Basic information

Investigator: RNDr. Karel Valeš, Ph.D.
Main recipient: University Hospital Hradec Králové - PharmDr. Ondřej Soukup, Ph.D.
Co-recipient: National Institute of Mental Health (NIMH); Institute of Experimental Medicine of the Czech Academy of Science - Mgr. Martin Horák Ph.D.
Research period: 1/1/2020 - 31/12/2022
Total budget: 14,980,000 CZK
NIMH budget: 4,996,000 CZK
Supported by: Czech Science Foundation (GAČR)

Annotation

In this project, we would like to follow-up the proof-of-concept project no. 16-08554S, focused on the dually acting tacrine derivatives, in the preclinically-oriented project focused on 7-MEOTA and its derivatives, where we would like to investigate and understand the mechanism of interaction of such compounds with the open-channel of the NMDA receptor. We will use in vitro data of native and specifically mutated NMDA receptors, molecular docking approaches and quantitative structure-activity relationship (QSAR) approach to describe such interaction. Such investigation is giving us also a tool for designing even more effective neuroprotectants. Therefore, the candidates with the most promising pre-clinical potential showing suitable NMDA receptor inhibitory properties while preserving anti-acetylcholinesterase activity will be subjected to thorough preclinical in vivo testing in order to evaluate and verify the real neuroprotective and pro-cognitive value rising from the dual character of such compounds.