Bernotas Ronald, Lenicek Steven, Antane Schuyler, Zhang Guo Ming, Smith Deborah, Coupet Joseph, Harrison Boyd, Schechter Lee E
Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA.
Bioorg Med Chem Lett. 2004 Nov 15;14(22):5499-502. doi: 10.1016/j.bmcl.2004.09.003.
Novel 1-(2-aminoethyl)-3-(arylsulfonyl)-1H-indoles were prepared. Binding assays indicated they are 5-HT(6) receptor ligands, among which N,N-dimethyl-N-(2-[3-(1-naphthylsulfonyl)-1H-indol-1-yl]ethyl)amine 8t and N-methyl-N-(2-[3-(1-naphthylsulfonyl)-1H-indol-1-yl]ethyl)amine 8u showed high affinity for 5-HT(6) receptors with K(i)=3.7 and 5.7 nM, respectively.
制备了新型的1-(2-氨基乙基)-3-(芳基磺酰基)-1H-吲哚。结合试验表明它们是5-HT(6)受体配体，其中N,N-二甲基-N-(2-[3-(1-萘基磺酰基)-1H-吲哚-1-基]乙基)胺8t和N-甲基-N-(2-[3-(1-萘基磺酰基)-1H-吲哚-1-基]乙基)胺8u对5-HT(6)受体表现出高亲和力，其K(i)分别为3.7和5.7 nM。
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