LY310762 free base
Based on 1 publication(s) in Google Scholar
LY310762 free base is a selective 5-HT1D receptor antagonist with a Ki value of 249 nM for the guinea pig receptor. LY310762 free base blocks presynaptic 5-HT1D autoreceptors and enhances potassium-stimulated [3H]5-HT outflow from guinea pig cortical slices. LY310762 free base abolishes the inhibitory effect of 5-CT (HY-135555)/L-694,247 (HY-101208) on sympathetic nerve-induced renal vasoconstriction mediated by prejunctional 5-HT1D receptors. LY310762 free base potentiates the increase in extracellular 5-HT concentration induced by Fluoxetine (HY-B0102). LY310762 free base is used in research related to depression and diabetic nephropathy.
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- CAS No.: 379215-96-0
- Formula: C24H27FN2O2
- Molecular Weight:394.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) LY310762 free base
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Biological Activity
Description
IC50 & Target
[1]|
5-HT1D Receptor 249 nM (Ki) |
In Vitro
LY310762 (1000 nM) shows preferential affinity for the guinea pig 5-HT1D receptor (Ki = 249 nM) over the guinea pig 5-HT1B receptor[1].
LY310762 potentiates potassium-stimulated [3H]5-HT release from guinea pig cortical slices with an EC50 of 31 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
LY310762 (1 mg/kg; i.v.) free base alone does not alter electrically stimulated-induced pressor responses in Fluoxetine-treated decerebrate rats[3].
LY310762 (1 mg/kg; i.v.) free base blocks the sympathoinhibitory effect of the 5-HT1D agonist L-694,247 (HY-101208), confirming the involvement of presynaptic 5-HT1D receptors in Fluoxetine-treated rats[3].
LY310762 (1 mg/kg; i.v.) free base, when combined with the 5-HT1A antagonist WAY-100,635, eliminates 5-HT-induced sympathoinhibition in Fluoxetine-treated rats, confirming the involvement of both presynaptic 5-HT1A and 5-HT1D receptors[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Dunkin Hartley (female, 350-400 g)[1]
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Dosage:10 mg/kg (after Fluoxetine); 10 mg/kg (alone)
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Administration:i.p.; single administration
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Result:Increased extracellular 5-HT levels from 312% to a maximum of 683% in fluoxetine-treated animals.
Increased basal 5-HT levels to a maximum of 258% when administered alone.
Chemical Information
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CAS No. 379215-96-0
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Molecular Weight 394.48
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Formula C24H27FN2O2
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SMILES
O=C(C1CCN(CC1)CCN2C(C(C)(C)C3=C2C=CC=C3)=O)C4=CC=C(C=C4)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)