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).

西域 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.). 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.

西域 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.). 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . 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]

  . 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]