Did you mean: Robert Zaczek

γ-secretase inhibitors for Alzheimer's disease: balancing efficacy and toxicity

DM Barten, JE Meredith, R Zaczek, JG Houston… - Drugs in R&D, 2006 - Springer
The amyloid hypothesis, which states that β-amyloid (Aβ) aggregates cause the onset and
progression of Alzheimer’s disease (AD), is a leading proposal to explain AD aetiology. …

Corticotropin releasing factor (CRF) receptor modulators: progress and opportunities for new therapeutic agents

…, DW Robertson, R Zaczek - Journal of medicinal …, 2000 - ACS Publications
Corticotropin releasing factor (or hormone, CRF or CRH) is a major modulator of the body’s
responses to stress, and modulation of CRF receptor function has become an important …

[HTML][HTML] Presenilin-1 and-2 are molecular targets for γ-secretase inhibitors

…, B Cordell, AM Stern, RE Olson, R Zaczek - Journal of Biological …, 2000 - ASBMB
Presenilins are integral membrane protein involved in the production of amyloid β-protein.
Mutations of the presenilin-1 and -2 gene are associated with familial Alzheimer's disease …

Discovery and evaluation of BMS-708163, a potent, selective and orally bioavailable γ-secretase inhibitor

…, KA Lentz, JG Houston, R Zaczek… - ACS medicinal …, 2010 - ACS Publications
During the course of our research efforts to develop a potent and selective γ-secretase
inhibitor for the treatment of Alzheimer's disease, we investigated a series of carboxamide-…

N‐Acetyl‐Aspartyl‐Glutamate: Regional Levels in Rat Brain and the Effects of Brain Lesions as Determined by a New HPLC Method

KJ Koller, R Zaczek, JT Coyle - Journal of neurochemistry, 1984 - Wiley Online Library
An isocratic HPLC method to measure endogenous N‐acetyl‐aspartyl‐glutamate (NAAG)
and N‐acetyl‐aspartate (NAA) is described. After removal of primary amines by passage of …

Kainic acid stimulates excitatory amino acid neurotransmitter release at presynaptic receptors

JW Ferkany, R Zaczek, JT Coyle - Nature, 1982 - nature.com
Kainic acid (KA), a conformationally restricted analogue of glutamic acid, exhibits potent
neuroexcitatory 1 and neurotoxic properties 2 . The mechanism of the neurotoxicity of KA, …

Distinctive transcriptome alterations of prefrontal pyramidal neurons in schizophrenia and schizoaffective disorder

…, D Datta, F Boothe, A He, AM Cacace, R Zaczek… - Molecular …, 2015 - nature.com
Schizophrenia is associated with alterations in working memory that reflect dysfunction of
dorsolateral prefrontal cortex (DLPFC) circuitry. Working memory depends on the activity of …

The Pharmacology of DMP696 and DMP904, Non‐Peptidergic CRF1 Receptor Antagonists

…, J McElroy, NJ Lodge, P Gilligan, R Zaczek - CNS drug …, 2005 - Wiley Online Library
CRF 1 antagonists DMP696 and DMP904 were designed as drug development candidates
for the treatment of anxiety and depression. Both compounds display nanomolar affinity for …

Postsynaptic diacylglycerol lipase α mediates retrograde endocannabinoid suppression of inhibition in mouse prefrontal cortex

…, Y Blat, RS Westphal, R Zaczek… - The Journal of …, 2011 - Wiley Online Library
Non‐Technical Summary In multiple brain regions, endogenous cannabinoids suppress
inhibitory synaptic transmission; however, the biochemical/molecular pathways for …

Synthesis and Structure− Activity Relationships of 8-(Pyrid-3-yl) pyrazolo [1, 5-a]-1, 3, 5-triazines: Potent, Orally Bioavailable Corticotropin Releasing Factor Receptor …

…, S Bai, J Saye, S Grossman, R Zaczek… - Journal of medicinal …, 2009 - ACS Publications
This report describes the syntheses and structure−activity relationships of 8-(substituted
pyridyl)pyrazolo[1,5-a]-1,3,5-triazine corticotropin releasing factor receptor-1 (CRF 1 ) receptor …
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