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氨基酸及其衍生物 抑制剂 常见氨基酸及蛋白质类药
LY310762
发布者:信康   浏览次数:
  • 产品名称:LY310762
  • CAS:192927-92-7
  • 别名:1-[2-[4-(4-氟苯甲酰基)-1-哌啶基]乙基]-1,3-二氢-3,3-二甲基-2H-吲哚-2-酮盐酸盐;LY310762;LY-310762
  • 英文名:LY310762
    • 储存条件 Desiccate at RT
    • 溶解度 DMSO: 10 mg/mL with heating, soluble
    • 形态white powder
    • 生物活性LY310762是一种5-HT1D受体拮抗剂,Ki为249 nM,对5-HT1B受体具有较低的亲和力。
    • 体外研究LY310762 has a higher affinity for the guinea pig 5-HT1D receptor than for the 5-HT1B receptor. LY310762 potentiates the potassium-induced [3H]5-HT outflow from guinea pig cortical slices with an EC50 of 30 nM. The maximum potentiation of the potassium-induced outflow which is obtained with LY310762 is about 40%. LY310762 blocks the decreased EPSC amplitude induced by Sumatriptan.
    • 体内研究Systemic administration of LY310762 (10 mg/kg i.p.) produces a further significant enhancement in the 5-HT response to fluoxetine (20 mg/kg i.p.) when compared to animals receiving a control vehicle injection. In fluoxetine treated animals, levels of 5-HT increases from 312±43% to a maximum of 683% after LY310762. In control animals, levels of 5-HT remains unchanged (250%). LY310762 administered alone also significantly increases basal levels of 5-HT above vehicle controls, reaching a maximum of 258% compared to the pre-injection control.