Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Lesopitron dihydrochloride with IC50 of 125 nM in rat hippocampal membranes, is a full and selective 5-HT1A receptor agonist.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 1,520.00 | |
50 mg | 6-8 weeks | $ 1,980.00 | |
100 mg | 6-8 weeks | $ 2,500.00 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Lesopitron dihydrochloride 132449-89-9 GPCR/G Protein Neuroscience 5-HT Receptor E4424 Lesopitron Dihydrochloride E-4424 Lesopitron E 4424 inhibitor inhibit