LY344864

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

LY344864 是一种特异性受体激动剂，对最近克隆的 5-HT1F 受体的亲和力为 6 nM (Ki)。

LY344864 is a selective 5-HT1F receptor agonist with an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor. LY344864 possesses little affinity for the 56 other serotonergic and non-serotonergic neuronal binding sites examined. LY344864 was shown to be a full agonist producing an effect similar in magnitude to serotonin itself.

LY 344864 binds to human 5-HT1F, 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT3A, 5-HT2B, 5-HT2C, 5-HT7, rat α1-adrenergic, rat α2-adrenergic receptors with Kis of 0.006, 0.530, 0.549, 0.575, 1.415, 3.935, 1.695, 3.499, 4.851, 5.06 and 3.69 μM, respectively.LY 344864 is a inducer of mitochondrial biogenesis.

LY 344864 (0-10 ng/kg; p.o. or i.v.; once) inhibits neurogenic dural inflammation in rat migraine pain model.LY 344864 (1 mg/kg; i.v.; once) can cross the blood brain barrier to some extent in rats.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. Animal Model:Male Wistar rats, migraine pain modelDosage:1-10 ng/kg (oral), 0.3-2 ng/kg (intravenous)Administration:Oral, 75 minutes before trigeminal stimulation or intravenous, 10 minutes before trigeminal stimulationResult: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 modelDosage: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.

LY-344864 | LY344864 | LY-344864 HCl

Angiogenesis

FGFR

5-HT1F

Neurological Disease

——

186544-26-3

351.42

C21H22FN3O

>98% (HPLC)

DMSO : ≥ 350 mg/mL; 995.96 mM

CN(C)[C@@H]1CCc2c(C1)c1c([nH]2)ccc(c1)NC(=O)c1ccc(cc1)F.Cl

N-[(3R)-3-(Dimethylamino)-2,3,4,9-tetrahydro-1H-carbazol-6-yl]-4-fluorobenzamide hydrochloride

(-20℃)

With Ice Pack

≥ 2 years