Chlorophenylpiperazine analogues as high affinity dopamine transporter ligands.

Chlorophenylpiperazine analogues as high affinity dopamine transporter ligands.
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DOI:
10.1016/j.bmcl.2013.09.038
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发表时间:
2013-12-15
影响因子:
2.7
通讯作者:
Coop, Andrew
Coop, Andrew
中科院分区:
医学4区
文献类型:
--
作者:
Motel, William C.;Healy, Jason R.;Viard, Eddy;Pouw, Buddy;Martin, Kelly E.;Matsumoto, Rae R.;Coop, Andrew

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选择性σ-2配体仍然是减轻精神刺激剂影响的药物的活性靶点。在我们的研究过程中,我们发现1-(3-氯苯基)-4-苯乙基哌嗪实际上优先增加了对多巴胺转运体的亲和力,从而产生了一个高选择性的σ-2-选择性苯基哌嗪类似物。
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.
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