LY334370 is an agonist of the serotonin (5-HT) receptor subtype 5-HT1F (Kd = 0.446 nM). It is selective for 5-HT1F over other G protein-coupled 5-HT receptor subtypes with Ki values ranging from 16.4 to greater than 3,000 nM in radioligand binding assays. LY334370 inhibits forskolin-induced cAMP accumulation in mouse L-M(TK-) cell membranes expressing the recombinant human 5-HT1F receptor (EC50 = 1.51 nM). It decreases electrically stimulated extravasation of plasma proteins in the dura mater in a guinea pig trigeminal nerve model of migraine headache.