Rigid analogues of buspirone and gepirone, 5-HT1A receptors partial agonists, were obtained. The compounds exhibited very low affinity to the receptors. Their structural features resembled to a large extent the arrangement of the respective structural elements found in the solid state of buspirone and in the theoretical structure of NAN-190 (5-HT1A… (More)
Modern concepts of buspirone activity as an anxiolytic drug are reviewed. Particular attention is focused on the molecular aspects of buspirone interactions in the phases that simulate cellular environment. Three-dimensional models of buspirone-serotonin receptor complexes are discussed as well.
A three-dimensional model of the 5-HT1A receptor in man was constructed by molecular-modelling techniques and used to study the molecular interactions of a series of buspirone analogues with the 5-HT1A receptor by molecular-mechanical-energy minimization and molecular-dynamics simulations. The receptor has seven trans-membrane alpha helices (TMHs) organized… (More)
The influence of 3-amino-2-oxazolidinone derivatives 1-9 on dopaminergic and serotoninergic neurotransmission was tested. It was found that all tested compounds exhibited modulating activity on one (or both) of the neurotransmissions, the effect being dependent on the aromatic ring substituent.