Moulder Center for Drug Discovery Research, Temple University School of Pharmacy, 3307 North Broad Street, Philadelphia, PA 194140, USA.
Department of Pharmacology and Neuroscience, University of North Texas Health Science Center, 3500 Camp Bowie Blvd, Fort Worth, TX 76107, USA.
Bioorg Med Chem Lett. 2019 Sep 15;29(18):2690-2694. doi: 10.1016/j.bmcl.2019.07.020. Epub 2019 Jul 11.
As part of our on-going effort to explore the role of dopamine receptors in drug addiction and identify potential novel therapies for this condition, we have a identified a series of N-(4-(4-phenyl piperazin-1-yl)butyl)-4-(thiophen-3-yl)benzamide D ligands. Members of this class are highly selective for D versus D, and we have identified two compounds (13g and 13r) whose rat in vivo IV pharmacokinetic properties that indicate that they are suitable for assessment in in vivo efficacy models of substance use disorders.
作为我们探索多巴胺受体在药物成瘾中的作用并为这种情况确定潜在新疗法的持续努力的一部分，我们已经鉴定了一系列 N-(4-(4-苯基哌嗪-1-基)丁基)-4-(噻吩-3-基)苯甲酰胺 D 配体。该类别的成员对 D 与 D 的选择性很高，我们已经鉴定出两种化合物（13g 和 13r），其大鼠体内 IV 药代动力学特性表明它们适合用于物质使用障碍的体内疗效模型的评估。
