ChemInform Abstract: N-(2-((Substituted Chroman-8-yl)oxy)ethyl)-4-(4-methoxyphenyl) butylamines: Synthesis and Wide Range of Antagonism at the Human 5- HT1A Receptor.
✍ Scribed by T. YASUNAGA; R. NAITO; T. KONTANI; S. TSUKAMOTO; T. NOMURA; T. YAMAGUCHI; T. MASE
- Publisher
- John Wiley and Sons
- Year
- 2010
- Weight
- 38 KB
- Volume
- 28
- Category
- Article
- ISSN
- 0931-7597
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✦ Synopsis
N-(2-((Substituted
Chroman-8-yl)oxy)ethyl)-4-(4-methoxyphenyl) butylamines: Synthesis and Wide Range of Antagonism at the Human 5-HT1A Receptor.
-A series of title compounds such as (VIII) and (XIV) as well as unsubstituted and 5-and 7-substituted derivatives are prepared from the corresponding 8-hydroxychroman intermediates. The compounds are evaluated for in vitro activity using radioligand binding assays and the forskolin-stimulated adenylate cyclase assay. Binding assays for 5-HT1A, α1, and D2 receptors are performed according to standard protocols using rat brain tissues. Among the series prepared (VIII) shows both extremely potent affinity and antagonism for the 5-HT1A receptor. -(YASUNAGA, T.;