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 alpha2C adrenergic receptor antagonist |
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| Authors: | 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 |
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| Institution: | Pfizer Global Research and Development, Cambridge Laboratories, Cambridge, MA 02139, USA. |
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| Abstract: | The discovery of the CNS-penetrant and selective alpha(2C) adrenergic receptor antagonist N-{2-4-(2,3-dihydro-benzo1,4]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 alpha(2)-AR subtypes. |
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