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Dokl Biochem Biophys. 2015;464:322-4. doi: 10.1134/S1607672915050142. Epub 2015 Oct 31.

Novel bivalent positive allosteric modulators of AMPA receptor.

Author information

1
Lomonosov Moscow State University, Moscow, 119991, Russia.
2
Institute of Physiologically Active Compounds, Russian Academy of Sciences, Chernogolovka, Moscow oblast, 142432, Russia.
3
Lomonosov Moscow State University, Moscow, 119991, Russia. vap@qsar.chem.msu.ru.
4
Institute of Physiologically Active Compounds, Russian Academy of Sciences, Chernogolovka, Moscow oblast, 142432, Russia. vap@qsar.chem.msu.ru.

Abstract

A positive allosteric modulator of AMPA receptors has been designed using computer-aided molecular modeling techniques. It possessed a record high experimentally confirmed potency in the picomolar concentration range and belongs to a new type of bivalent AMPA receptor ligands containing bicyclo[3.3.1]nonane scaffold. The suggested structure could serve as a basis for further optimization and development of drugs for the treatment of neurodegenerative diseases, cognition enhancement, and improvement of memory.

PMID:
26518559
DOI:
10.1134/S1607672915050142
[Indexed for MEDLINE]

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