Lesopitron dihydrochloride  (Synonyms: E4424)

Lesopitron dihydrochloride is a full and selective 5-HT_1A receptor agonist with IC₅₀ of 125 nM in rat hippocampal membranes.

In vitro binding and autoradiographic studies with [³H]8-OH-DPAT and [³H]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 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

393.74

C₁₅H₂₃Cl₃N₆

132449-89-9

Solid

White to off-white

ClC1=CN(CCCCN2CCN(C3=NC=CC=N3)CC2)N=C1.[H]Cl.[H]Cl

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [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.  [Content Brief]

  [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.  [Content Brief]