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N-Substituted-2-alkyl- and 2-arylnorapomorphines: Novel, highly active D2 agonists by Laura Herm; Sándor Berényi; Argo Vonk; Ago Rinken; Attila Sipos is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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Two synthesis routes have been elaborated for the preparation of novel N-substituted-2-alkyl- and 2-arylnorapomorphines. The first one utilizes the traditional methodology of N-substitution of morphinans before acid-catalyzed rearrangements into aporphinoids, while our new approach involves the N-substitution directly on the aporphine backbone. The aimed compounds were obtained in similar overall yields in different synthesis routes and were investigated with respect to their binding affinities and activities to dopamine D(2) and D(1) receptors. These studies revealed remarkable affinity and selectivity of some compounds for D(2) over D(1) receptor subtypes. Partial or full agonist properties were confirmed for all tested compounds.

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Author

Laura Herm; Sándor Berényi; Argo Vonk; Ago Rinken; Attila Sipos

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)

Published

2009

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)