192927-92-7
192927-92-7 structure
- Name: LY310762
- Chemical Name: 1-[2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl]-3,3-dimethylindol-2-one,hydrochloride
- CAS Number: 192927-92-7
- Molecular Formula: C24H28ClFN2O2
- Molecular Weight: 430.94300
- Catalog: Biochemical Inhibitor Neuronal Signaling 5-HT Receptor Antagonist
- Create Date: 2018-12-25 19:18:03
- Modify Date: 2024-01-02 12:40:56
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LY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, having a weaker affinity for 5-HT1B receptor.IC50 value: 249 nM (Ki) [1]Target: 5-HT1D in vitro: 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% [1]. LY310762 blocks the decreased EPSC amplitude induced by Sumatriptan [2]. 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 [1].
| Name | 1-[2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl]-3,3-dimethylindol-2-one,hydrochloride |
|---|---|
| Synonyms |
LY-310,762 hydrochloride
3,3-Dimethyl-1-{2-[4-(4-fluorobenzoyl)-1-piperidinyl]-1-ethyl}-1,3-dihydro-2H-indol-2-one hydrochloride LY310762 |
| Description | LY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, having a weaker affinity for 5-HT1B receptor.IC50 value: 249 nM (Ki) [1]Target: 5-HT1D in vitro: 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% [1]. LY310762 blocks the decreased EPSC amplitude induced by Sumatriptan [2]. 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 [1]. |
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| Related Catalog | |
| References |
| Molecular Formula | C24H28ClFN2O2 |
|---|---|
| Molecular Weight | 430.94300 |
| Exact Mass | 430.18200 |
| PSA | 40.62000 |
| LogP | 4.84970 |
| Appearance | white powder |
| Storage condition | Desiccate at RT |
| Water Solubility | DMSO: 10 mg/mL with heating, soluble |