期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 54, 期 20, 页码 7422-7426出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm200676f
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资金
- DFG [EN 875/1-1]
Racemic and enantiopure 8-substituted derivatives of the lead dopamine receptor antagonist LE 300 (1) were prepared, and their affinities for the dopamine receptors (D(1)-D(5)) were tested. The separate enantiomers showed significantly different affinities; the (8S)-methyl and (8R)-hyroxymethyl derivatives where the substituents point below the reference plane of the indolo[3,2-f][3]benzazecine scaffold were markedly more active than their enantiomeric counterparts. The racemic 8-carboxy derivative was shown to be selective for the D(5)-receptor, even against D(1).
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