Tacrine and its 7-methoxy derivate; time-change concentration in plasma and brain tissue and basic toxicological profile in rats

J Zdarova Karasova, O Soukup… - Drug and Chemical …, 2021 - Taylor & Francis
… The explanation that lower po acute toxicity of 7-MEOTA depends only on differences in …
peak area ratio tacrine or 7-MEOTA/IS versus the tacrine or 7-MEOTA concentration showed a …

Inhibitors of acetylcholinesterase derived from 7-methoxytacrine and their effects on the choline transporter CHT1

Z Kristofikova, J Ricny, O Soukup… - Dementia and Geriatric …, 2017 - karger.com
… 7-methoxytacrine (7-MEOTA), since this analogue of tacrine is … differences between tacrine
and the 7-MEOTA/K576/K577 group (p = 0.5895); (ii) significant differences between tacrine

UHPLC-Orbitrap study of the first phase tacrine in vitro metabolites and related Alzheimer's drug candidates using human liver microsomes

M Novak, B Svobodova, J Konecny, A Kuratkova… - … of Pharmaceutical and …, 2023 - Elsevier
… to be a culprit of toxicity) was found compared to tacrine and 7-MEOTA, probably due to the
… and characterization of ten tacrine and ten 7-MEOTA dihydroxymetabolites (accounting for a …

Effects of novel tacrine derivatives on mitochondrial energy metabolism and monoamine oxidase activity—in vitro study

J Hroudová, T Nováková, J Korábečný, D Maliňák… - Molecular …, 2021 - Springer
7-MEOTA was evaluated as a comparative molecule in all measurements; MAO-A
inhibition by the compounds was compared … Our finding that all compounds of the tacrine/7-MEOTA/6-…

Tacrine first-phase biotransformation and associated hepatotoxicity: a possible way to avoid quinone methide formation

M Novak, M Vajrychova, S Koutsilieri… - ACS Chemical …, 2023 - ACS Publications
… toxicity, we first incubated HLMs together with tacrine derivatives (tacrine, 7-MEOTA, 7-Ph-O-…
Specifically, we compared the metabolic profiles of tacrine and its derivatives using the well-…

Tacrine-based Multifunctional Agents in Alzheimer's Disease: An Old Story in Continuous Development §

A Milelli, A De Simone, N Ticchi… - Current Medicinal …, 2017 - ingentaconnect.com
… in HepG2 cell line in comparison with tacrine at 24h and 0-50 μM and it could be observed
that compound 68 is characterized by a safer profile compared to compound 65 and tacrine. …

[HTML][HTML] Multi-target-directed therapeutic potential of 7-methoxytacrine-adamantylamine heterodimers in the Alzheimer's disease treatment

Z Gazova, O Soukup, V Sepsova, K Siposova… - … et Biophysica Acta (BBA …, 2017 - Elsevier
… Our findings provide evidence solely for a comparison of … tacrine effects stem from long-term
and repeated administration [86]. Since we do not have all these data in hand for 7-MEOTA-…

UHPLC-HRMS study of anti-Alzheimer's drug candidates: metabolism of 7-MEOTA-tryptophan hybrids hampers their passage into brain

M Mžik, J Žďárová-Karasová, K Chalupová… - … of Pharmaceutical and …, 2019 - Elsevier
tacrine led to its withdrawal from clinical use several years later [5]. Many studies show that
chemical modification of tacrine reduces its toxicity, eg: 7-methoxytacrine (7-MEOTAcompare

Psychotomimetic agent BZ (3-quinuclidinyl benzilate)

J Fusek, A Dlabkova, J Misik - Handbook of toxicology of chemical warfare …, 2020 - Elsevier
7-MEOTA was found to be markedly less toxic than tacrine also for dogs and rabbits. …
lower compared with parent compound tacrine and eight times lower compared with 7-MEOTA. …

An HPLC–MS method for the quantification of new acetylcholinesterase inhibitor PC 48 (7-MEOTA-donepezil like compound) in rat plasma: Application to a …

M Mzik, J Korabecny, E Nepovimova, V Voříšek… - … of Chromatography B, 2016 - Elsevier
7-MEOTA, was developed as a derivative of tacrine (1,2,3,4-tetrahydroacridin-9-amine, THA),
and was the first AD drug approved by FDA for clinical practice [8]. 7-MEOTA … by comparing