Ligand-5-HT1A receptor interaction

In the present paper the general structure and pharmacophore of some 5-HT1A receptor ligands are described, For several compounds (similar to 15)the i ntrinsic activity in lower lip retraction (postsynaptic, rat) and hypotherm ia (presynaptic, mice) tests was determined. For the identified functional presynaptic agonists and antagonists the influence on the brain serotonin l evel was examined. No direct correlation between the functional intrinsic a ctivity and the influence on the level was observed. Molecular modelling re vealed the possibility of the existence of different binding sites for diff erent examined compounds. (C) 2000 Elsevier Science S.A. All rights reserve d.