LY334370 is an agonist of the serotonin (5-HT) receptor subtype 5-HT1F (Kd = 0.446 nM).1 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).2 It decreases electrically stimulated extravasation of plasma proteins in the dura mater in a guinea pig trigeminal nerve model of migraine headache.
1.Wainscott, D.B., Krushinski, J.H., Jr., Audia, J.E., et al.[3H]LY334370, a novel radioligand for the 5-HT1F receptor. I. In vitro characterization of binding propertiesNaunyn Schmiedebergs Arch. Pharmacol.371(3)169-177(2005) 2.Johnson, K.W., Schaus, J.M., Durkin, M.M., et al.5-HT1F receptor agonists inhibit neurogenic dural inflammation in guinea pigsNeuroreport8(9-10)2237-2240(1997)