Search Results - "Korábečny, J."
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The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease
Published in European journal of medicinal chemistry (25-04-2018)“…Novel tacrine-benzyl quinolone carboxylic acid (tacrine-BQCA) hybrids were designed based on multi-target directed ligands (MTLDs) paradigm, synthesized and…”
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UHPLC-HRMS study of anti-Alzheimer’s drug candidates: metabolism of 7-MEOTA-tryptophan hybrids hampers their passage into brain
Published in Journal of pharmaceutical and biomedical analysis (10-09-2019)“…•Potent multitarget anti-Alzheimer’s compounds – S-K1025 and S-K1026 – fail to enter the brain in rats.•These compounds are prone to metabolism both in vitro…”
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UHPLC-HRMS study of pharmacokinetics of a novel hybrid cholinesterase inhibitor K1234: A comparison between in silico, in vitro and in vivo data
Published in Journal of pharmaceutical and biomedical analysis (20-09-2022)“…Alzheimer's disease (AD) is one of the most common forms of dementia. Current anti-AD therapeutics exploit the cholinergic hypothesis of its pathophysiology;…”
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UHPLC-Orbitrap study of the first phase tacrine in vitro metabolites and related Alzheimer's drug candidates using human liver microsomes
Published in Journal of pharmaceutical and biomedical analysis (05-02-2023)“…Tacrine was the first drug used in the therapy of Alzheimer’s disease (AD) and is one of the leading structures frequently pursued in the drug discovery of…”
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Tetroxime: reactivation potency - in vitro and in silico study
Published in RSC advances (01-01-2017)“…Acetylcholinesterase (AChE) reactivators (oximes) are generally used as treatment in cases of nerve agent poisoning. There is no single oxime applicable in…”
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A 7-methoxytacrine-4-pyridinealdoxime hybrid as a novel prophylactic agent with reactivation properties in organophosphate intoxication
Published in Toxicology research (Cambridge) (01-07-2016)“…Chemical warfare agents constitute an increasing threat to both military and civilian populations. Therefore, effective prophylactic approaches are urgently…”
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P.5.a.001 - In vitro effects of newly developed cholinesterase inhibitors and ABAD modulators on mitochondrial respiration
Published in European neuropsychopharmacology (01-10-2017)Get full text
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In vitro effects of newly developed cholinesterase inhibitors and ABAD modulators on mitochondrial respiration
Published in European neuropsychopharmacology (01-10-2017)Get full text
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P.8.b.001 Interaction of acetylcholinesterase reactivators with albumin
Published in European neuropsychopharmacology (01-10-2012)Get full text
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P-451 - Changes of cellular respiration in patients with alzheimer's disease
Published in European psychiatry (2012)“…Introduction Alzheimer's disease (AD) is the most frequent neurodegenerative disease, characterized by progressive decline in variety of higher brain functions…”
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P.760 Effects of novel cholinesterase inhibitors on mitochondrial respiration and MAO activity - in vitro study
Published in European neuropsychopharmacology (01-11-2020)Get full text
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7-methoxyderivative of tacrine is a potent open channel blocker of NMDA receptors
Published in Journal of the neurological sciences (15-10-2017)Get full text
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Non-peptide orexin 2 receptor modulators as promising way to treatment of narcolepsy/insomnia
Published in Journal of the neurological sciences (15-10-2019)Get full text
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P.525 Tacrine derivatives as potent inhibitors of N-methyl-D-aspartate receptors with neuroprotective activity
Published in European neuropsychopharmacology (01-12-2019)Get full text
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Tacrine First-Phase Biotransformation and Associated Hepatotoxicity: A Possible Way to Avoid Quinone Methide Formation
Published in ACS chemical biology (15-09-2023)“…Tacrine was withdrawn from clinical use as a drug against Alzheimer’s disease in 2013, mainly due to drug-induced liver injury. The culprit of…”
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Tacrine - tryptophan derivatives – novel agents against the Alzheimer’s disease
Published in Journal of the neurological sciences (15-10-2017)Get full text
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1-Benzyl-4-methylpiperidinyl moiety in donepezil: The priority ticket across the blood-brain-barrier in rats
Published in Journal of chromatography. B, Analytical technologies in the biomedical and life sciences (15-08-2018)“…•We present a validated UHPLC-HRMS method used for pharmacokinetic analysis of donepezil and its three structural “fragments”.•One of the fragments accumulates…”
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Rare genetic variability in human drug target genes modulates drug response and can guide precision medicine
Published in Science advances (03-09-2021)“…Interindividual variability in drug response constitutes a major concern in pharmacotherapy. While polymorphisms in genes involved in drug disposition have…”
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