title: Novel bivalent positive allosteric modulators of AMPA receptor.
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.
authors.affiliation: Lomonosov Moscow State University, Moscow, 119991, Russia.|Institute of Physiologically Active Compounds, Russian Academy of Sciences, Chernogolovka, Moscow oblast, 142432, Russia.
authors.forename: M I
authors.initials: MI
authors.lastname: Lavrov
authors.affiliation: Institute of Physiologically Active Compounds, Russian Academy of Sciences, Chernogolovka, Moscow oblast, 142432, Russia.
authors.forename: V V
authors.initials: VV
authors.lastname: Grigor'ev
authors.affiliation: Institute of Physiologically Active Compounds, Russian Academy of Sciences, Chernogolovka, Moscow oblast, 142432, Russia.
authors.forename: S O
authors.initials: SO
authors.lastname: Bachurin
authors.affiliation: Lomonosov Moscow State University, Moscow, 119991, Russia. vap@qsar.chem.msu.ru.|Institute of Physiologically Active Compounds, Russian Academy of Sciences, Chernogolovka, Moscow oblast, 142432, Russia. vap@qsar.chem.msu.ru.
authors.forename: V A
authors.initials: VA
authors.lastname: Palyulin
authors.affiliation: Lomonosov Moscow State University, Moscow, 119991, Russia.|Institute of Physiologically Active Compounds, Russian Academy of Sciences, Chernogolovka, Moscow oblast, 142432, Russia.
authors.forename: N S
authors.initials: NS
authors.lastname: Zefirov
mesh_terms: D000494:Allosteric Regulation; D000818:Animals; D001643:Bridged Bicyclo Compounds / Q000737:chemistry / Q000494:pharmacology; D002478:Cells, Cultured; D017076:Computer-Aided Design; D015195:Drug Design; D018683:Excitatory Amino Acid Agents / Q000737:chemistry / Q000494:pharmacology*; D008024:Ligands; D008564:Membrane Potentials / Q000187:drug effects; D062105:Molecular Docking Simulation; D015394:Molecular Structure; D018696:Neuroprotective Agents / Q000737:chemistry / Q000494:pharmacology*; D018697:Nootropic Agents / Q000737:chemistry / Q000494:pharmacology*; D018408:Patch-Clamp Techniques; D011689:Purkinje Cells / Q000187:drug effects / Q000502:physiology; D051381:Rats; D018091:Receptors, AMPA / Q000378:metabolism*; D012984:Software
chemical_list: D001643:Bridged Bicyclo Compounds; D018683:Excitatory Amino Acid Agents; D008024:Ligands; D018696:Neuroprotective Agents; D018697:Nootropic Agents; D018091:Receptors, AMPA