Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, United States.
Bioorg Med Chem Lett. 2010 Feb 1;20(3):1114-7. doi: 10.1016/j.bmcl.2009.12.023. Epub 2009 Dec 6.
Preclinical studies suggest that compounds with dual norepinephrine reuptake inhibitor (NRI) and 5-HT(1A) partial agonist properties may provide an important new therapeutic approach to ADHD, depression, and anxiety. Reported herein is the discovery of a novel chemical series with a favorable NRI and 5-HT(1A) partial agonist pharmacological profile as well as excellent selectivity for the norepinephrine transporter over the dopamine transporter.
临床前研究表明,具有双重去甲肾上腺素再摄取抑制剂(NRI)和 5-HT(1A)部分激动剂特性的化合物可能为 ADHD、抑郁症和焦虑症提供一种重要的新治疗方法。本文报道了一类具有良好 NRI 和 5-HT(1A)部分激动剂药理学特性的新型化学系列,以及对去甲肾上腺素转运体相对于多巴胺转运体具有优异选择性的化合物。