Modulation of selective serotonin reuptake inhibitor and 5-HT 1A antagonist activity in 8-aza-bicyclo [3.2. 1] octane derivatives of 2, 3-dihydro-1, 4-benzodioxane

…, R Nilakantan, J Kodah, M Tran, R Scerni, X Shi…

文献索引：Gilbert, Adam M.; Stack, Gary P.; Nilakantan, Ramaswamy; Kodah, Jason; Tran, Megan; Scerni, Rosemary; Shi, Xiaojie; Smith, Deborah L.; Andree, Terrance H. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 2 p. 515 - 518

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被引用次数: 16

摘要

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 ...