基于γ-氨基醇官能团合成一种强效广谱5-羟色胺、去甲肾上腺素、多巴胺再摄取抑制剂（SNDRI）和一种物种选择性多巴胺再摄取抑制剂。
Synthesis of a potent wide-spectrum serotonin-, norepinephrine-, dopamine-reuptake inhibitor (SNDRI) and a species-selective dopamine-reuptake inhibitor based on the gamma-amino alcohol functional group.
作者信息
Carlier P R, Lo M M, Lo P C, Richelson E, Tatsumi M, Reynolds I J, Sharma T A
机构信息
Department of Chemistry, Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong.
出版信息
Bioorg Med Chem Lett. 1998 Mar 3;8(5):487-92. doi: 10.1016/s0960-894x(98)00062-6.
A series of gamma-amino alcohols were synthesized and screened for reuptake inhibition and noncompetitive NMDA antagonism. Compound (+/-)-3f simultaneously and potently inhibits reuptake of 5-HT, NE, and DA, representing a potential wide-spectrum reuptake inhibitor antidepressant. In addition, comparative rat and human studies uncovered a species-selective DA reuptake inhibitor (+/-)-2e, KD(hDAT)/KD(rDAT) = 97.
合成了一系列γ-氨基醇，并对其进行再摄取抑制和非竞争性NMDA拮抗作用的筛选。化合物(±)-3f同时且强效地抑制5-羟色胺、去甲肾上腺素和多巴胺的再摄取，是一种潜在的广谱再摄取抑制型抗抑郁药。此外，大鼠与人的对比研究发现了一种物种选择性多巴胺再摄取抑制剂(±)-2e，KD(人多巴胺转运体)/KD(大鼠多巴胺转运体)=97。
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