A 5-HT1F receptor antagonist
LY344864 is an agonist of the serotonin (5-HT) receptor subtype 5-HT1F (Ki = 6 nM).1 It is selective for 5-HT1F over 5-HT1A-E , 5-HT2A-C, and 5-HT7 receptors (Kis = 0.53-4.85 ?M), as well as dopamine D1 and D2, GABAA, histamine H1, muscarinic, and α1-, α2-, and β-adrenergic receptors with Ki values ranging from 3.69 to greater than 100 ?M. LY344864 inhibits forskolin-induced cAMP accumulation in L-M(TK-) cells expressing recombinant human 5-HT1F receptors with an EC50 value of 3 nM. It decreases electrically stimulated extravasation of plasma proteins in the dura mater in a rat trigeminal nerve model of migraine headache (ID50s = 0.6 and 2.1 ng/kg for i.v. and oral administration, respectively).
1.Phebus, L.A., Johnson, K.W., Zgombick, J.M., et al.Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: Binding affinities, brain penetration and activity in the neurogenic dural inflammation model of migraineLife Sci.61(21)2117-2126(1997)
动态评分
0.0