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Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes. | [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) | | [IC 50]
5-HT1A Receptor: 125 nM (IC50, in rat hippocampal membranes) | [References]
[1] Haj-Dahmane S, et al. Interactions of Lesopitron (E-4424) with central 5-HT1A receptors: in vitro and in vivo studies in the rat. Eur J Pharmacol. 1994 Apr 1;255(1-3):185-96. DOI:10.1016/0014-2999(94)90097-3
[2] Ballarín M, et al. Effect of acute administration of the 5-HT1A receptor ligand, Lesopitron, on rat cortical 5-HT and dopamine turnover. Br J Pharmacol. 1994 Oct;113(2):425-30. DOI:10.1111/j.1476-5381.1994.tb17006.x |
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