ChemicalBook Product Catalog Biochemical Engineering Biochemical Reagents Agonist Inhibitors LY 344864

LY 344864

Product NameLY 344864
CAS186544-26-3
MFC21H22FN3O
MW351.42
EINECS
MOL File186544-26-3.mol

Chemical Properties

Boiling point	471.9±45.0 °C(Predicted)
Density	1.28±0.1 g/cm3(Predicted)
storage temp.	Store at +4°C
solubility	DMSO : ≥ 350 mg/mL (995.96 mM)
pka	14.12±0.40(Predicted)
form	Powder
color	White to off-white
Water Solubility	water: 10mM DMSO: 100mM
InChI	1S/C21H22FN3O.ClH/c1-25(2)16-8-10-20-18(12-16)17-11-15(7-9-19(17)24-20)23-21(26)13-3-5-14(22)6-4-13;/h3-7,9,11,16,24H,8,10,12H2,1-2H3,(H,23,26);1H/t16-;/m1./s1
InChIKey	OKUHLSYESBLBCP-PKLMIRHRSA-N

Safety Information

WGK Germany	WGK 3
Storage Class	11 - Combustible Solids

Usage And Synthesis

Uses

LY-344864 Hydrochloride is used as a selective 5-HTIF receptor agonist.

Biological Activity

Potent, selective 5-HT 1F receptor agonist (EC 50 = 3 nM). Displays > 80-fold selectivity over other 5-HT receptors (K i values are 0.006, 0.53, 0.55, 0.56, 1.42, 1.70, 3.50, 3.94 and 4.85 μ M for 5-HT 1F , 5-HT 1A , 5-HT 1B , 5-HT 1D , 5-HT 1E , 5-HT 2B , 5-HT 2C , 5-HT 2A and 5-HT 7 receptors respectively). Inhibits neurogenic dural inflammation in vivo following i.v. and oral administration.

in vivo

LY 344864 (0-10 ng/kg; p.o. or i.v.; once) inhibits neurogenic dural inflammation in rat migraine pain model^[1].
LY 344864 (1 mg/kg; i.v.; once) can cross the blood brain barrier to some extent in rats^[1].
LY 344864 (2 mg/kg; i.p.; daily for 14 days) attenuates dopaminergic neuron loss and improved behavioral endpoints in a Parkinson’s disease mouse model^[2].

Animal Model:	Male Wistar rats, migraine pain model^[1]
Dosage:	1-10 ng/kg (oral), 0.3-2 ng/kg (intravenous)
Administration:	Oral, 75 minutes before trigeminal stimulation or intravenous, 10 minutes before trigeminal stimulation
Result:	When given intravenously 10 minutes before stimulation, inhibited inflammation with an ID₅₀ (median infective dose) of 0.6 ng/kg. When administered orally 75 minutes before trigeminal stimulation, an ID₅₀ of 1.2 ng/kg was obtained.

Animal Model:	Male C57BL/6 mice, Parkinson’s disease model^[2]
Dosage:	2 mg/kg
Administration:	Intraperitoneal injection, daily for 14d beginning 7d post-lesion
Result:	Attenuated TH-ir loss in the striatum and substantia nigra compared to vehicle-treated lesioned animals, also increased locomotor activity in 6-hydroxydopamine lesioned mice, while vehicle treatment had no effect.

IC 50

human 5-HT_1F Receptor: 0.006 μM (Ki); human 5-HT_1A Receptor: 0.530 μM (Ki); human 5-HT_1B Receptor: 0.549 μM (Ki); human 5-HT_1D Receptor: 0.575 μM (Ki); human 5-HT_1E Receptor: 1.415 μM (Ki); human 5-HT_2B Receptor: 1.695 μM (Ki); Human 5-HT_2A Receptor: 3.499 μM (Ki); Human 5-HT_3A Receptor: 3.935 mM (Ki); Human 5-HT₇ Receptor: 4.851 μM (Ki); rat α2-adrenergic receptor: 3.69 μM (Ki); rat α1-adrenergic receptor: 5.06 μM (Ki)

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