CAS NO: | 192927-92-7 |
规格: | ≥98% |
包装 | 价格(元) |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
1g | 电议 |
Molecular Weight (MW) | 430.94 |
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Formula | C24H27FN2O2.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. |
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. |
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In Vivo | 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. |
Animal model | Animals |
Formulation & Dosage | 10, 20 mg/kg i.p. |
References | Eur J Pharmacol. 2004 Jun 16;493(1-3):85-93; Br J Pharmacol. 2012 Sep;167(2):356-67. |