ly344864

LY344864 is a **potent, highly selective small molecule agonist** of the **5-hydroxytryptamine 1F receptor** (5-HT1F or serotonin 1F receptor)[1][3][5][7][9]. It displays >80-fold selectivity for 5-HT1F compared to other serotonin receptors, with low nanomolar binding affinity (Ki ≈ 6 nM) and potent functional activity (EC50 ≈ 3 nM) as a full agonist[1][3][7][9]. LY344864’s mechanism of action is **orthosteric agonism** at the 5-HT1F receptor, inhibiting neurogenic dural inflammation and trigeminovascular nociception in animal models, relevant to migraine pathophysiology[3][5][6]. It has demonstrated efficacy inhibiting dural protein extravasation and modulating trigeminal neuronal activation[3][6]. More recently, LY344864 has been shown to induce mitochondrial biogenesis and restore vascular integrity and locomotor function in models of spinal cord injury[2]. Despite antimigraine activity in preclinical studies, LY344864 was not advanced for clinical development, but continues to be widely used as a research tool compound for 5-HT1F biology[5][7].

Brand names

LY344864LY-344864LY 344864

Other names

LY344864 hydrochlorideLY-344864 hydrochlorideLY 344864 hydrochloride