产品
编 号:F233719
分子式:C21H22FN3O
分子量:351.42
产品类型
结构图
CAS No: 186544-26-3
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产品详情
生物活性:
LY 344864 is a selective, orally active 5-HT1F receptor agonist with a Ki of 6 nM. LY 344864 is a full agonist producing an effect similar in magnitude to serotonin itself. LY 344864 can cross the blood brain barrier to some extent.
体内研究:
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 model
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
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.
体外研究:
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.