Mesolimbic selective antipsychotic arylcarbamates

Article abstract of DOI:10.1016/S0223-5234(99)80009-9

4-(6-Fluoro-1,2-benzisoxazol-3-yl)piperidine has been linked to various arylcarbamates to obtain compounds having affinity for dopamine-D₁ and -D₂, serotonin 5HT(2A) and α₁-adrenoceptors. When linkers with restricted flexibility are used, the biological activity is reduced indicating that a bended conformation is needed in this series of bioactive molecules. Compounds with a relatively low D₂/5HT(2A) affinity ratio in receptor binding experiments and high affinity for the α₁-adrenoceptors exhibit a pharmacological profile which suggests a preferential effect on the mesocorticolimbic dopaminergic system and an 'atypical' antipsychotic activity.