琥珀酸拉斯米迪坦

  • 化学数据
CAS号 439239-92-6 货号 BCP17272
中文名 琥珀酸拉斯米迪坦
英文名 Lasmiditan succinate
中文别名 琥珀酸拉米地坦;
英文别名 COL-144; COL144; COL 144; LY573144; LY-573144; LY 573144;
分子式 C42H42F6N6O8 分子量 872.82
  • 用途
生物活性 Lasmiditan succinate is a novel and selective 5-HT(1F) receptor agonist with Ki of 2.1 nM versus Ki of 1043 nM and 1357 nM at the 5-HT(1B) and 5-HT(1D) receptors, respectively. For the understanding of migraine pathophysiology, it is very important to note that a selective 5-HT(1F) receptor agonist like lasmiditan is effective in the acute treatment of migraine. Thus, migraine can be treated with a drug that has no vasoconstrictor ability. While lasmiditan most likely is effective in the treatment of migraine attacks it had, unfortunately, a high incidence of CNS related AEs in the oral RCT. If confirmed in larger studies in phase III, this might adversely limit the use of this highly specific non-vascular acute treatment of migraine. Larger studies including the parameters of patients' preferences are necessary to accurately position this new treatment principle in relation to the triptans.
信号通路 Neuro Signaling Pathway GPCR/G Protein 
靶 点 5 HT Receptor/Serotonin Receptor 

结构式

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