5-Alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists |
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| Authors: | Slassi A Edwards L O'Brien A Meng C Q Xin T Seto C Lee D K MacLean N Hynd D Chen C Wang H Kamboj R Rakhit S |
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| Institution: | NPS Allelix Corp., Mississauga, Ontario, Canada. slassi@allelix.com |
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| Abstract: | A series of 5-alkyltryptamines (6) and the corresponding conformationally constrained analogues (8) have been synthesized. The structure activity relationships (SAR) at the 5-position of the indole skeleton and the ethylamine side chain have been studied. Functional activities were assessed using isolated rabbit saphenous vein. Potent, selective ligands were found (6e, Ki 2.5 nM, 5-HT1B/5-HT1D 125-fold) that have potential for treating acute migraine. |
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