新型3,3-二取代吡咯烷作为选择性5-羟色胺/去甲肾上腺素/多巴胺三重再摄取抑制剂
Novel 3,3-disubstituted pyrrolidines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors.
作者信息
Bannwart Linda M, Carter David S, Cai Hai-Ying, Choy Jason C, Greenhouse Robert, Jaime-Figueroa Saul, Iyer Pravin S, Lin Clara J, Lee Eun Kyung, Lucas Matthew C, Lynch Stephen M, Madera Ann Marie, Moore Amy, Ozboya Kerem, Raptova Lubica, Roetz Ralf, Schoenfeld Ryan C, Stein Karin Ann, Steiner Sandra, Villa Marzia, Weikert Robert J, Zhai Yansheng
机构信息
Roche Palo Alto LLC, 3431 Hillview Avenue, Palo Alto, CA 94304, USA.
出版信息
Bioorg Med Chem Lett. 2008 Dec 1;18(23):6062-6. doi: 10.1016/j.bmcl.2008.10.025. Epub 2008 Oct 11.
A series of 3,3-disubstituted pyrrolidine monoamine triple reuptake inhibitors were discovered. Analogues with low nanomolar potency, good human in vitro microsomal stability and in vitro permeability, and low drug-drug interaction potential are described. One example showed in vivo anti-depressant-like effects in the mouse tail suspension assay with a minimum effective dose of 30 mg/kg i.p.
发现了一系列3,3-二取代吡咯烷单胺三重再摄取抑制剂。描述了具有低纳摩尔效力、良好的人源体外微粒体稳定性和体外渗透性以及低药物-药物相互作用潜力的类似物。一个例子在小鼠悬尾试验中显示出体内抗抑郁样作用，腹腔注射的最小有效剂量为30 mg/kg。
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