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Lesopitron dihydrochloride
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Catalog No. T11839Cas No. 132449-89-9
Alias E4424
Lesopitron dihydrochloride with IC50 of 125 nM in rat hippocampal membranes, is a full and selective 5-HT1A receptor agonist.
Lesopitron dihydrochloride
😃Good
Catalog No. T11839Alias E4424Cas No. 132449-89-9
Lesopitron dihydrochloride with IC50 of 125 nM in rat hippocampal membranes, is a full and selective 5-HT1A receptor agonist.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 25 mg | $1,520 | 1-2 weeks | |
| 50 mg | $1,980 | 1-2 weeks | |
| 100 mg | $2,500 | 1-2 weeks |
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Product Introduction
Bioactivity
Chemical Properties
| Description | Lesopitron dihydrochloride with IC50 of 125 nM in rat hippocampal membranes, is a full and selective 5-HT1A receptor agonist. |
| Targets&IC50 | 5-HT1A receptor:125 nM |
| In vitro | As expected of a full agonist at postsynaptic 5-HT1A receptors, Lesopitron (IC50=125 nM) inhibits forskolin-stimulated adenylate cyclase activity in rat hippocampal membranes to the same extent as 5-HT. Lesopitron inhibits the firing of serotoninergic neurons both in vitro (in brainstem slices, IC50=120 nM)[1].In vitro binding and autoradiographic studies with [3H]8-OH-DPAT and [3H]Lesopitron as radioligands confirm that Lesopitron binds to 5-HT1A receptors in the rat brain with a relatively high affinity (pKi=7.35). |
| In vivo | Administering lesopitron at a dose known to elicit anxiolytic behavior in rats (30 μg/kg, i.p.) significantly decreases serotonin (5-HT) levels in cortical perfusates to 45% of the baseline. Additionally, lesopitron effectively suppresses the activity of serotoninergic neurons in live conditions, specifically in chloral hydrate-anesthetized rats, with an ID50 of 35 μg/kg when administered intravenously[1][2]. |
| Alias | E4424 |
| Molecular Weight | 393.74 |
| Formula | C15H23Cl3N6 |
| Cas No. | 132449-89-9 |
| Relative Density. | 1.31g/cm3 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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