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Bioorg Med Chem Lett. 2000 Aug 7;10(15):1707-9.

5-Alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists.

Author information

1
NPS Allelix Corp., Mississauga, Ontario, Canada. slassi@allelix.com

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.

PMID:
10937729
DOI:
10.1016/s0960-894x(00)00322-x
[Indexed for MEDLINE]

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