产品描述: 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 |
靶点:
human 5-HT1F Receptor:0.006 μM (Ki);human 5-HT1A Receptor:0.530 μM (Ki);human 5-HT1B Receptor:0.549 μM (Ki);human 5-HT1D Receptor:0.575 μM (Ki);human 5-HT1E Receptor:1.415 μM (Ki);human 5-HT2B Receptor:1.695 μM (Ki);Human 5-HT2A Receptor:3.499 μM (Ki);Human 5-HT3A 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) |
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 |
参考文献:
1. Phebus LA, Johnson KW, Zgombick JM, Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brainpenetration and activity in the neurogenic dural inflammation model of migraine. Life Sci. 1997;61(21):2117-26. 2. Scholpa NE, et al. 5-HT1F receptor-mediated mitochondrial biogenesis for the treatment of Parkinson's disease. Br J Pharmacol. 2018 Jan;175(2):348-358. |
溶解性:
Soluble in DMSO |
保存条件:
RT |
配置溶液浓度参考:
|
1mg |
5mg |
10mg |
1 mM |
2.578 ml |
12.891 ml |
25.781 ml |
5 mM |
0.516 ml |
2.578 ml |
5.156 ml |
10 mM |
0.258 ml |
1.289 ml |
2.578 ml |
50 mM |
0.052 ml |
0.258 ml |
0.516 ml |
|
注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |