[Neurotensin receptor antagonists and therapeutical perspectives]

SR 48692 is the first non-peptide antagonist of neurotensin receptors. It is potent and selective vs the high-affinity binding sites and with a small activity on the levocabastine-sensitive binding sites. It is active on several species including man without partial agonist properties. In vivo, it is active by oral route with a long duration of action and it is able to cross the blood-brain barrier. As an antagonist of neurotensin receptors, SR 48692 modulates central dopaminergic neurons. Thus it might be considered as a good tool for investigating the pathophysiological role of neurotensin in psychiatric diseases.