Tetracyclic analogues of [+]-S 14297: Synthesis and determination of affinity and selectivity at cloned human dopamine D3 vs D2 receptors
摘要:
Starting from the structure of the preferential D-3 antagonist S 14297 (1), we have prepared a series of cis and trans tetracyclic derivatives of general formula I in order to improve potency and selectivity for D-3 receptors. The trans oxazino derivative 2c, showed slightly increased affinity at D-3 receptors and double the selectivity for D-3 over D-2 receptors, in comparison to S 14297. Cis derivatives and compounds where R-1 is aralkyl were totally devoid of activity. (C) 1997 Elsevier Science Ltd.
Tetracyclic analogues of [+]-S 14297: Synthesis and determination of affinity and selectivity at cloned human dopamine D3 vs D2 receptors
摘要:
Starting from the structure of the preferential D-3 antagonist S 14297 (1), we have prepared a series of cis and trans tetracyclic derivatives of general formula I in order to improve potency and selectivity for D-3 receptors. The trans oxazino derivative 2c, showed slightly increased affinity at D-3 receptors and double the selectivity for D-3 over D-2 receptors, in comparison to S 14297. Cis derivatives and compounds where R-1 is aralkyl were totally devoid of activity. (C) 1997 Elsevier Science Ltd.