LY 344864 hydrochloride is a selective receptor agonist with an affinity of 6 nM (Ki) at the 5-HT1F receptor.

5-HT7 receptor (human):4.851 μM (Ki), human 5-HT 1E Receptor:1.415 μM (Ki), 5-HT1D receptor (human):0.575 μM (Ki), human 5-HT 1F Receptor:0.006 μM (Ki), 5-HT2C receptor (human):3.499 μM (Ki), α1 adrenergic receptor (rat):5.06 μM (Ki), 5-HT3A Receptor (human):3.935 μM (Ki), 5-HT1B receptor (human):0.549 μM (Ki), α2 adrenergic receptor (rat):3.69 μM (Ki), 5-HT1A receptor (human):0.530 μM (Ki), 5-HT2B receptor (human):1.695 μM (Ki)

LY344864 is a selective 5-HT1F receptor agonist with an affinity of 6 nM (Ki). It possesses little affinity for the 56 other serotonergic and non-serotonergic neuronal binding sites examined. When examined for its ability to inhibit forskolininduced cyclic AMP accumulation in cells stably transfected with human 5-HT1F receptors, LY344864 is shown to be a full agonist producing an effect similar in magnitude to serotonin itself [1].

After an intravenous dose of 1 mg/kg, rat plasma LY344864 levels decrease over time, whereas brain cortex levels remaine relatively constant for the first 6 hours after injection. Oral and intravenous LY344864 administration potently inhibit dural protein extravasation caused by electrical stimulation of the trigeminal ganglion in rats [1]. Co-injection of LY 344864 and systemically ineffective doses of METH significantly decreases preference scores and the rewarding properties of METH during the reinstatement phase. In addition, administration of LY 344864 has no effect on the acquisition of CPP in rats [2].