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

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Slassi A, Edwards L, O'Brien A, Meng CQ, Xin T, Seto C, Lee DK, MacLean N, Hynd D, Chen C, Wang H, Kamboj R, Rakhit S

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

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

PubMed ID

10937729 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Sumatriptan	5-hydroxytryptamine receptor 1B	Ki (nM)	47.9	N/A	N/A	Details
Sumatriptan	5-hydroxytryptamine receptor 1D	Ki (nM)	5.5	N/A	N/A	Details