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Novel tryptophan dioxygenase inhibitors and combined tryptophan dioxygenase/5-HT reuptake inhibitors

DJ Madge, R Hazelwood, R Iyer, HT Jones…

文献索引:Madge; Hazelwood; Iyer; Jones; Salter Bioorganic and Medicinal Chemistry Letters, 1996 , vol. 6, # 7 p. 857 - 860

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被引用次数: 19

摘要

Tryptophan dioxygenase (TDO) is a liver enzyme that is responsible for the majority of the metabolism of tryptophan. A series of novel 3-(2-pyridylethenyl) indoles are shown to be potent inhibitors of TDO with selected members of the series also having 5-hydroxy tryptamine (5-HT) reuptake inhibitory activity. These compounds are shown to provide significant increases in the levels of tryptophan and 5-HT in the cerebrospinal fluid and ...