Abstract:
In this paper, we describe the latest results involving molecular modeling and pharmacodynamic studies of the
selected highly lipophilic compounds acting by human GABA transporter 1 (hGAT1) inhibition. The chemical interaction of 17
GABA analogues with a model of hGAT1 is described using the molecular docking method. The biological role of GAT1 is
related to the regulation of GABA level in the central nervous system and GAT1 inhibition plays an important role in the
control of seizure threshold. To confirm that GAT1 can be also a molecular target for drugs used to treat other neurological and
psychiatric diseases (e.g., pain and anxiety), in the in vivo part of this study, potential antinociceptive and anxiolytic-like
properties of tiagabine, a selective GAT1 inhibitor, are described.
