下一代抗抑郁药的研究。第4部分：对5-羟色胺转运体和5-HT1A受体有亲和力的4-(5-氟-1H-吲哚-3-基)环己胺衍生物。
Studies towards the next generation of antidepressants. Part 4: derivatives of 4-(5-fluoro-1H-indol-3-yl)cyclohexylamine with affinity for the serotonin transporter and the 5-HT1A receptor.
作者信息
Evrard Deborah A, Zhou Ping, Yi Soo Y, Zhou Dahui, Smith Deborah L, Sullivan Kelly M, Hornby Geoffrey A, Schechter Lee E, Andree Terrance H, Mewshaw Richard E
机构信息
Chemical and Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543, USA.
出版信息
Bioorg Med Chem Lett. 2005 Feb 15;15(4):911-4. doi: 10.1016/j.bmcl.2004.12.064.
Derivatives of the serotonin reuptake inhibitor 4-(5-fluoro-1H-indol-3-yl)cyclohexylamine, in which serotonin 1A (5-HT(1A)) receptor pharmacophoric elements are incorporated, are reported. Analogs exhibiting affinity for both the serotonin transporter and the 5-HT(1A) receptor are described. Compounds containing 1-(4-indolyl)piperazine and 2-(1H-indol-4-yloxy)ethylamine are promising leads for further SAR studies.
据报道，5-羟色胺再摄取抑制剂4-(5-氟-1H-吲哚-3-基)环己胺的衍生物中引入了5-羟色胺1A（5-HT(1A)）受体药效基团。描述了对5-羟色胺转运体和5-HT(1A)受体均具有亲和力的类似物。含有1-(4-吲哚基)哌嗪和2-(1H-吲哚-4-基氧基)乙胺的化合物是进一步进行构效关系研究的有前景的先导化合物。
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