Further studies on the binding of N1-substituted tryptamines at h5-HT6 receptors
Further studies on the binding of N1-substituted tryptamines at h5-HT6 receptors
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DOI：
10.1016/j.bmcl.2006.12.089
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发表时间：
2007-03-15
影响因子：
2.7
通讯作者：
Glennon, Richard A.
中科院分区：
文献类型：
--
作者：
Nyandege, Abner;Kolanos, Renata;Glennon, Richard A.
N-1-芳磺酰基取代的N，N-二甲基色胺类似物与5-HT6受体结合。用类似的疏水性烷基取代芳基部分会导致亲和力降低，用苯磺酰基取代苯磺酰基部分也会导致亲和力降低。目前的研究结果表明，芳基(或取代芳基)磺酰基(而不是烷基磺酰基或苄基)部分最适合高亲和力结合，并进一步表明N-1-苯磺酰基-及其对应的N-1-苯基色胺以不同的方式结合。(C)2007爱思唯尔有限公司。保留所有权利。
N-1-Arylsulfonyl-substituted analogs of N,N-dimethyltryptamine bind at 5-HT6 receptors. Replacement of the aryl moiety with similarly hydrophobic alkyl substituents results in decreased affinity, as does replacement of a benzenesulfonyl moiety with a benzyl group. Current findings indicate that an aryl (or substituted aryl) sulfonyl (rather than alkylsulfonyl or benzyl) moiety is optimal for high-affinity binding, and further suggest that the N-1-benzenesulfonyl- and their corresponding N-1-benzyltryptamine counterparts bind in a different fashion. (c) 2007 Elsevier Ltd. All rights reserved.