Prisinzano T, Law H, Dukat M, Slassi A, MaClean N, Demchyshyn L, Glennon R A
Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond 23298-0540, USA.
Bioorg Med Chem. 2001 Mar;9(3):613-9. doi: 10.1016/s0968-0896(00)00275-3.
Sumatriptan, a h5-HT1D and h5-HT1B receptor agonist used clinically as a migraine-abortive, produces certain side effects thought to result from its affinity for h5-HT1B receptors. The present investigation extends our work with benzylimidazolines as novel non-tryptamine h5-HT(1D/1B) ligands. The effect of N-methylation, N-benzylation, ring-aromatization, and variation of the imidazoline ring on affinity both at h5-HT1D and h5-HT1B receptors was examined. Several compounds were identified with good affinity and enhanced (i.e., > 100-fold) h5-HT1D versus hS-HT1B selectivity.
舒马曲坦是一种临床上用作偏头痛缓解药的5-羟色胺1D（h5-HT1D）和5-羟色胺1B（h5-HT1B）受体激动剂，它会产生某些副作用，这些副作用被认为是由其对h5-HT1B受体的亲和力所致。本研究扩展了我们以苄基咪唑啉作为新型非色胺类h5-HT(1D/1B)配体的工作。研究了N-甲基化、N-苄基化、环芳构化以及咪唑啉环的变化对h5-HT1D和h5-HT1B受体亲和力的影响。鉴定出了几种具有良好亲和力且h5-HT1D与h5-HT1B选择性增强（即>100倍）的化合物。
