Ward Simon E, Johnson Christopher N, Lovell Peter J, Scott Claire M, Smith Paul W, Stemp Geoffrey, Thewlis Kevin M, Vong Antonio K, Watson Jeannette M
Psychiatry Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK.
Bioorg Med Chem Lett. 2007 Sep 15;17(18):5214-7. doi: 10.1016/j.bmcl.2007.06.078. Epub 2007 Jun 30.
A series of 5-(piperidinylethyloxy)quinoline 5-HT(1) receptor ligands have been studied by elaboration of the series of dual 5-HT(1)-SSRIs reported previously. These new compounds display a different pharmacological profile with potent affinity across the 5-HT(1A), 5-HT(1B) and 5-HT(1D) receptors and selectivity against the serotonin transporter. Furthermore, they have improved pharmacokinetic profiles and CNS penetration.
通过对先前报道的一系列双重5-HT(1)-SSRI进行拓展，对一系列5-(哌啶基乙氧基)喹啉5-HT(1)受体配体进行了研究。这些新化合物表现出不同的药理特性，对5-HT(1A)、5-HT(1B)和5-HT(1D)受体具有强效亲和力，对5-羟色胺转运体具有选择性。此外，它们还具有改善的药代动力学特性和中枢神经系统渗透性。
