Conformationally constrained 5-(thienyl)tryptamine derivatives as serotonin 5-HT1B/1D receptor agonists:: Potential treatments for migraine

In the search for human 5-HT1D selective agonists, a series of conformationally constrained 5-(2- or 3-thienyl)tryptamine derivatives 7, 10, and 12 have been synthesized. In vitro binding experiments at the cloned human 5-HT1D and 5-HT1B receptors has shown that some these compounds are potent and 5-HT1D versus 5- HT1B selective ligands. These compounds were evaluated as agonists in the model of rabbit. isolated saphenous vein constriction, therefore, potential treatments for migraine.