Biological Activity
Potent, selective 5-HT 1F receptor agonist (EC 50 = 3 nM). Displays > 80-fold selectivity over other 5-HT receptors (K i values are 0.006, 0.53, 0.55, 0.56, 1.42, 1.70, 3.50, 3.94 and 4.85 μ M for 5-HT 1F , 5-HT 1A , 5-HT 1B , 5-HT 1D , 5-HT 1E , 5-HT 2B , 5-HT 2C , 5-HT 2A and 5-HT 7 receptors respectively). Inhibits neurogenic dural inflammation in vivo following i.v. and oral administration.
IC 50
human 5-HT1F Receptor: 0.006 μM (Ki); human 5-HT1A Receptor: 0.530 μM (Ki); human 5-HT1B Receptor: 0.549 μM (Ki); human 5-HT1D Receptor: 0.575 μM (Ki); human 5-HT1E Receptor: 1.415 μM (Ki); human 5-HT2B Receptor: 1.695 μM (Ki); Human 5-HT2A Receptor: 3.499 μM (Ki); Human 5-HT3A Receptor: 3.935 mM (Ki); Human 5-HT7 Receptor: 4.851 μM (Ki); rat α2-adrenergic receptor: 3.69 μM (Ki); rat α1-adrenergic receptor: 5.06 μM (Ki)
