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| | lesopitron Basic information |
| Product Name: | lesopitron | | Synonyms: | Lesopitron (dihydrochloride);E4424;Lesopitron (dihydrochloride) (E4424) | | CAS: | 132449-89-9 | | MF: | C15H22Cl2N6 | | MW: | 357.28 | | EINECS: | | | Product Categories: | | | Mol File: | 132449-89-9.mol |  |
| | lesopitron Chemical Properties |
| Melting point | 194-197.5° | | storage temp. | Store at -20°C | | solubility | Soluble in DMSO | | form | Solid | | color | White to off-white |
| | lesopitron Usage And Synthesis |
| Biological Activity | Lesopitron dihydrochloride is a selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membrane. | | in vitro | In vitro binding and autoradiographic studies with [ 3 H]8-OH-DPAT and [ 3 H]Lesopitron as radioligands confirm that Lesopitron binds to 5 -HT 1A receptors in the rat brain with a relatively high affinity (pK i =7.35). As expected of a full agonist at postsynaptic 5-HT 1A < /sub> receptors, Lesopitron (IC 50 =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, IC 50 =120 nM). | | in vivo | Lesopitron inhibits the firing of serotoninergic neurons both in vivo (in chloral hydrate-anaesthetized rats, ID 50 =35 μg/kg iv). It administered at a dose which induces anxiolytic behaviour in rats (30 μg/kg, ip) markedly reduces 5-HT levels (to 45% of the basal value) in cortical perfusates. | | target | | 5-HT 1A Receptor 125 nM (IC 50 , in rat hippocampal membranes) | |
| | lesopitron Preparation Products And Raw materials |
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