Molecular Formula | C24H27O2N2FHCl |
Solubility | DMSO: 10mg/mL with heating, soluble |
Appearance | white powder |
Storage Condition | Sealed in dry,Room Temperature |
Use | LY310762 is a 5-HT1D receptor antagonist, Ki is 249 nM, and has a low affinity for 5-HT1B receptors. |
In vitro study | 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 vivo study | 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. |
Hazard Symbols | Xi - Irritant |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.321 ml | 11.603 ml | 23.205 ml |
5 mM | 0.464 ml | 2.321 ml | 4.641 ml |
10 mM | 0.232 ml | 1.16 ml | 2.321 ml |
5 mM | 0.046 ml | 0.232 ml | 0.464 ml |
Biological activity | LY310762 is a 5-HT1D receptor antagonist, Ki is 249 nM, and has a low affinity for 5-HT1B receptors. |
in vitro study | LY310762 has a higher affinity for the guineapig 5-HT1D receptor than for the 5-HT1B receptor. LY310762 potentiates the potassium-induced [3H]5-HT outflow from guineapig 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 vivo study | 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 one also significantly increases basic levels of 5-HT above vehicle controls, reaching a maximum of 258% compared to the pre-injection control. |
target | 5-HT 1D Receptor 249 nM (Ki) |