LY310762192927-92-7赫澎生物說明書
發(fā)布時(shí)間：2016-09-13瀏覽次數(shù)：1177返回列表
" LY310762
分子式：C24H27FN2O2.HCl 分子量：430.94
產(chǎn)品描述
LY310762 是5-HT1D受體拮抗劑，Ki為249 nM,對(duì)5-HT1B 受體具有較低的親和力。
靶點(diǎn)
5-HT1D
IC50
0.2 μM (Ki)
體外研究
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.
體內(nèi)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.
溶解性
DMSO 0.4 mg/mL，水 <1 mg/mL，乙醇 <1 mg/mL
穩(wěn)定性
2年 -20°C粉狀，6月-80°C溶于DMSO"
分子式：C24H27FN2O2.HCl 分子量：430.94
產(chǎn)品描述
LY310762 是5-HT1D受體拮抗劑，Ki為249 nM,對(duì)5-HT1B 受體具有較低的親和力。
靶點(diǎn)
5-HT1D
IC50
0.2 μM (Ki)
體外研究
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.
體內(nèi)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.
溶解性
DMSO 0.4 mg/mL，水 <1 mg/mL，乙醇 <1 mg/mL
穩(wěn)定性
2年 -20°C粉狀，6月-80°C溶于DMSO"
