Author/Authors :
Abdelmalik Slassi*، نويسنده , , Louise Edwards، نويسنده , , Anne OʹBrien، نويسنده , , Charles Q. Meng، نويسنده , , Tao Xin، نويسنده , , Caroline Seto، نويسنده , , David K. H. Lee، نويسنده , , Neil MacLean، نويسنده , , Donna Hynd، نويسنده , , Cora Chen، نويسنده , , Hong Wang، نويسنده , , Rajender Kamboj، نويسنده , , Suman Rakhit، نويسنده ,
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.
