Synthesis and Serotonergic Activity of 3-[2-(Pyrrolidin-1-yl) ethyl] indoles: Potent Agonists for the h5-HT1D Receptor with High Selectivity over the h5-HT1B Receptor

…, MS Beer, A Heald, JA Stanton, B Sohal…

Index: Sternfeld, Francine; Guiblin, Alexander R.; Jelley, Richard A.; Matassa, Victor G.; Reeve, Austin J.; Hunt, Peter A.; Beer, Margaret S.; Heald, Anne; Stanton, Josephine A.; Sohal, Bindi; Watt, Alan P.; Street, Leslie J. Journal of Medicinal Chemistry, 1999 , vol. 42, # 4 p. 677 - 690

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Citation Number: 34

Abstract

The design, synthesis, and biological evaluation of a novel series of 3-[2-(pyrrolidin-1-yl) ethyl] indoles with excellent selectivity for h5-HT1D (formerly 5-HT1Dα) receptors over h5- HT1B (formerly 5-HT1Dβ) receptors are described. Clinically effective antimigraine drugs such as Sumatriptan show little selectivity between h5-HT1D and h5-HT1B receptors. The differential expression of h5-HT1D and h5-HT1B receptors in neural and vascular tissue ...