氯苯哌嗪类似物作为高亲和力多巴胺转运体配体。
Chlorophenylpiperazine analogues as high affinity dopamine transporter ligands.
机构信息
Department of Pharmaceutical Sciences, University of Maryland, School of Pharmacy, 20 North Pine Street, Baltimore, MD, 21201, USA.
Department of Basic Pharmaceutical Sciences, West Virginia University, School of Pharmacy, One Medical Center Drive, Morgantown, WV, 26506, USA.
出版信息
Bioorg Med Chem Lett. 2013 Dec 15;23(24):6920-6922. doi: 10.1016/j.bmcl.2013.09.038. Epub 2013 Oct 15.
Abstract
Selective σ2 ligands continue to be an active target for medications to attenuate the effects of psychostimulants. In the course of our studies to determine the optimal substituents in the σ2-selective phenyl piperazines analogues with reduced activity at other neurotransmitter systems, we discovered that 1-(3-chlorophenyl)-4-phenethylpiperazine actually had preferentially increased affinity for dopamine transporters (DAT), yielding a highly selective DAT ligand.
摘要
选择性σ2 配体继续成为药物的一个活跃靶点，以减轻精神兴奋剂的影响。在我们研究确定减少其他神经递质系统活性的σ2 选择性苯基哌嗪类似物的最佳取代基的过程中，我们发现 1-(3-氯苯基)-4-苯乙基亚基哌嗪实际上对多巴胺转运体 (DAT) 具有优先增加的亲和力，产生了一种高度选择性的 DAT 配体。
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