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LY310762
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LY310762图片
CAS NO:192927-92-7
规格:≥98%
包装与价格:
包装价格(元)
10mg询价
25mg询价
50mg询价
100mg询价
250mg询价
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理化性质和储存条件
Molecular Weight (MW)430.94
FormulaC24H27FN2O2.HCl
CAS No.192927-92-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: <1 mg/mL
Water: <1 mg/mL
Ethanol: <1 mg/mL
SMILES Code O=C1N(CCN2CCC(C(C3=CC=C(F)C=C3)=O)CC2)C4=C(C=CC=C4)C1(C)C.[H]Cl
Synonyms LY310762; LY 310762; LY-310762; LY310762 HCl.
实验参考方法
In Vitro

In vitro activity: 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.


Kinase Assay: LY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, having a weaker affinity for 5-HT1B receptor.


Cell Assay: 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.

In VivoSystemic 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.
Animal modelAnimals
Formulation & Dosage10, 20 mg/kg i.p.
ReferencesEur J Pharmacol. 2004 Jun 16;493(1-3):85-93; Br J Pharmacol. 2012 Sep;167(2):356-67.
 
 
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