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[3AlarmLampscooter]

http://www.ncbi.nlm.nih.gov/pubmed/26518559

 

 

Novel bivalent positive allosteric modulators of AMPA receptor.

Lavrov MI1,2, Grigor'ev VV2, Bachurin SO2, Palyulin VA3,4, Zefirov NS1,2.

Author information

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