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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 | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $1,520 | 1-2 weeks | 1-2 weeks | |
| 50 mg | $1,980 | 1-2 weeks | 1-2 weeks | |
| 100 mg | $2,500 | 1-2 weeks | 1-2 weeks |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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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]. |
| Synonyms | 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/Shipping at ambient temperature. |
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (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.
(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 μLSaline/PBS/ddH2O 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 μLSaline/PBS/ddH2O 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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