Identification and SAR around N-{2-[4-(2, 3-dihydro-benzo [1, 4] dioxin-2-ylmethyl)-[1, 4] diazepan-1-yl]-ethyl}-2-phenoxy-nicotinamide, a selective α 2C adrenergic …
…, B Campbell, C Li, D Hidayetoglu, DS Johnson…
文献索引：Patel, Snahel D.; Habeski, Wendy M.; Min, Hyunsuk; Zhang, Jiansu; Roof, Robin; Snyder, Bradley; Bora, Gary; Campbell, Brian; Li, Cheryl; Hidayetoglu, Debra; Johnson, Douglas S.; Chaudhry, Archana; Charlton, Maura E.; Kablaoui, Natasha M. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 20 p. 5689 - 5693
The discovery of the CNS-penetrant and selective α2C adrenergic receptor antagonist N-{2- [4-(2, 3-dihydro-benzo [1, 4] dioxin-2-ylmethyl)-[1, 4] diazepan-1-yl]-ethyl}-2-phenoxy- nicotinamide, 13 is described. Structure–activity studies demonstrate the structural requirements for binding affinity, functional activity, and selectivity over other α2-AR subtypes.
