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
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
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DOI：
10.1016/s0960-894x(98)00062-6
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发表时间：
1998-03-03
影响因子：
2.7
通讯作者：
Sharma, TA
中科院分区：
文献类型：
--
作者：
Carlier, PR;Lo, MMC;Sharma, TA
合成了一系列γ-氨基醇，并筛选了其再摄取抑制和非竞争性NMDA拮抗作用。化合物（+/-）-3f同时且有效地抑制5-HT、NE和DA的再摄取，代表潜在的广谱再摄取抑制剂抗抑郁药。此外，大鼠和人体比较研究发现了一种物种选择性DA再摄取抑制剂（+/-）-2e，K（D）（kDAT）/K（D）（rDAT）= 97。(C)1998爱思唯尔科技有限公司版权所有。
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, K(D)(kDAT)/K(D)(rDAT) = 97. (C) 1998 Elsevier Science Ltd. All rights reserved.