Mahaney Paige E, Vu An T, McComas Casey C, Zhang Puwen, Nogle Lisa M, Watts William L, Sarkahian Ani, Leventhal Liza, Sullivan Nicole R, Uveges Albert J, Trybulski Eugene J
Chemical and Screening Sciences, Discovery Medicinal Chemistry, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA.
Bioorg Med Chem. 2006 Dec 15;14(24):8455-66. doi: 10.1016/j.bmc.2006.08.039. Epub 2006 Sep 14.
Compounds with a combination of norepinephrine and serotonin reuptake inhibition have been approved in the US and Europe for a number of indications, including major depressive disorder and pain disorders such as diabetic neuropathy and fibromyalgia. Efforts to design selective norepinephrine reuptake inhibitors based on SAR from the aryloxypropanamine series of monoamine reuptake inhibitors have led to the identification of a potent new class of dual acting norepinephrine and serotonin reuptake inhibitors, namely the 3-(1H-indol-1-yl)-3-arylpropan-1-amines.
去甲肾上腺素和5-羟色胺再摄取抑制相结合的化合物已在美国和欧洲获批用于多种适应症，包括重度抑郁症以及疼痛性疾病，如糖尿病性神经病变和纤维肌痛。基于芳氧基丙胺系列单胺再摄取抑制剂的构效关系设计选择性去甲肾上腺素再摄取抑制剂的研究工作，已促使人们鉴定出一类强效的新型双重作用去甲肾上腺素和5-羟色胺再摄取抑制剂，即3-(1H-吲哚-1-基)-3-芳基丙-1-胺。
