. ; Hanis, Craig L. ; Lee, Jean-Pyo ; Sreenan, Seamus K. ; Cox, Nancy J. ; Otani, Kenichi ; Pan, Chien-Yuan ; Hansen, Polly A. ; Bell, Graeme I. ; Currie, Kevin P.M.

Studies of the genetic basis of type 2 diabetes suggest that variation in the calpain-10 gene affects susceptibility to this common disorder, raising the possibility that calpain-sensitive pathways may play a role in regulating insulin secretion and/or action. Calpains are ubiquitously expressed cysteine proteases that are thought to regulate a variety of normal cellular functions. Here, we report that short-term (4-h) exposure to the cell-permeable calpain inhibitors calpain inhibitor II and E-64-d increases the insulin secretory response to glucose in mouse pancreatic islets. This dose-dependent effect is observed at glucose concentrations above 8 mmol/l. This effect was also seen with other calpain inhibitors with different mechanisms of action but not with cathepsin inhibitors or other protease inhibitors. Enhancement of insulin secretion with short-term exposure to calpain inhibitors is not mediated by increased responses in intracellular Ca2+ or increased glucose metabolism in islets but by accelerated exocytosis of insulin granules. In muscle strips and adipocytes, exposure to both calpain inhibitor II and E-64-d reduced insulin-mediated glucose transport. Incorporation of glucose into glycogen in muscle also was reduced. These results are consistent with a role for calpains in the regulation of insulin secretion and insulin action.

2001-04-01·Archives of Pathology & Laboratory Medicine

Intraneuronal Aβ-Amyloid Precedes Development of Amyloid Plaques in Down Syndrome

Article

作者: Stewart, Walter F. ; Gyure, Kymberly A. ; Durham, Robert ; Smialek, John E. ; Troncoso, Juan C.

AbstractContext.—Down syndrome patients who live to middle age invariably develop the neuropathologic features of Alzheimer disease, providing a unique situation in which to study the early and sequential development of these changes.Objective.—To study the development of amyloid deposits, senile plaques, astrocytic and microglial reactions, and neurofibrillary tangles in the brains of young individuals (<30 years of age) with Down syndrome.Methods.—Histologic and immunocytochemical study of a series of autopsy brains (n = 14, from subjects aged 11 months to 56 years, with 9 subjects <30 years) examined at the Office of the Chief Medical Examiner of the State of Maryland and The Johns Hopkins Hospital.Results.—The principal observations included the presence of intraneuronal Aβ immunostaining in the hippocampus and cerebral cortex of very young Down syndrome patients (preceding the extracellular deposition of Aβ) and the formation of senile plaques and neurofibrillary tangles.Conclusions.—We propose the following sequence of events in the development of neuropathologic changes of Alzheimer disease in Down syndrome: (1) intracellular accumulation of Aβ in neurons and astrocytes, (2) deposition of extracellular Aβ and formation of diffuse plaques, and (3) development of neuritic plaques and neurofibrillary tangles with activation of microglial cells.

100 项与 Parke Davis Pharmaceutical Research Div Warner Lambert Co 相关的药物交易

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100 项与 Parke Davis Pharmaceutical Research Div Warner Lambert Co 相关的转化医学

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当前项目

药物(靶点)	适应症	全球最高研发状态

CI-990 ( Top II )	细菌感染更多	临床前
PD-131628 ( Top II )	细菌感染更多	临床前
苯妥英钠 ( SCNA )	癫痫持续状态更多	撤市
Chloramphenicol/Polymyxin B Sulfate ( 50S subunit x PBPs )	眼部炎症更多	撤市
PD-151746 ( CAPN1 )	脑卒中更多	无进展