219811-17-3Relevant academic research and scientific papers
Synthesis and structure-affinity relationships of 1,3,5-alkylsubstituted cyclohexylamines binding at NMDA receptor PCP site
Jirgensons, Aigars,Kauss, Valerjans,Kalvinsh, Ivars,Gold, Markus R.,Danysz, Wojciech,Parsons, Chris G.,Quack, Gunter
, p. 555 - 565 (2007/10/03)
A series of 1,3,5-alkylsubstituted cyclohexylamines 2 were synthesized as ligands for the N-methyl-D-aspartate (NMDA) receptor phencyclidine (PCP) binding site. Pure diastereomers with defined configuration of amino group 2- ax and 2-eq were obtained. The optimal size of 1,3,5-substituents was determined for cyclohexylamines 2 with an equatorial amino group in the lowest energy conformation using Hansch analysis. According to the data, the lipophilic part of cyclohexylamines 2 does not discriminate between hydrophobic regions of the PCP binding site but rather recognizes this site as a whole lipophilic pocket. (C) 2000 Editions scientifiques et medicales Elsevier SAS.
