Title of article :
Modulation of selective serotonin reuptake inhibitor and 5-HT1A antagonist activity in 8-aza-bicyclo[3.2.1]octane derivatives of 2,3-dihydro-1,4-benzodioxane
Author/Authors :
Adam M. Gilbert، نويسنده , , Gary P. Stack، نويسنده , , Ramaswamy Nilakantan، نويسنده , , Jason Kodah، نويسنده , , Megan Tran، نويسنده , , Rosemary Scerni، نويسنده , , Xiaojie Shi، نويسنده , , Deborah L. Smith، نويسنده , , Terrance H. Andree، نويسنده ,
Abstract :
2,3-Dihydro-1,4-benzodioxanes with aryl 8-aza-bicyclo[3.2.1]oct-3-ene attachments 2 produce compounds with potent 5-HT-T affinity, and weak 5-HT1A affinity and α1 affinity. This compares with 2,3-dihydro-1,4-benzodioxanes containing 8-aza-bicyclo[3.2.1] octan-3-ol attachments 4 which possess potent 5-HT1A affinity, moderate to good selectivity over α1 and little 5-HT-T affinity. A 3-benzothiophene analogue of 4 (30) was synthesized which possesses potent 5-HT1A affinity and especially good selectivity over both α1 and 5-HT-T.
