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Novel bivalent positive allosteric modulators of AMPA receptor.

ampa ampakine allosteric cognitive enhancement

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#1 3AlarmLampscooter

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Posted 10 November 2015 - 09:15 AM


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

 


 

Novel bivalent positive allosteric modulators of AMPA receptor.
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.

 







Also tagged with one or more of these keywords: ampa, ampakine, allosteric, cognitive enhancement

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