European Journal of Medicinal Chemistry p. 839 - 858 (1998)
Update date:2022-09-26
Topics:
Hansen, John Bondo
Fink-Jensen, Anders
Christensen, Birgitte V.
Gronvald, Frederick C.
Jeppesen, Lone
Mogensen, John P.
Nielsen, Erik B.
Scheideler, Mark A.
White, Francis J.
Zhang, Xu-Feng
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.
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