3-(Piperazinylpropyl) indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents

…, LJ Street, S Goodacre, SC Hobbs, P Hunt…

文献索引：Chambers, Mark S.; Street, Leslie J.; Goodacre, Simon; Hobbs, Sarah C.; Hunt, Peter; Jelley, Richard A.; Matassa, Victor G.; Reeve, Austin J.; Sternfeld, Francine; Beer, Margaret S.; Stanton, Josephine A.; Rathbone, Denise; Watt, Alan P.; MacLeod, Angus M. Journal of Medicinal Chemistry, 1999 , vol. 42, # 4 p. 691 - 705

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被引用次数: 30

摘要

Clinically effective antimigraine drugs such as Sumatriptan have similar affinity at h5-HT1D and h5-HT1B receptors. In the search for a h5-HT1D-selective agonist as an antimigraine agent, a novel series of 3-(propylpiperazinyl) indoles have been synthesized and evaluated at h5-HT1D and h5-HT1B receptors. This class of compounds has provided subnanomolar, fully efficacious h5-HT1D agonists with up to 200-fold selectivity for the h5-HT1D receptor ...