Schmitz William D, Denhart Derek J, Brenner Allison B, Ditta Jonathan L, Mattson Ronald J, Mattson Gail K, Molski Thaddeus F, Macor John E
Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492-7660, USA.
Bioorg Med Chem Lett. 2005 Mar 15;15(6):1619-21. doi: 10.1016/j.bmcl.2005.01.059.
A series of N,N-dimethylhomotryptamines was prepared and their binding affinities at the serotonin transporter (SERT) were determined. Compounds possessing an electron withdrawing substituent at the C5-position of the indole nucleus were found to be potent SSRIs. Initial attempts at conformational restriction of the propylamine sidechain by incorporation of a quinuclidine bicyclic structure did not improve binding affinity at SERT.
制备了一系列N，N-二甲基高色胺，并测定了它们在5-羟色胺转运体（SERT）上的结合亲和力。发现在吲哚核的C5位具有吸电子取代基的化合物是有效的选择性5-羟色胺再摄取抑制剂（SSRI）。通过引入奎宁环双环结构对丙胺侧链进行构象限制的初步尝试并没有提高在SERT上的结合亲和力。
