Home Neuronal Signaling 5-HT Receptor antagonist LY310762 HCl

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LY310762 HCl 5-HT Receptor antagonist

Cat.No.S2669

LY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, having a weaker affinity for 5-HT1B receptor.
LY310762 HCl 5-HT Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 430.94

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Quality Control

Batch: S266901 4-Methylpyridine]24 mg/mL]true]DMSO]0.4 mg/mL]false]Water]Insoluble]false Purity: 98.74%
98.74

Chemical Information, Storage & Stability

Molecular Weight 430.94 Formula

C24H27FN2O2.HCl

 Storage (From the date of receipt)
CAS No. 192927-92-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1(C2=CC=CC=C2N(C1=O)CCN3CCC(CC3)C(=O)C4=CC=C(C=C4)F)C.Cl

Solubility

In vitro
Batch:

4-Methylpyridine : 24 mg/mL

DMSO : 0.4 mg/mL (0.92 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

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Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
5-HT1D [1]
249 nM(Ki)
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]
References

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