Campiani, Giuseppe Angelis, Meri De Armaroli, Silvia Fattorusso, Caterina Catalanotti, Bruno Ramunno, Anna Nacci, Vito Novellino, Ettore Grewer, Christof Ionescu, Diana Rauen, Thomas Griffiths, Roger Sinclair, Colin Fumagalli, Elena Mennini, Tiziana A Rational Approach to the Design of Selective Substrates and Potent Nontransportable Inhibitors of the Excitatory Amino Acid Transporter EAAC1 (EAAT3). New Glutamate and Aspartate Analogues as Potential Neuroprotective Agents Two three-dimensional receptor interaction models for EAAT substrates and nontransportable inhibitors have been developed, and new glutamate (Glu) and aspartate (Asp) analogues have been synthesized. The analogues <b>1a</b> and <b>3</b> represent novel lead compounds for the development of EAAT substrates and nontransportable inhibitors, selective for EAATs over iGluRs, as possible neuroprotective agents useful to minimize the progression of chronic or acute neurodegenerative diseases. The role played by the protonatable amine function in the interaction with EAATs has been discussed. analogue;nontransportable inhibitors;protonatable amine function;Potent Nontransportable Inhibitors;EAAT substrates;receptor interaction models;Transporter EAAC 1;Potential Neuroprotective Agents 2001-07-12
    https://acs.figshare.com/articles/journal_contribution/A_Rational_Approach_to_the_Design_of_Selective_Substrates_and_Potent_Nontransportable_Inhibitors_of_the_Excitatory_Amino_Acid_Transporter_EAAC1_EAAT3_New_Glutamate_and_Aspartate_Analogues_as_Potential_Neuroprotective_Agents/3680784
10.1021/jm015509z.s001