| Bioactivity | Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes. |
| Invitro | 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). 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 Vivo | Lesopitron inhibits the firing of serotoninergic neurons both in vivo (in chloral hydrate-anaesthetized rats, ID50=35 μg/kg i.v.)[1]. Lesopitron administered at a dose which induces anxiolytic behaviour in rats (30 μg/kg, i.p.) markedly reduces 5-HT levels (to 45% of the basal value) in cortical perfusates[2]. |
| Name | Lesopitron dihydrochloride |
| CAS | 132449-89-9 |
| Formula | C15H23Cl3N6 |
| Molar Mass | 393.74 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [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. [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. |
Lesopitron dihydrochloride
CAS: 132449-89-9 F: C15H23Cl3N6 W: 393.74
Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membra
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