Razet R, Thomet U, Furtmüller R, Jursky F, Sigel E, Sieghart W, Dodd R H
Institut de Chimie des Substances Naturelles, Centre National de la Recherche Scientifique, Gif-sur-Yvette, France.
Bioorg Med Chem Lett. 2000 Nov 20;10(22):2579-83. doi: 10.1016/s0960-894x(00)00514-x.
Analogues of bicuculline devoid of the benzo ring fused to the lactone moiety were prepared by reacting 2-(tert-butyl-dimethylsiloxy)furans with 3,4-dihydroisoquinolinium salts. Some of these compounds (e.g., ROD185, 8) acted as modulators of the GABAA receptor, displacing ligands of the benzodiazepine binding site. They also strongly stimulated GABA currents mediated by recombinant GABA(A) receptors expressed in Xenopus oocytes.
通过使2-(叔丁基-二甲基硅氧基)呋喃与3,4-二氢异喹啉鎓盐反应，制备了不含与内酯部分稠合的苯环的荷包牡丹碱类似物。其中一些化合物（例如ROD185、8）作为GABAA受体的调节剂，取代苯二氮䓬结合位点的配体。它们还强烈刺激由非洲爪蟾卵母细胞中表达的重组GABA(A)受体介导的GABA电流。
