| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
LY310762 targets the 5-HT1D receptor. It is a selective antagonist with a Ki of 249 nM for the guinea pig 5-HT1D receptor. It has lower affinity for the 5-HT1B receptor; at 1,000 nM, it inhibits radiolabeled citalopram binding by only 32%.
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| ln Vitro |
In guinea pig cortical slices, LY310762 (0.01-1 µM) exhibits potassium-induced increase of [3H]5-HT efflux, with an EC50 value of 31 nM [1]. The decrease in excitatory postsynaptic potential (EPSC) caused by sumatriptan is largely, albeit not fully, blocked by LY310762 (10 µM) [3].
In vitro, LY310762 has higher affinity for the guinea pig 5-HT1D receptor than for the 5-HT1B receptor. It potentiates potassium-induced [³H]5-HT outflow from guinea pig cortical slices with an EC₅₀ of 30 nM. This suggests the compound acts as a 5-HT1D autoreceptor antagonist, enhancing serotonin release in the brain. |
| ln Vivo |
Fluoxetine, a selective serotonin reuptake inhibitor, produces extracellular 5-HT concentrations in vivo. LY310762 (10 mg/kg; i.p.; single dose) greatly boosts these concentrations [1]. In a rat model of phenylephrine infusion, LY310762 (1 mg/kg; intravenous injection; single dosage) completely eliminates the vasodilatory effects of 5-HT [2].
In vivo activity data for LY310762 is limited in publicly available sources. As a 5-HT1D receptor antagonist, it is used as a research tool to study the role of 5-HT1D receptors in serotoninergic neurotransmission. The compound's effects on serotonin release and behavior in animal models would be consistent with 5-HT1D autoreceptor blockade. |
| Enzyme Assay |
Non-cellular receptor binding assays for LY310762 involve radioligand displacement using membrane preparations expressing the 5-HT1D receptor. Membranes are incubated with a radiolabeled 5-HT1D ligand and varying concentrations of the test compound. Bound radioactivity is measured by filtration. Ki values are calculated from competition binding curves.
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| Cell Assay |
In vitro cellular experiments include measuring [³H]5-HT outflow from guinea pig cortical slices. Cortical slices are pre-loaded with [³H]5-HT, then superfused with buffer containing LY310762. Potassium-induced [³H]5-HT release is measured by liquid scintillation counting. EC₅₀ values are calculated from concentration-response curves.
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| Animal Protocol |
Animal/Disease Models: Dunkin Hartley guinea pig (female; 350-400 g, Harlan) [1].
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip) injection; Single Experimental Results:Further significant enhancement of 5-HT response to fluoxetine. Animal/Disease Models: Male Wistar rat (270-330 g; phenylephrine infusion rat model) [2]. Doses: 1 mg/kg Route of Administration: intravenous (iv) (iv)injection; Single Experimental Results:Complete elimination of the vasodilatory effect of 5-HT. In vivo animal studies for LY310762 have not been extensively reported. As a research tool, the compound may be used in behavioral and neurochemical studies to investigate 5-HT1D receptor function. Specific protocols would involve administration to rodents and assessment of serotonin-related behaviors or microdialysis measurements of extracellular serotonin. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for LY310762 is limited. The compound has a molecular weight of 430.94 g/mol (C₂₄H₂₈ClFN₂O₂). It is typically used in in vitro assays at concentrations in the nanomolar to micromolar range. Storage conditions: powder at -20°C for 3 years; in solution at -20°C for 6 months.
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| Toxicity/Toxicokinetics |
LY310762 is a research chemical; specific toxicity data is not available in publicly accessible sources. As a receptor antagonist, it should be handled with standard laboratory safety precautions. No LD₅₀ or specific toxicity information has been reported.
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| References |
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| Additional Infomation |
LY-310762 hydrochloride is a hydrochloride formed by the formal reaction of equimolar amounts of LY-310762 with hydrogen chloride. It is a potent and selective 5-hydroxytryptamine 1D (5-HT1D) receptor antagonist. It has the functions of a receptor modulator and a serotonergic antagonist. It contains LY-310762(1+).
LY310762 HCl is a selective 5-HT1D receptor antagonist used as a research tool. It has a Ki of 249 nM for the guinea pig 5-HT1D receptor and potentiates potassium-induced serotonin release (EC₅₀ = 30 nM). This product is for research purposes only and is not for human therapeutic use. |
| Molecular Formula |
C24H28CLFN2O2
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|---|---|
| Molecular Weight |
430.94
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| Exact Mass |
430.182
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| CAS # |
192927-92-7
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| PubChem CID |
11957576
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| Appearance |
White to off-white solid powder
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| LogP |
4.849
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
606
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl[H].FC1C([H])=C([H])C(=C([H])C=1[H])C(C1([H])C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])N2C3=C([H])C([H])=C([H])C([H])=C3C(C([H])([H])[H])(C([H])([H])[H])C2=O)C([H])([H])C1([H])[H])=O
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| Synonyms |
LY-310762; LY 310762; LY310762
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~18.33 mg/mL (~42.53 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.83 mg/mL (4.25 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 18.3 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.83 mg/mL (4.25 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 18.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.83 mg/mL (4.25 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3205 mL | 11.6025 mL | 23.2051 mL | |
| 5 mM | 0.4641 mL | 2.3205 mL | 4.6410 mL | |
| 10 mM | 0.2321 mL | 1.1603 mL | 2.3205 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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